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MedKoo Cat#: 407104 | Name: Fasudil hydrochloride
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

Fasudil hydrochloride
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: 0.0000

Molecular Weight: 327.83

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
1g USD 250.00 Ready to ship
2g USD 425.00 Ready to ship
5g USD 750.00 Ready to ship
10g USD 1,250.00 2 weeks
20g USD 1,950.00 2 weeks
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Related CAS #
105628-07-7 (HCl) 103745-39-7 (free base) 186694-02-0 (hydrochloride hydrate)
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
More Info
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.
Product Data
Product Data
Certificate of Analysis
View CoA: current batch, Lot#LC80702
Safety Data Sheet (SDS)
View Safety Data Sheet (SDS)
Instruction
View handling instruction
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
Solvent mg/mL mM
Solubility
DMSO 31.0 94.56
Water 55.0 167.77
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 327.83 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
Formulation protocol:
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.
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.

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