Fasudil
Fasudil
CAS: 103745-39-7
Molecular Formula: C14H17N3O2S
Fasudil - Names and Identifiers
| Name | Fasudil |
| Synonyms | at877 Fasudil 103745-39-7 Fasudil HCI Fasudil Hydrchloride Fasudil Hydrochloride Injection (5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE 1-(5-Isoquinolinesulphonyl)homopiperazine 5-(1,4-Diazepan-1-ylsulfonyl)isoquinoline 1-(5-Isoquinolinylsulfonyl)homopiperazine 1-(5-ISOQUINOLINE-SULFONYL)-HOMOPIPERAZINE 5-(1,4-diazepan-4-ium-1-ylsulfonyl)isoquinoline N-(5-Isoquinolinesulfonyl)-1,4-perhydrodiazepine 5-(AZEPAN-4-YLSULFONYL)ISOQUINOLINE DIHYDROCHLORIDE hexahydro-1-(5-isoquinolinylsulfonyl)-1h-4-diazepine 5-(1,4-diazepan-1-ylsulfonyl)isoquinoline dihydrochloride isoquinoline, 5-[(hexahydro-1H-1,4-diazepin-1-yl)sulfonyl]- |
| CAS | 103745-39-7 |
| EINECS | 816-154-4 |
| InChI | InChI=1/C14H17N3O2S.2ClH/c18-20(19,17-9-2-6-15-8-10-17)14-4-1-3-12-11-16-7-5-13(12)14;;/h1,3-5,7,11,15H,2,6,8-10H2;2*1H |
Fasudil - Physico-chemical Properties
| Molecular Formula | C14H17N3O2S |
| Molar Mass | 291.37 |
| Density | 1.289±0.06 g/cm3(Predicted) |
| Boling Point | 506.2±60.0 °C(Predicted) |
| Flash Point | 284.9°C |
| Water Solubility | Soluble in water or DMSO |
| Solubility | H2O: >200mg/mL |
| Vapor Presure | 2.55E-12mmHg at 25°C |
| Appearance | solid |
| Color | white |
| pKa | 9.73±0.20(Predicted) |
| Storage Condition | Store at RT |
| Physical and Chemical Properties | Fasudil Hydrochloride: C14H17N3O2S? HCl. [105628-07-7]. Crystallization from water, melting point 220.5 °c. White crystalline powder, melting point 219.3 °c. The solubility in water can reach 2 × 10-2mol/L at Ph = 5.0~7.0. Acute toxicity LD50 mice, rats (mg/kg):67.5,59.9 intravenous; 124.5,123.2 subcutaneous; 273.9,335.0 oral. |
| In vivo study | Fasudil (intravenous injection; 0.01, 0.03, 0.1 and 0.3 mg/kg) decreases MBP and increases HR, VBF, CBF, RBF, and FBF. Fasudil (1.0 ng/mL) increases cardiac output. Fasudil via i.v. produces a significant fall in MBP, left ventricular systolic pressure and total peripheral resistance with an increase in HR and cardiac output, but without obvious effect on right atrial pressure, dP/dt or left ventricular minute work in dogs. Fasudil exhibits protectable effects on cardiovascular disease and reduces the activation of JNK and attenuates mitochondrial-nuclear translocation of AIF under ischemic injury. Fasudil (orally administration; 100 mg/kg/day) significantly reduces incidence and mean maximum clinical score of EAE in SJL/J mice immunized with PLP p139-151. Fasudil inhibits the proliferative response of splenocytes to the antigen in mice. Fasudil decreases inflammation, demyelination, axonal loss and APP positivein spinal cord of Fasudil-treated mice via p.o. administration. |
Fasudil - Risk and Safety
| WGK Germany | 3 |
| RTECS | HM4031166 |
| HS Code | 29334900 |
Fasudil - Reference Information
| overview | researchers said that a drug called fasudil can effectively block the feedback loop, protect synapses and memories in Alzheimer's animal models, and reduce the content of beta-amyloid in the brain. I hope that the research will enter the clinical stage as soon as possible, and I hope that Alzheimer's will completely disappear in our generation. |
| biological activity | Fasudil (HA-1077; AT877) is a non-specific RhoA/ROCK inhibitor, which also inhibits protein kinase. The Ki value of ROCK1 is 0.33 μM, the IC50 values of ROCK2 and PKA,PKC and PKG are 0.158 μM and 4.58 μM and 12.30 μM respectively, 1.650 μM. Fasudil is also an effective Ca2 + channel antagonist and vasodilator. |
| Cell Line: | Rat HSCs and human HSC-derived TWNT-4 cells Rat HSCs and human HSC-derived TWNT-4 cells |
| Concentration: | 50 μM; 100 μM 25 μM; 50 μM; 100 μM |
| Incubation Time: | 24 hours 24 hours |
| Result: | Suppressed the LPA-induced phosphorylation of ERK1/2, JNK and p38 MAPK by 60%, 70%,and 90%, respectively. Reduced the expression of type I collagen, a-SMA, and TIMP-1. |
| use | calcium antagonist. It is used for vasospasm after subarachnoid hemorrhage surgery. It can also be used for neuroprotection, acute cerebral artery embolism, chronic cerebral infarction and angina pectoris. |
| Production method | Isoquinoline is sulfonated with fuming sulfuric acid, and the generated sulfonic acid is converted into sulfonyl chloride, which is then reacted with diazo leather to obtain the product. |
Last Update：2024-04-09 20:49:11
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