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CAS No. :	393105-53-8
Formula :	C₂₄H₁₆F₃NO₄
M.W :	439.38
SMILES Code :	O=C(C1=CN(CC2=CC=CC=C2)C3=C1C=C(C4=CC=C(OC(F)(F)F)C=C4)C=C3)C(O)=O
Synonyms :	PAI-039; Tiplasinin
MDL No. :	MFCD09475615
InChI Key :	ODXQFEWQSHNQNI-UHFFFAOYSA-N
Pubchem ID :	6450819

GHS Pictogram:
Signal Word:	Danger
Hazard Statements:	H302+H312-H315-H318-H411
Precautionary Statements:	P264-P270-P273-P280-P301+P312+P330-P302+P352+P312-P305+P351+P338+P310-P332+P313-P391-P501
Class:	9
UN#:	3077
Packing Group:	Ⅲ

MDA-MB-231 cells	5 µM	17 hours	Inhibited PAI1 activity and reduced cell migration	Mol Cancer Res. 2019 May;17(5):1142-1154
SUM159 cells	5 µM	17 hours	Inhibited PAI1 activity and reduced cell migration	Mol Cancer Res. 2019 May;17(5):1142-1154
UROtsa cells	70.3 ± 0.1 µM (IC50)	24 hours	Inhibition of cellular proliferation and colony formation	Mol Cancer Ther. 2013 Dec;12(12):2697-708
UM-UC-14 cells	52.8 ± 1.6 µM (IC50)	24 hours	Inhibition of cellular proliferation and colony formation	Mol Cancer Ther. 2013 Dec;12(12):2697-708
T24 cells	43.7 ± 6.3 µM (IC50)	24 hours	Inhibition of cellular proliferation and colony formation	Mol Cancer Ther. 2013 Dec;12(12):2697-708
Newborn rat arterial smooth muscle cells (RASMCs)	10 µM	24 hours	To evaluate the effect of Tiplaxtinin on RASMCs apoptosis; results showed that Tiplaxtinin dose-dependently induced RASMCs apoptosis.	Cell Signal. 2015 May;27(5):923-33
HaCaT keratinocytes	10 µM	24 hours	To assess the effect of Tiplaxtinin on recombinant PAI-1-stimulated keratinocyte migration, results showed that Tiplaxtinin significantly attenuated PAI-1-induced motility.	Adv Wound Care (New Rochelle). 2015 Jun 1;4(6):321-328
Human lung microvascular endothelial cells	11 µM	4 hours	Tiplaxtinin significantly attenuated PAK-induced increase in protein permeability and RhoA activity in HMVEC monolayers.	Thorax. 2011 Sep;66(9):788-96
Bovine pulmonary arterial endothelial cells	11 µM	4 hours	Tiplaxtinin significantly attenuated PAK-induced increase in protein permeability and RhoA activity in BPAEC monolayers.	Thorax. 2011 Sep;66(9):788-96
Human umbilical vein endothelial cells (HUVECs)	10 μg/mL	4 hours	PAI-1 inhibits VEGF-induced VEGFR-2 phosphorylation	Arterioscler Thromb Vasc Biol. 2015 Jan;35(1):111-20
HUVEC cells	30 µM and 50 µM	6 hours	Inhibition of endothelial tube formation	Mol Cancer Ther. 2013 Dec;12(12):2697-708
A549 cells	50.00 µM	72 hours	PAI-039 induced apoptosis in A549 cells	J Natl Cancer Inst. 2012 Oct 3;104(19):1470-84
HT-1080 cells	50.00 µM	72 hours	PAI-039 induced apoptosis in HT-1080 cells	J Natl Cancer Inst. 2012 Oct 3;104(19):1470-84
HeLa cells	29.9 ± 3.1 µM (IC50)	72 hours	Inhibition of PAI-1 activity resulted in significant reduction in cellular proliferation	Mol Cancer Res. 2014 Mar;12(3):322-34
UM-UC-14 cells	52.8 ± 1.6 µM (IC50)	72 hours	Inhibition of PAI-1 activity resulted in significant reduction in cellular proliferation	Mol Cancer Res. 2014 Mar;12(3):322-34
T24 cells	43.7 ± 6.3 µM (IC50)	72 hours	Inhibition of PAI-1 activity resulted in significant reduction in cellular proliferation	Mol Cancer Res. 2014 Mar;12(3):322-34
KYSE-450 cells	100 ng/mL	72 hours	PAI-1 significantly promoted the proliferation and colony formation of KYSE-450 cells and reduced cisplatin-induced apoptosis.	Cell Death Dis. 2018 Jul 9;9(7):759
KYSE-30 cells	100 ng/mL	72 hours	PAI-1 significantly promoted the proliferation and colony formation of KYSE-30 cells and reduced cisplatin-induced apoptosis.	Cell Death Dis. 2018 Jul 9;9(7):759
HaCaT keratinocytes	10 µM	72 hours	To assess the effect of Tiplaxtinin on keratinocyte proliferation, results showed that Tiplaxtinin had no effect on cell cycle progression.	Adv Wound Care (New Rochelle). 2015 Jun 1;4(6):321-328

BALB/c nude mice	KYSE-30 cells and CAF CIS co-transplantation model	Oral gavage	10 mg/kg	Every 3 days for 3 weeks	Tiplaxtinin combined with cisplatin significantly inhibited tumor growth and enhanced the chemotherapeutic effects.	Cell Death Dis. 2018 Jul 9;9(7):759
Mice	APP/PS1 mouse model	Oral	12 mg/kg	Once daily for 8 weeks	To evaluate the effect of Tiplaxtinin on PbAc-induced CAA pathology. Results showed that Tiplaxtinin significantly reduced vascular amyloid deposition and improved cognitive function.	Environ Health Perspect. 2024 Oct;132(10):107004
Mice	Ins2WT/C96Y mice (model of adolescent-onset type 1 diabetes)	Oral	2 mg/kg	Twice daily for 5 days	Pharmacologic inhibition of PAI-1 with orally administered PAI-039 restored the early regenerative impairments in noninsulin-treated Ins2WT/C96Y mice. Results showed that PAI-039 treatment increased active uPA and MMP9 levels, reduced collagen content, and restored Myh3 expression.	Diabetes. 2011 Jul;60(7):1964-72
FVB/NJ mice	Carotid artery ligation model	Oral gavage	3 mg/kg	Once daily for 14 days	To evaluate the effect of Tiplaxtinin on neointima formation after carotid artery ligation; results showed that Tiplaxtinin significantly reduced neointimal thickening.	Cell Signal. 2015 May;27(5):923-33
Mice	Pseudomonas aeruginosa pneumonia model	Intraperitoneal injection	30 mg/kg	Twice, 1 h before and at the time of airspace instillation of P aeruginosa	Tiplaxtinin significantly attenuated P aeruginosa-induced increase in lung vascular permeability, but was associated with higher mortality at 24 h and decreased bacterial clearance in the lungs.	Thorax. 2011 Sep;66(9):788-96
C57BL/6J mice	Chronic allergic asthma model	Oral	5 mg/day	From 1 day before challenge until Day 36	Tiplaxtinin significantly decreased levels of active PAI-1 in BALF, reduced infiltration of inflammatory cells in the lungs of OVA-challenged mice, significantly attenuated goblet cell hyperplasia and collagen deposition, and effectively reduced methacholine-induced airway hyperresponsiveness.	Am J Respir Cell Mol Biol. 2012 Jun;46(6):842-6
LDL receptor-deficient mice	Western diet-induced obesity and metabolic syndrome model	Oral	5 mg/g of diet	Continued for 12-24 weeks	To evaluate the effects of PAI-039 on atherosclerosis and metabolic dysfunction, results showed PAI-039 significantly inhibited obesity and atherosclerosis formation, reduced macrophage accumulation and cell senescence	Arterioscler Thromb Vasc Biol. 2020 Jun;40(6):1479-1490
Mice	Lung fibrosis model	Intragastrically	5 mg/kg	Once daily for 21 days	Inhibition of PAI-1 mitigated lung fibrosis	Redox Biol. 2024 Apr;70:103038
BALB/c nu/nu mice	Human bladder cancer T24 xenograft model and human cervical cancer HeLa xenograft model	Oral gavage	5 mg/kg and 20 mg/kg	Once daily for 5 weeks	Inhibition of tumor growth, angiogenesis and induction of apoptosis	Mol Cancer Ther. 2013 Dec;12(12):2697-708
FVB/NJ mice	4 mm biopsy punch skin wound model	Topical administration	6 mg/kg	Once daily for 5 days	To evaluate the effect of Tiplaxtinin on skin wound healing, results showed that Tiplaxtinin significantly reduced wound closure and re-epithelialization, and decreased fibroblast proliferation and myofibroblast differentiation.	Adv Wound Care (New Rochelle). 2015 Jun 1;4(6):321-328

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CAS No.: 393105-53-8

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CAS No.: 393105-53-8

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Precautionary Statements-General

Prevention

Response

Storage

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Physical hazards

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Preparing Stock Solutions		1mg	5mg	10mg
Preparing Stock Solutions	1 mM 5 mM 10 mM	2.28mL 0.46mL 0.23mL	11.38mL 2.28mL 1.14mL	22.76mL 4.55mL 2.28mL
Dissolving Methods	Animal experiment Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn: in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day; The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound. Protocol 1 Protocol 2

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