CAS Number103745-39-7
SynonymsFasudilum [inn-latin]; H-1077 dihydrochloride; 1-(5-Isoquinolinesulfonyl)-1H-hexahydro-1,4-diazepine,Dihydrochloride; 1-(5-ISOQUINOLINE-SULFONYL)-HOMOPIPERAZINE; HA 1077,DIHYDROCHLORIDE; 5-(1,4-Diazepan-1-ylsulfonyl)isoquinoline; HA-1077 DIHYDROCHLORIDE NOVEL VASODILATO R AGE; at877; 5-(1,4-DIAZEPAN-1-SULFONYL)ISOQUINOLINE; Fasudilum; 1-(5-Isoquinolinylsulfonyl)homopiperazine; Fasudil; MFCD00866182; hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine; 1-(5-isoquinolinesulphonyl)-homopiperazine; 1-(5-Isoquinolinesulphonyl)homopiperazine; N-(5-Isoquinolinesulfonyl)-1,4-perhydrodiazepine; (5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE
Molecular FormulaC14H17N3O2S
Molecular Weight364.29
Purity≥98 (HPLC)%
Density1.3±0.1 g/cm3
Boiling Point506.2±60.0 °C at 760 mmHg
Appearancesolid
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 103745-39-7 |
| Catalog No. | 2A-9010452 |
| Chinese Name | 法舒地尔 |
| Synonyms | Fasudilum [inn-latin]; H-1077 dihydrochloride; 1-(5-Isoquinolinesulfonyl)-1H-hexahydro-1,4-diazepine,Dihydrochloride; 1-(5-ISOQUINOLINE-SULFONYL)-HOMOPIPERAZINE; HA 1077,DIHYDROCHLORIDE; 5-(1,4-Diazepan-1-ylsulfonyl)isoquinoline; HA-1077 DIHYDROCHLORIDE NOVEL VASODILATO R AGE; at877; 5-(1,4-DIAZEPAN-1-SULFONYL)ISOQUINOLINE; Fasudilum; 1-(5-Isoquinolinylsulfonyl)homopiperazine; Fasudil; MFCD00866182; hexahydro-1-(5-isoquinolinylsulfonyl)-1H-1,4-diazepine; 1-(5-isoquinolinesulphonyl)-homopiperazine; 1-(5-Isoquinolinesulphonyl)homopiperazine; N-(5-Isoquinolinesulfonyl)-1,4-perhydrodiazepine; (5-ISOQUINOLINESULFONYL)HOMOPIPERAZINE |
| Molecular Formula | C14H17N3O2S |
| Molecular Weight | 364.29 |
| Purity | ≥98 (HPLC) |
| Density | 1.3±0.1 g/cm3 |
| Boiling Point | 506.2±60.0 °C at 760 mmHg |
| Appearance | solid |
| Water Solubility | H2O: >200 mg/mL |
| Storage Condition | Store at RT |
| Application | Fasudil is a potent inhibitor of ROCK1, PKA, PKC and MLCK with Ki values of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM respectively. |
| HTC | 2933990090 |
| MDL Number | MFCD00866182 |
| SMILES | [S](=O)(=O)(N3CCNCCC3)c1c2c(cncc2)ccc1 |
| InChI | 1S/C14H17N3O2S/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 |
| InChI Key | NGOGFTYYXHNFQH-UHFFFAOYSA-N |
| NACRES Code | NA.77 |
| UNSPSC | 12352200 |
| MSDS | msds/10452_1_103745_39_7.pdf |
| Use of | Fasudil is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively. Properties Name fasudil Synonym More Synonyms Fasudil Biological Activity Description Fasudil is a potent inhibitor of ROCK1, PKA, PKC, and MLCK with Ki of 0.33 μM, 1.0 μM, 9.3 μM and 55 μM, respectively. Related Catalog Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PKA Signaling Pathways >> Stem Cell/Wnt >> PKA Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK Signaling Pathways >> Stem Cell/Wnt >> ROCK Signaling Pathways >> TGF-beta/Smad >> ROCK Research Areas >> Cancer p160ROCK:0.33 μM (Ki) PKA:1 μM (Ki) PKC:9.3 μM (Ki) MLCK:55 μM (Ki) References [1]. Ono-Saito N, et al. H-series protein kinase inhibitors and potential clinical applications. Pharmacol Ther. 1999 May-Jun;82(2-3):123-31. [2]. Asano T, et al. Mechanism of action of a novel antivasospasm drug, HA1077. J Pharmacol Exp Ther. 1987 Jun;241(3):1033-40. [3]. Asano T, et al. Vasodilator actions of HA1077 in vitro and in vivo putatively mediated by the inhibition of protein kinase. Br J Pharmacol. 1989 Dec;98(4):1091-100. [4]. Negoro N, et al. The kinase inhibitor fasudil (HA-1077) reduces intimal hyperplasia through inhibiting migration and enhancing cell loss of vascular smooth muscle cells. Biochem Biophys Res Commun. 1999 Aug 19;262(1):211-5. [5]. Fukushima M, et al. Fasudil hydrochloride hydrate, a Rho-kinase (ROCK) inhibitor, suppresses collagen production and enhances collagenase activity in hepatic stellate cells. Liver Int. 2005 Aug;25(4):829-38. [6]. Zhang J, et al. Inhibition of the activity of Rho-kinase reduces cardiomyocyte apoptosis in heart ischemia/reperfusion via suppressing JNK-mediated AIF translocation. Clin Chim Acta. 2009 Mar;401(1-2):76-80. [7]. Sun X, et al. The selective Rho-kinase inhibitor Fasudil is protective and therapeutic in experimental autoimmune encephalomyelitis. J Neuroimmunol. 2006 Nov;180(1-2):126-34. [8]. Uehata M, et al. Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension. Nature. 1997 Oct 30;389(6654):990-4. Chemical & Physical Properties Molecular Formula C14H17N3O2S PSA 70.68000 Index of Refraction 1.622 InChIKey NGOGFTYYXHNFQH-UHFFFAOYSA-N Storage condition Store at RT Safety Information WGK Germany 3 RTECS HM4031166 HS Code 2933990090 Synthetic Route Total: 1 Page Homopiperazine CAS#:505-66-8 ISOQUINOLINE-5-... CAS#:84468-15-5 CAS#:103745-39-7 Literature: Asahi Kasei Kogyo Kabushiki Kaisha Patent: US5942505 A1, 1999 ; Homopiperazine CAS#:505-66-8 Isoquinoline-5-... CAS#:105627-79-0 CAS#:103745-39-7 Literature: Asahi Kasei Kogyo Kabushiki Kaisha Patent: US4678783 A1, 1987 ; US 4678783 A Precursor & DownStream Precursor 3 CAS#:505-66-8 Homopiperazine CAS#:84468-15-5 ISOQUINOLINE-5-... CAS#:105627-79-0 Isoquinoline-5-... DownStream 1 CAS#:105628-07-7 Fasudil Hydroch... |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Product name: Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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