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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
Structure of 530-78-9
*Storage: {[sel_prStorage]}
*Shipping: {[sel_prShipping]}
The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
Flufenamic Acid is a COX inhibitor and prevents formation of prostaglandins, binds to and reduce the activity of prostaglandin F synthase and activate TRPC6, it is a NSAID drug.
Synonyms: Flufenamic acid; CI-440; INF-1837
4.5
*For Research Use Only !
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Tonduru, Arun Kumar ; Maljaei, Seyed Hamed ; Adla, Santosh Kumar ; Anamea, Landry ; Tampio, Janne ; Kralova, Adela , et al.
Abstract: OATP1C1 (organic anion-transporting polypeptide 1C1) transports thyroid hormones, particularly thyroxine (T4), into human astrocytes. In this study, we investigated the potential of utilizing OATP1C1 to improve the delivery of anti-inflammatory drugs into glial cells. We designed and synthesized eight novel prodrugs by incorporating T4 and 3,5-diiodo-L-tyrosine (DIT) as promoieties to selected anti-inflammatory drugs. The prodrug uptake in OATP1C1-expressing human U-87MG glioma cells demonstrated higher accumulation with T4 promoiety compared to those with DIT promoiety or the parent drugs themselves. In silico models of OATP1C1 suggested dynamic binding for the prodrugs, wherein the pose changed from vertical to horizontal. The predicted binding energies correlated with the transport profiles, with T4 derivatives exhibiting higher binding energies when compared to prodrugs with a DIT promoiety. Interestingly, the prodrugs also showed utilization of oatp1a4/1a5/1a6 in mouse primary astrocytes, which was further supported by docking studies and a great potential for improved brain drug delivery.
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Purchased from AmBeed: 22071-15-4 ; 10236-47-2 ; 22204-53-1 ; 530-78-9 ; 5104-49-4 ; 5104-49-4 ; 22204-53-1
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| CAS No. : | 530-78-9 |
| Formula : | C14H10F3NO2 |
| M.W : | 281.23 |
| SMILES Code : | O=C(O)C1=CC=CC=C1NC2=CC=CC(C(F)(F)F)=C2 |
| Synonyms : |
Flufenamic acid; CI-440; INF-1837
|
| MDL No. : | MFCD00002422 |
| InChI Key : | LPEPZBJOKDYZAD-UHFFFAOYSA-N |
| Pubchem ID : | 3371 |
| GHS Pictogram: |
|
| Signal Word: | Danger |
| Hazard Statements: | H301-H315-H319 |
| Precautionary Statements: | P264-P270-P280-P301+P310+P330-P302+P352-P305+P351+P338-P332+P313-P337+P313-P405-P501 |
| Class: | 6.1 |
| UN#: | 2811 |
| Packing Group: | Ⅲ |
In Vitro:
|
Cell Line
|
Concentration | Treated Time | Description | References |
| Pig ventricular myocytes | 100 µM | >5 minutes | Investigate the effect of FFA on membrane ion currents, FFA caused an increase in currents with a reversal potential of +38 mV | Br J Pharmacol. 2010 Sep;161(2):416-29. |
| Mouse precursor osteoblasts (D1 cells) | 1.0 and 2.0 mg/mL | 21 days | Investigate the effect of FA on the proliferation and mineralization of D1 cells. Results showed that high concentrations of FA were not conducive to the proliferation of D1 cells but enhanced mineralization activity. | Pharmaceuticals (Basel). 2023 May 1;16(5):680. |
| Primary microglial cells | 100 µM | 24 hours | FA suppressed Syk activation, restored AMPK activity, and improved mitochondrial fission/fusion balance. | Aging Cell. 2022 May;21(5):e13623. |
| Primary microglial cells | 200 µM | 24 hours | FA inhibited microglial NLRP3 inflammasome activation by regulating Syk and AMPK, reducing ASC speck formation and IL-1β secretion. | Aging Cell. 2022 May;21(5):e13623. |
| Candida albicans SC5314 strain | ≥8 mg/L | 24 hours | Evaluate the preventive effect of FFA combined with FLU on Candida albicans biofilm formation, results showed that FFA ≥8 mg/L combined with FLU 32 mg/L could increase antifungal activity to 99% | Int J Antimicrob Agents. 2014 Jan;43(1):86-91. |
| Candida albicans mature biofilms | 1024 mg/L | 24 hours | Evaluate the therapeutic effect of FFA on mature Candida albicans biofilms, results showed that FFA concentrations of 1024 mg/L could reduce >85% of biofilm metabolic activity | Int J Antimicrob Agents. 2014 Jan;43(1):86-91. |
| Candida albicans biofilms | ≥512 mg/L | 24 hours | Evaluate the preventive effect of FFA on Candida albicans biofilm formation, results showed that FFA concentrations of ≥512 mg/L could prevent >80% of biofilm formation | Int J Antimicrob Agents. 2014 Jan;43(1):86-91. |
| Hippocampal pyramidal neurons | 200 µM | 30 ms | To investigate the effect of FFA on voltage-gated sodium currents, results showed that FFA inhibits ~50% of the sodium current with an IC50 of 189 μM. | J Physiol. 2010 Oct 15;588(Pt 20):3869-82. |
| Airway smooth muscle cells (ASMCs) | 100 µM | 330 seconds | Evaluate the relaxing effect of FFA on ASMCs, results showed FFA significantly reduced cell stiffness at 100 μM. | Theranostics. 2024 Feb 17;14(4):1744-1763. |
| Airway smooth muscle cells (ASMCs) | 1 µM | 330 seconds | Evaluate the relaxing effect of FFA on ASMCs, results showed FFA rapidly reduced cell stiffness at 1 μM. | Theranostics. 2024 Feb 17;14(4):1744-1763. |
| Rat supraoptic nucleus neuroendocrine cells | 0.3 mM–5 mM | 5–10 minutes | To examine the effects of flufenamic acid (FFA) on depolarizing afterpotentials (DAPs), results showed that FFA reversibly inhibited DAPs with an IC50 of 13.8 mM. | J Physiol. 2002 Dec 1;545(2):537-42. |
| Human adipose-derived stem cells (hASCs) | 25, 50, 100, 200 µM | 7 days | Low concentrations of FFA (25, 50, 100 μM) significantly enhanced osteogenic differentiation of hASCs, as evidenced by increased ALP activity and accelerated mineralization; 200 μM FFA inhibited osteogenic differentiation. The optimal concentration was 50 μM. | Stem Cell Res Ther. 2019 Jul 19;10(1):213. |
| Human bone marrow-derived mesenchymal stem cells (hBMMSCs) | 25, 50, 100, 200 µM | 7 days | Low concentrations of FFA (25, 50, 100 μM) significantly enhanced osteogenic differentiation of hBMMSCs, as evidenced by increased ALP activity and accelerated mineralization; 200 μM FFA inhibited osteogenic differentiation. The optimal concentration was 50 μM. | Stem Cell Res Ther. 2019 Jul 19;10(1):213. |
| HEK293 cells | 2.49 µM (IC50) | 72 hours | Assessed cytotoxicity, showing lower toxicity towards HEK293 cells, indicating selectivity for cancer cells over non-cancerous cells | Angew Chem Int Ed Engl. 2024 Feb 5;63(6):e202317940. |
| HMLER-shEcad cells | 0.18 µM (IC50) | 72 hours | Assessed cytotoxicity, showing sub-micromolar toxicity towards HMLER-shEcad cells, with 24-fold and 31-fold higher potency than salinomycin and cisplatin, respectively | Angew Chem Int Ed Engl. 2024 Feb 5;63(6):e202317940. |
| HMLER cells | 0.27 µM (IC50) | 72 hours | Assessed cytotoxicity, showing sub-micromolar toxicity towards HMLER cells | Angew Chem Int Ed Engl. 2024 Feb 5;63(6):e202317940. |
In Vivo:
|
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
| Mice | 4T1 metastatic triple-negative breast cancer model | Intraperitoneal injection | 10 mg/kg | Three times a week for 14 days | Evaluated in vivo antitumour efficacy, showing significant inhibition of tumour growth and reduced lung metastasis without inducing significant systemic toxicity | Angew Chem Int Ed Engl. 2024 Feb 5;63(6):e202317940. |
| C57BL/6 mice and Thy1-GFP-M mice | T10 spinal cord contusion model | Intraperitoneal injection | 12.5 mg/kg | Once daily for one week | FFA inhibited Trpm4 expression, reduced secondary hemorrhage and capillary fragmentation, and promoted angiogenesis; inhibited the expression of MMP-2 and MMP-9, attenuated BSCB disruption; decreased the activation of microglia/macrophages, reduced lesion size and cavity formation, protected motor neurons, and improved locomotor function. | Theranostics. 2018 Jul 30;8(15):4181-4198 |
| C57BL/6J mice | Cardiac arrest/cardiopulmonary resuscitation model | Intraperitoneal injection | 12.5 mg/kg | Once daily for one week | FFA improved survival and neurologic outcome after CA/CPR in mice, reduced neuropathological injuries, attenuated brain edema, lessened the leakage of IgG and Evans blue dye, restored tight junction protein expression, and promoted microglia/macrophages from the pro-inflammatory subtype toward the anti-inflammatory subtype. | J Neuroinflammation. 2022 Sep 1;19(1):214 |
| BALB/c mice | Ovalbumin-induced asthmatic Mice model | Inhalation | 2, 4, 8 μg | Single administration | Evaluate the effect of FFA on airway resistance in vivo, results showed FFA significantly reduced airway resistance at 8 μg. | Theranostics. 2024 Feb 17;14(4):1744-1763. |
| ADLPAPT mice | Alzheimer's disease model | Intraperitoneal injection | 5 mg/kg | Once daily for 8 weeks | FA inhibited microglial NLRP3 inflammasome activation, significantly reducing amyloid plaques and phosphorylated tau pathology while improving cognitive function. | Aging Cell. 2022 May;21(5):e13623. |
| BALB/C nude mice | Heterotopic bone formation model | Subcutaneous implantation | 50 μM | Single implantation, lasting 8 weeks | 50 μM FFA promoted osteogenic differentiation of hBMMSCs in vivo, as evidenced by more newly formed bone and collagen organization. | Stem Cell Res Ther. 2019 Jul 19;10(1):213. |
Clinical Trial:
| NCT Number | Conditions | Phases | Recruitment | Completion Date | Locations |
| NCT03238612 | Influenza A | Phase 2 | Recruiting | October 31, 2020 | Hong Kong ... More >> Ivan Hung Recruiting Hong Kong, Hong Kong Contact: Ivan FN Hung, MD FRCP 852 22554049 ivanfn@gmail.com Sub-Investigator: Kelvin To, MD FRCPath Sub-Investigator: KY Yuen, MD FRCPath Less << |
| Bio Calculators | ||||
| Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.56mL 0.71mL 0.36mL |
17.78mL 3.56mL 1.78mL |
35.56mL 7.11mL 3.56mL |
|
Tags: Flufenamic acid | COX Inhibitor | AMPK | Potassium Channel | Chloride Channel | Calcium Channel |Cyclooxygenase | AMP-activated protein kinase | MPK activation | ion channel modulation | TEAD2-YAP | Cl− Channels | Ca2+ channels | Ca channels | 530-78-9
Precautionary Statements-General | |
| Code | Phrase |
| P101 | If medical advice is needed,have product container or label at hand. |
| P102 | Keep out of reach of children. |
| P103 | Read label before use |
Prevention | |
| Code | Phrase |
| P201 | Obtain special instructions before use. |
| P202 | Do not handle until all safety precautions have been read and understood. |
| P210 | Keep away from heat/sparks/open flames/hot surfaces. - No smoking. |
| P211 | Do not spray on an open flame or other ignition source. |
| P220 | Keep/Store away from clothing/combustible materials. |
| P221 | Take any precaution to avoid mixing with combustibles |
| P222 | Do not allow contact with air. |
| P223 | Keep away from any possible contact with water, because of violent reaction and possible flash fire. |
| P230 | Keep wetted |
| P231 | Handle under inert gas. |
| P232 | Protect from moisture. |
| P233 | Keep container tightly closed. |
| P234 | Keep only in original container. |
| P235 | Keep cool |
| P240 | Ground/bond container and receiving equipment. |
| P241 | Use explosion-proof electrical/ventilating/lighting/equipment. |
| P242 | Use only non-sparking tools. |
| P243 | Take precautionary measures against static discharge. |
| P244 | Keep reduction valves free from grease and oil. |
| P250 | Do not subject to grinding/shock/friction. |
| P251 | Pressurized container: Do not pierce or burn, even after use. |
| P260 | Do not breathe dust/fume/gas/mist/vapours/spray. |
| P261 | Avoid breathing dust/fume/gas/mist/vapours/spray. |
| P262 | Do not get in eyes, on skin, or on clothing. |
| P263 | Avoid contact during pregnancy/while nursing. |
| P264 | Wash hands thoroughly after handling. |
| P265 | Wash skin thouroughly after handling. |
| P270 | Do not eat, drink or smoke when using this product. |
| P271 | Use only outdoors or in a well-ventilated area. |
| P272 | Contaminated work clothing should not be allowed out of the workplace. |
| P273 | Avoid release to the environment. |
| P280 | Wear protective gloves/protective clothing/eye protection/face protection. |
| P281 | Use personal protective equipment as required. |
| P282 | Wear cold insulating gloves/face shield/eye protection. |
| P283 | Wear fire/flame resistant/retardant clothing. |
| P284 | Wear respiratory protection. |
| P285 | In case of inadequate ventilation wear respiratory protection. |
| P231 + P232 | Handle under inert gas. Protect from moisture. |
| P235 + P410 | Keep cool. Protect from sunlight. |
Response | |
| Code | Phrase |
| P301 | IF SWALLOWED: |
| P304 | IF INHALED: |
| P305 | IF IN EYES: |
| P306 | IF ON CLOTHING: |
| P307 | IF exposed: |
| P308 | IF exposed or concerned: |
| P309 | IF exposed or if you feel unwell: |
| P310 | Immediately call a POISON CENTER or doctor/physician. |
| P311 | Call a POISON CENTER or doctor/physician. |
| P312 | Call a POISON CENTER or doctor/physician if you feel unwell. |
| P313 | Get medical advice/attention. |
| P314 | Get medical advice/attention if you feel unwell. |
| P315 | Get immediate medical advice/attention. |
| P320 | |
| P302 + P352 | IF ON SKIN: wash with plenty of soap and water. |
| P321 | |
| P322 | |
| P330 | Rinse mouth. |
| P331 | Do NOT induce vomiting. |
| P332 | IF SKIN irritation occurs: |
| P333 | If skin irritation or rash occurs: |
| P334 | Immerse in cool water/wrap n wet bandages. |
| P335 | Brush off loose particles from skin. |
| P336 | Thaw frosted parts with lukewarm water. Do not rub affected area. |
| P337 | If eye irritation persists: |
| P338 | Remove contact lenses, if present and easy to do. Continue rinsing. |
| P340 | Remove victim to fresh air and keep at rest in a position comfortable for breathing. |
| P341 | If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
| P342 | If experiencing respiratory symptoms: |
| P350 | Gently wash with plenty of soap and water. |
| P351 | Rinse cautiously with water for several minutes. |
| P352 | Wash with plenty of soap and water. |
| P353 | Rinse skin with water/shower. |
| P360 | Rinse immediately contaminated clothing and skin with plenty of water before removing clothes. |
| P361 | Remove/Take off immediately all contaminated clothing. |
| P362 | Take off contaminated clothing and wash before reuse. |
| P363 | Wash contaminated clothing before reuse. |
| P370 | In case of fire: |
| P371 | In case of major fire and large quantities: |
| P372 | Explosion risk in case of fire. |
| P373 | DO NOT fight fire when fire reaches explosives. |
| P374 | Fight fire with normal precautions from a reasonable distance. |
| P376 | Stop leak if safe to do so. Oxidising gases (section 2.4) 1 |
| P377 | Leaking gas fire: Do not extinguish, unless leak can be stopped safely. |
| P378 | |
| P380 | Evacuate area. |
| P381 | Eliminate all ignition sources if safe to do so. |
| P390 | Absorb spillage to prevent material damage. |
| P391 | Collect spillage. Hazardous to the aquatic environment |
| P301 + P310 | IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician. |
| P301 + P312 | IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell. |
| P301 + P330 + P331 | IF SWALLOWED: Rinse mouth. Do NOT induce vomiting. |
| P302 + P334 | IF ON SKIN: Immerse in cool water/wrap in wet bandages. |
| P302 + P350 | IF ON SKIN: Gently wash with plenty of soap and water. |
| P303 + P361 + P353 | IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower. |
| P304 + P312 | IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell. |
| P304 + P340 | IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing. |
| P304 + P341 | IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing. |
| P305 + P351 + P338 | IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. |
| P306 + P360 | IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes. |
| P307 + P311 | IF exposed: call a POISON CENTER or doctor/physician. |
| P308 + P313 | IF exposed or concerned: Get medical advice/attention. |
| P309 + P311 | IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician. |
| P332 + P313 | IF SKIN irritation occurs: Get medical advice/attention. |
| P333 + P313 | IF SKIN irritation or rash occurs: Get medical advice/attention. |
| P335 + P334 | Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages. |
| P337 + P313 | IF eye irritation persists: Get medical advice/attention. |
| P342 + P311 | IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician. |
| P370 + P376 | In case of fire: Stop leak if safe to Do so. |
| P370 + P378 | In case of fire: |
| P370 + P380 | In case of fire: Evacuate area. |
| P370 + P380 + P375 | In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion. |
| P371 + P380 + P375 | In case of major fire and large quantities: Evacuate area. Fight fire remotely due to the risk of explosion. |
Storage | |
| Code | Phrase |
| P401 | |
| P402 | Store in a dry place. |
| P403 | Store in a well-ventilated place. |
| P404 | Store in a closed container. |
| P405 | Store locked up. |
| P406 | Store in corrosive resistant/ container with a resistant inner liner. |
| P407 | Maintain air gap between stacks/pallets. |
| P410 | Protect from sunlight. |
| P411 | |
| P412 | Do not expose to temperatures exceeding 50 oC/ 122 oF. |
| P413 | |
| P420 | Store away from other materials. |
| P422 | |
| P402 + P404 | Store in a dry place. Store in a closed container. |
| P403 + P233 | Store in a well-ventilated place. Keep container tightly closed. |
| P403 + P235 | Store in a well-ventilated place. Keep cool. |
| P410 + P403 | Protect from sunlight. Store in a well-ventilated place. |
| P410 + P412 | Protect from sunlight. Do not expose to temperatures exceeding 50 oC/122oF. |
| P411 + P235 | Keep cool. |
Disposal | |
| Code | Phrase |
| P501 | Dispose of contents/container to ... |
| P502 | Refer to manufacturer/supplier for information on recovery/recycling |
Physical hazards | |
| Code | Phrase |
| H200 | Unstable explosive |
| H201 | Explosive; mass explosion hazard |
| H202 | Explosive; severe projection hazard |
| H203 | Explosive; fire, blast or projection hazard |
| H204 | Fire or projection hazard |
| H205 | May mass explode in fire |
| H220 | Extremely flammable gas |
| H221 | Flammable gas |
| H222 | Extremely flammable aerosol |
| H223 | Flammable aerosol |
| H224 | Extremely flammable liquid and vapour |
| H225 | Highly flammable liquid and vapour |
| H226 | Flammable liquid and vapour |
| H227 | Combustible liquid |
| H228 | Flammable solid |
| H229 | Pressurized container: may burst if heated |
| H230 | May react explosively even in the absence of air |
| H231 | May react explosively even in the absence of air at elevated pressure and/or temperature |
| H240 | Heating may cause an explosion |
| H241 | Heating may cause a fire or explosion |
| H242 | Heating may cause a fire |
| H250 | Catches fire spontaneously if exposed to air |
| H251 | Self-heating; may catch fire |
| H252 | Self-heating in large quantities; may catch fire |
| H260 | In contact with water releases flammable gases which may ignite spontaneously |
| H261 | In contact with water releases flammable gas |
| H270 | May cause or intensify fire; oxidizer |
| H271 | May cause fire or explosion; strong oxidizer |
| H272 | May intensify fire; oxidizer |
| H280 | Contains gas under pressure; may explode if heated |
| H281 | Contains refrigerated gas; may cause cryogenic burns or injury |
| H290 | May be corrosive to metals |
Health hazards | |
| Code | Phrase |
| H300 | Fatal if swallowed |
| H301 | Toxic if swallowed |
| H302 | Harmful if swallowed |
| H303 | May be harmful if swallowed |
| H304 | May be fatal if swallowed and enters airways |
| H305 | May be harmful if swallowed and enters airways |
| H310 | Fatal in contact with skin |
| H311 | Toxic in contact with skin |
| H312 | Harmful in contact with skin |
| H313 | May be harmful in contact with skin |
| H314 | Causes severe skin burns and eye damage |
| H315 | Causes skin irritation |
| H316 | Causes mild skin irritation |
| H317 | May cause an allergic skin reaction |
| H318 | Causes serious eye damage |
| H319 | Causes serious eye irritation |
| H320 | Causes eye irritation |
| H330 | Fatal if inhaled |
| H331 | Toxic if inhaled |
| H332 | Harmful if inhaled |
| H333 | May be harmful if inhaled |
| H334 | May cause allergy or asthma symptoms or breathing difficulties if inhaled |
| H335 | May cause respiratory irritation |
| H336 | May cause drowsiness or dizziness |
| H340 | May cause genetic defects |
| H341 | Suspected of causing genetic defects |
| H350 | May cause cancer |
| H351 | Suspected of causing cancer |
| H360 | May damage fertility or the unborn child |
| H361 | Suspected of damaging fertility or the unborn child |
| H361d | Suspected of damaging the unborn child |
| H362 | May cause harm to breast-fed children |
| H370 | Causes damage to organs |
| H371 | May cause damage to organs |
| H372 | Causes damage to organs through prolonged or repeated exposure |
| H373 | May cause damage to organs through prolonged or repeated exposure |
Environmental hazards | |
| Code | Phrase |
| H400 | Very toxic to aquatic life |
| H401 | Toxic to aquatic life |
| H402 | Harmful to aquatic life |
| H410 | Very toxic to aquatic life with long-lasting effects |
| H411 | Toxic to aquatic life with long-lasting effects |
| H412 | Harmful to aquatic life with long-lasting effects |
| H413 | May cause long-lasting harmful effects to aquatic life |
| H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
Sorry,this product has been discontinued.
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