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CAS No. :	105628-72-6
Formula :	C₁₄H₁₇N₃O₃S
M.W :	307.37
SMILES Code :	O=C1NC=CC2=C1C=CC=C2S(=O)(N3CCNCCC3)=O
Synonyms :	HA-1100
MDL No. :	MFCD01752417
InChI Key :	ZAVGJDAFCZAWSZ-UHFFFAOYSA-N
Pubchem ID :	3064778

GHS Pictogram:
Signal Word:	Warning
Hazard Statements:	H302-H315-H319-H335
Precautionary Statements:	P261-P305+P351+P338

Bovine aortic endothelial cells (BAEC)	0.1 to 100 μmol/L	48 hours	Hydroxyfasudil (0.1 to 100 μmol/L) did not affect eNOS promoter activity.	Stroke. 2005 Oct;36(10):2251-7
Human saphenous vein endothelial cells (HSVEC)	10 μmol/L	18 hours	Treatment with hydroxyfasudil increased eNOS mRNA expression to 156±20% (n=3, P<0.05).	Stroke. 2005 Oct;36(10):2251-7
Human umbilical vein endothelial cells (HUVEC)	10 μmol/L	18 hours	Treatment with hydroxyfasudil increased eNOS mRNA expression to 156±10% (n=3, P<0.05).	Stroke. 2005 Oct;36(10):2251-7
Human aortic endothelial cells (HAEC)	0.1 to 100 μmol/L	18 hours	Hydroxyfasudil increased eNOS mRNA and protein expression in a concentration-dependent manner, resulting in a 1.9- and 1.6-fold increase, respectively, at 10 μmol/L (P<0.05 for both). This correlated with a 1.5- and 2.3-fold increase in eNOS activity and NO production, respectively (P<0.05).	Stroke. 2005 Oct;36(10):2251-7
Bovine aortic endothelial cells	10 μmol/L	24 hours	Inhibited hyperglycemia-induced PAI-1 promoter activity	Circulation. 2005 Jun 21;111(24):3261-8
Human saphenous vein endothelial cells (HSVECs)	10 μmol/L	24 hours	Inhibited hyperglycemia-induced PAI-1 mRNA expression	Circulation. 2005 Jun 21;111(24):3261-8
bovine aortic endothelial cells (BAECs)	30 μmol/L	60 minutes	HF treatment led to a 4-fold increase in NO2 release, which was completely blocked by PI3-kinase inhibitor LY294002 or Akt inhibitor SH-5.	Arterioscler Thromb Vasc Biol. 2004 Oct;24(10):1842-7
human saphenous endothelial cells	1 to 100 μmol/L	5 to 15 minutes	HF produced a 1.8-fold increase in Akt serine-473 phosphorylation as early as 5 minutes, with a maximum 4.6-fold increase after 15 minutes.	Arterioscler Thromb Vasc Biol. 2004 Oct;24(10):1842-7
Primary mouse neurons	10 µM	15 minutes	Hydroxyfasudil significantly attenuated propofol-induced cleaved caspase-3 activation	Anesthesiology. 2012 Feb;116(2):352-61
Guinea pig left atrium	10^-7 – 10^-4 M		To evaluate the effect of Hydroxyfasudil on the contractile force of electrically paced guinea pig left atrium, showing no significant effect.	Br J Pharmacol. 2001 Dec;134(8):1724-30
Guinea pig right atrium	10^-7 – 10^-4 M		To evaluate the effect of Hydroxyfasudil on the spontaneous beating rate of guinea pig right atrium, showing no significant effect.	Br J Pharmacol. 2001 Dec;134(8):1724-30
Mouse motor neuron cells (NSC34)	0.3, 3, 30 nM	27 hours	To evaluate the protective effect of Hydroxyfasudil on SOD1G93A-induced motor neuron cell death. Results showed that at concentrations of 3-30 nM, Hydroxyfasudil reduced SOD1G93A-induced cell death in a concentration-dependent manner.	Br J Pharmacol. 2013 Sep;170(2):341-51
Human PKD1 cystic cell line (OX161)	1–30 μM	7 days	To test the efficacy of the ROCK inhibitor hydroxyfasudil in 3D cyst assays, results showed that hydroxyfasudil significantly reduced cyst area.	JCI Insight. 2020 Aug 20;5(16):e135385
rat basilar artery	3 μmol/L	60 mins hypoxia	ACh-induced endothelium-dependent relaxation was abolished during hypoxia and restored upon reoxygenation	J Cereb Blood Flow Metab. 2007 May;27(5):998-1009
mouse aorta	3 μmol/L	90 mins (including 60 mins hypoxia)	Partially restored endothelium-dependent ACh-induced relaxations during hypoxia, which was abolished by L-NAME, indicating eNOS mediation	J Cereb Blood Flow Metab. 2007 May;27(5):998-1009

Mice	Wild-type or eNOS-deficient mice	Intraperitoneal injection	1, 3, or 10 mg/kg/day（fasudil）	Once daily for 2 days	Fasudil increased cerebral blood flow to both ischemic and nonischemic brain areas, reduced cerebral infarct size by 33%, and improved neurologic deficit score by 37% (P<0.05). This correlated with inhibition of brain and vascular ROCK activity and increased eNOS expression and activity. The neuroprotective effects of fasudil were absent in eNOS-deficient mice.	Stroke. 2005 Oct;36(10):2251-7
Mice	Mesenteric ischemia-reperfusion injury model in wild-type and eNOS−/− mice	Intraperitoneal	10 mg/kg（fasudil）	Single dose 1 hour before ischemia	Fasudil decreased leukocyte recruitment and adhesion to the mesenteric endothelium after I/R injury in wild-type but not in eNOS?/? mice.	Arterioscler Thromb Vasc Biol. 2004 Oct;24(10):1842-7
Dogs	Myocardial ischemia model induced by left anterior descending coronary artery stenosis	Intravenous injection	0.1 and 0.3 mg/kg	30 minutes	To evaluate the effect of Hydroxyfasudil on ST-segment depression in a canine myocardial ischemia model, showing dose-dependent suppression of ST-segment depression and increased blood flow in the LAD-perfused endomyocardium region.	Br J Pharmacol. 2001 Dec;134(8):1724-30
Mice	SOD1G93A mutant mice (ALS model)	Administered via drinking water	30 and 100 mg/kg fasudil	From 5 weeks of age until the experimental endpoint	To evaluate the effect of Fasudil on disease progression and motor neuron loss in SOD1G93A mutant mice. Results showed that Fasudil delayed disease onset, prolonged survival time, and reduced motor neuron loss.	Br J Pharmacol. 2013 Sep;170(2):341-51
Mouse	Tetracycline-inducible kidney-specific Pkd1 mouse model (Pax8rtTA-TetO-Cre-Pkd1fl/fl)	Intraperitoneal injection	10 mg/kg/day	Once daily for 7 days	To test the inhibitory effect of hydroxyfasudil on cyst growth in vivo, results showed that treated mice had significantly reduced kidney weights and cystic indices, and increased cilia length.	JCI Insight. 2020 Aug 20;5(16):e135385
Mice (C57BL/6J and eNOS−/−)	Distal middle cerebral artery occlusion (dMCAO) model	Intraperitoneal or intravenous	10 mg/kg	Single dose, 60 mins before or 5 mins after dMCAO	In wild-type mice, hydroxyfasudil reduced the area of ischemic core and penumbra, but had no effect in eNOS?/? mice, indicating eNOS-dependent action	J Cereb Blood Flow Metab. 2007 May;27(5):998-1009

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CAS No.: 105628-72-6

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CAS No.: 105628-72-6

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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