Fasudil hydrochloride
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MedKoo CAT#: 407104

CAS#: 105628-07-7 (HCl)

Description: Fasudil, also known as HA-1077, is a potent Rho-kinase inhibitor and vasodilator. Since it was discovered, it has been used for the treatment of cerebral vasospasm, which is often due to subarachnoid hemorrhage, as well as to improve the cognitive decline seen in stroke victims. It has been found to be effective for the treatment of pulmonary hypertension. It was demonstrated in February 2009 that fasudil could also be used to enhance memory and improve the prognosis of Alzheimers patients. It is approved for use in Japan and China.


Chemical Structure

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Fasudil hydrochloride
CAS# 105628-07-7 (HCl)

Theoretical Analysis

MedKoo Cat#: 407104
Name: Fasudil hydrochloride
CAS#: 105628-07-7 (HCl)
Chemical Formula: C14H18ClN3O2S
Exact Mass:
Molecular Weight: 327.827
Elemental Analysis: C, 51.29; H, 5.53; Cl, 10.81; N, 12.82; O, 9.76; S, 9.78

Price and Availability

Size Price Availability Quantity
1.0g USD 250.0 Same day
2.0g USD 450.0 Same day
5.0g USD 750.0 Same day
10.0g USD 1250.0 2 weeks
20.0g USD 1950.0 2 weeks
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Related CAS #: 105628-07-7 (HCl)   103745-39-7 (free base)    

Synonym: HA-1077; HA1077; HA 1077; HA-1077 HCl; Fasudil hydrochloride.

IUPAC/Chemical Name: 5-((1,4-diazepan-1-yl)sulfonyl)isoquinoline hydrochloride

InChi Key: LFVPBERIVUNMGV-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H17N3O2S.ClH/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;1H

SMILES Code: O=S(C1=CC=CC2=C1C=CN=C2)(N3CCNCCC3)=O.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Product Data:

Certificate of Analysis:

Safety Data Sheet (SDS):

Biological target: Fasudil Hydrochloride (HA-1077 Hydrochloride; AT877 Hydrochloride), is a nonspecific RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an Ki of 0.33 μM for ROCK1, IC50s of 0.158 μM and 4.58 μM, 12.30 μM, 1.650 μM for ROCK2 and PKA, PKC, PKG, respectively.
In vitro activity: Fasudil (100 microM) inhibited cell spreading, the formation of stress fibers, and expression of alpha-SMA with concomitant suppression of cell growth, although it did not induce apoptosis. Fasudil inhibited phosphorylation of ERK1/2, JNK, and p38. Treatment with fasudil suppressed the production and transcription of collagen and TIMP, stimulated the production and transcription of MMP-1, and enhanced collagenase activity. Reference: Liver Int. 2005 Aug;25(4):829-38. https://doi.org/10.1111/j.1478-3231.2005.01142.x
In vivo activity: Ischemia followed by reperfusion caused a significant increase in Rho-kinase, c-Jun NH2-terminal kinase (JNK) and apoptosis-inducing factor (AIF) activity. Administration of fasudil, an inhibitor of Rho-kinase, decreased myocardial infarction size from 59.89+/-3.83% to 38.62+/-2.66% (P<0.05) and cell apoptosis from 32.78+/-5.1% to 17.05+/-4.2% (P<0.05). Western blot analysis showed that administration of fasudil reduced the activation of JNK and attenuated mitochondrial-nuclear translocation of AIF. Reference: Clin Chim Acta. 2009 Mar;401(1-2):76-80. https://linkinghub.elsevier.com/retrieve/pii/S0009-8981(08)00560-3

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 31.0 94.56
Water 55.0 167.77

Preparing Stock Solutions

The following data is based on the product molecular weight 327.827 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
In vitro protocol: 1. Fukushima M, Nakamuta M, Kohjima M, Kotoh K, Enjoji M, Kobayashi N, Nawata H. 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. doi: 10.1111/j.1478-3231.2005.01142.x. PMID: 15998434.
In vivo protocol: 1. Zhang J, Li XX, Bian HJ, Liu XB, Ji XP, Zhang Y. 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. doi: 10.1016/j.cca.2008.11.016. Epub 2008 Nov 24. PMID: 19061880.

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1: Shi J, Wei L. Rho kinases in cardiovascular physiology and pathophysiology: the effect of fasudil. J Cardiovasc Pharmacol. 2013 Oct;62(4):341-54. doi: 10.1097/FJC.0b013e3182a3718f. Review. PubMed PMID: 23921309; PubMed Central PMCID: PMC3884946.

2: Chen M, Liu A, Ouyang Y, Huang Y, Chao X, Pi R. Fasudil and its analogs: a new powerful weapon in the long war against central nervous system disorders? Expert Opin Investig Drugs. 2013 Apr;22(4):537-50. doi: 10.1517/13543784.2013.778242. Epub 2013 Mar 5. Review. PubMed PMID: 23461757.

3: Raja SG. Evaluation of clinical efficacy of fasudil for the treatment of pulmonary arterial hypertension. Recent Pat Cardiovasc Drug Discov. 2012 Aug;7(2):100-4. Review. PubMed PMID: 22670803.

4: Kitazono T. [Fasudil hydrochloride]. Nihon Rinsho. 2006 Oct 28;64 Suppl 7:617-21. Review. Japanese. PubMed PMID: 17461215.

5: Ishida T, Takanashi Y, Kiwada H. Safe and efficient drug delivery system with liposomes for intrathecal application of an antivasospastic drug, fasudil. Biol Pharm Bull. 2006 Mar;29(3):397-402. Review. PubMed PMID: 16508135.

6: Shibuya M, Asano T, Sasaki Y. Effect of Fasudil HCl, a protein kinase inhibitor, on cerebral vasospasm. Acta Neurochir Suppl. 2001;77:201-4. Review. PubMed PMID: 11563286.

7: Seto M, Takuwa Y, Sasaki Y. [The molecular mechanism of vasospasm and the attenuation by fasudil]. Nihon Yakurigaku Zasshi. 1999 Oct;114 Suppl 1:66P-70P. Review. Japanese. PubMed PMID: 10629857.



Additional Information

ROCK is an enzyme that plays an important role in mediating vasoconstriction and vascular remodeling in the pathogenesis of PH. ROCK induces vasoconstriction by phosphorylating the myosin-binding subunit of myosin light chain (MLC) phosphatase, thus decreasing MLC phosphatase activity and enhancing vascular smooth muscle contraction.