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CAS No. :	51987-99-6
Formula :	C₈H₆N₄OS
M.W :	206.22
SMILES Code :	O=C(NC1=NN=CS1)C2=CN=CC=C2
MDL No. :	MFCD00708771
InChI Key :	AGEGZHOPKZFKBP-UHFFFAOYSA-N
Pubchem ID :	4173511

GHS Pictogram:
Signal Word:	Warning
Hazard Statements:	H302
Precautionary Statements:	P280-P305+P351+P338

Astrocytes in rat supraoptic nucleus brain slices	10 µM	10 minutes	To investigate the inhibitory effect of TGN-020 on VP neuronal activity under hyposmotic challenge. Results showed that TGN-020 blocked the rebound increase in firing rate of VP neurons induced by HOC.	Acta Physiol (Oxf). 2021 Jul;232(3):e13672
Primary astrocytes	10 µM	24 or 48 hours	TGN020 changed cell morphology, diminished cell proliferation and suppressed astrocyte activation	Neurotherapeutics. 2024 Mar;21(2):e00306
Astrocytes in brain slices	10 µM	30 minutes	To study the effect of TGN-020 on GFAP and AQP4 expression under OGD conditions, results showed that TGN-020 could partially block the OGD-induced decrease in GFAP expression.	ASN Neuro. 2020 Jan-Dec;12:1759091420960550

Wistar rats	Streptozotocin-induced diabetic rat model	Intravitreal injection	0.02 mg/μL	Single injection, evaluated after 48 hours	To investigate the effects of TGN-020 on diabetic retinal edema. Results showed that TGN-020 suppressed the expression of VEGF and AQP4 in diabetic rat retinas, reduced retinal thickness and vascular leakage.	Int J Mol Sci. 2020 Mar 27;21(7):2324
Wistar rats	Middle cerebral artery occlusion (MCAO) model	Microinjection into the SON	10 μM	Single injection, observation for 8 hours	To study the effect of TGN-020 on MCAO-induced brain injury, results showed that TGN-020 could reduce MCAO-induced increases in pERK1/2 and AQP4 expression and decrease in GFAP expression.	ASN Neuro. 2020 Jan-Dec;12:1759091420960550
C57BL/6 mice	MPTP-induced PD mouse model	Intraperitoneal injection	100 mg/kg	Single administration	To evaluate the inhibitory effect of TGN020 on AQP4 in the MPTP-induced PD mouse model and its impact on neuropathology. Results showed that TGN020 inhibited AQP4 expression, exacerbated astrogliosis, and further aggravated PD pathological manifestations.	J Adv Res. 2024 Feb;56:125-136
Male C57BL/6 mice	Collagenase-induced intracranial hemorrhage model	Intraperitoneal injection	100 mg/kg	30 minutes before each exosomes administration, continued until the end of the experiment	To evaluate the effect of TGN020 as an AQP4-specific inhibitor on H-Exo's promotion of intracranial lymphatic drainage and neurological recovery. Results showed that TGN020 successfully reversed H-Exo's ability to promote solute efflux and neurological recovery, indicating that H-Exo's effects depend on intact GLS function.	Fluids Barriers CNS. 2025 Apr 14;22(1):37
Sprague-Dawley rats	T13 spinal cord hemisection model	Intrathecal injection	15 μg	Once a day for 7 consecutive days	TGN020 suppressed astrocyte activation, attenuated the development and maintenance of below-level CNP and promoted motor function recovery in vivo	Neurotherapeutics. 2024 Mar;21(2):e00306
Male Sprague-Dawley rats	Hyposmotic challenge model	Intraperitoneal injection	20 mL/kg	Single injection, lasting 10-30 minutes	To investigate the regulatory effect of TGN-020 on VP neuronal activity under hyposmotic challenge in vivo. Results showed that TGN-020 blocked the rebound increase in firing rate of VP neurons induced by hyposmotic challenge.	Acta Physiol (Oxf). 2021 Jul;232(3):e13672
Mice	C57BL/6 mice	Superfusion	20 μM	Continuous superfusion	TGN-020 was used to block AQP4 water channels to investigate its effect on light-evoked ECS α decrease. The results showed that TGN-020 had no effect on the light-evoked ECS α decrease.	Glia. 2022 Oct;70(10):1927-1937
C57BL/6J mice	Traumatic brain injury (TBI) model	Intraperitoneal injection	200 mg/kg	Every 24 hours until mice sacrifice	To evaluate the effect of TGN020 on BBB integrity and astrocyte function after TBI, results showed that TGN020 significantly downregulated AQP4 expression, optimized BBB integrity and astrocyte function	Int J Biol Sci. 2022 Jan 1;18(1):441-458
Sprague-Dawley rats	Middle cerebral artery occlusion (MCAO) model	Intraperitoneal injection	200 mg/kg	Single dose, administered 10 minutes after MCAO	To evaluate the effect of TGN-020 on brain edema and infarct volume after cerebral ischemia. Results showed that the TGN-020-treated group exhibited reduced infarct volumes and brain swelling at 1 day and 14 days after stroke, and better neurological recovery at 14 days.	Front Immunol. 2022 May 3;13:870029
C57/BL6 male mice	Middle cerebral artery occlusion (MCAO) model	Intraperitoneal injection	200 mg/kg	Single dose, lasting 48 hours	TGN-020 alleviates inflammation and apoptosis after cerebral ischemia-reperfusion injury by improving glymphatic function and inhibiting the ERK1/2 pathway.	Mol Neurobiol. 2024 Feb;61(2):1175-1186
C57BL/6J mice	Traumatic brain injury (TBI) model	Intraperitoneal injection	200 mg/kg	22 consecutive days	TGN-020 significantly reduced the water content in the hippocampus and cortex of TBI mice and improved cognitive abilities.	Heliyon. 2023 Nov 13;9(11):e22035
Mice	RTg4510 transgenic mice	Intraperitoneal injection	250 mg/kg	Single dose	To assess the effect of AQP4 inhibitor TGN-020 on CSF-ISF exchange and tau clearance in the brain. Results showed that TGN-020 significantly inhibited CSF-ISF exchange and tau clearance.	Brain. 2020 Aug 1;143(8):2576-2593
Mice	Chronic cerebral hypoperfusion model	Intraperitoneal injection	250 mg/kg	Single dose	Inhibits AQP4 polarity, disrupts the polarized distribution of AQP4 in astrocytes, thereby inhibiting glymphatic system function.	Neurosci Bull. 2022 Feb;38(2):181-199
BALB/c mice	DSS-induced experimental colitis model	Intraperitoneal injection	250 mg/kg	Once daily for 7 days	TGN-020 treatment effectively alleviated DSS-induced experimental colitis in mice and reduced apoptosis of colon epithelial cells	Cell Death Discov. 2022 Jun 28;8(1):298
C57BL/6 mice	Perioperative neurocognitive disorder (PND) mouse model	Intraperitoneal injection	250 mg/kg	Single dose	TGN-020 further aggravated AQP4 depolarization in the hippocampus of PND mice, leading to exacerbated neuroinflammation and cognitive dysfunction.	J Cereb Blood Flow Metab. 2024 Aug;44(8):1450-1466
Mice	Traumatic brain injury (TBI) model	Intraperitoneal injection	250 mg/kg	Single dose	TGN-020, a specific inhibitor of AQP4, was used for pharmacological blocking of the glymphatic system. The results showed that TGN-020 effectively blocked the glymphatic transport of RITC-dextran.	CNS Neurosci Ther. 2023 Dec;29(12):3876-3888
Male C57BL/6J mice	Healthy mice	Intraperitoneal injection	400 mg/kg	Single dose, experiments conducted 30 minutes post-injection	To investigate the effect of AQP4 inhibitor TGN-020 on Aβ40 clearance. Results showed that TGN-020 significantly increased perivascular accumulation of Aβ40, indicating impaired perivascular clearance of Aβ40 due to AQP4 inhibition.	Mol Neurobiol. 2020 Nov;57(11):4720-4734
Mice	Tau propagation model	Intraperitoneal injection	50 mg/kg	3 doses/week for 10 weeks	To investigate the impact of long-term AQP4 inhibition on tau propagation, results showed TGN-020 treatment increased tau aggregation and transhemispheric spread in the brain.	Alzheimers Res Ther. 2024 Apr 5;16(1):71

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CAS No.: 51987-99-6

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CAS No.: 51987-99-6

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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