Catalog No. size PriceQuantity
M6860-2 2mg solid $148
M6860-10 10mg solid $611



Product Information

Hydroxy-Fasudil is a metabolite of Fasudil, acting as a potent Rho-kinase inhibitor and vasodilator.


Chemical Formula: C14H17N3O3S


Exact Mass: 307.0991


Molecular Weight: 307.368


Elemental Analysis: C, 54.71; H, 5.58; N, 13.67; O, 15.62; S, 10.43


Chemical Name:



InChi Key: 



InChi Code: InChI=1S/C14H17N3O3S/c18-14-12-3-1-4-13(11(12)5-7-16-14)21(19,20)17-9-2-6-15-8-10-17/h1,3-5,7,15H,2,6,8-10H2,(H,16,18)


Smiles Code:




Technical Data:


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

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


In Vitro:

Hydroxyfasudil is a ROCK inhibitor, with IC50s of 0.73 and 0.72 μM for ROCK1 and ROCK2, respectively. Hydroxyfasudil also less potently inhibits PKA, with an IC50 of 37 μM, 50-fold higher than those of the ROCKs. Hydroxyfasudil increases eNOS mRNA levels, with an EC50 value of 0.8 ± 0.3 μM. Hydroxyfasudil (0-100 μM) concentration-dependently increases eNOS activity and stimulates NO production in human aortic endothelial cells (HAEC). Hydroxyfasudil (10 μM) increases the half-life of eNOS mRNA from 13 to 16 hours, but does not affect eNOS promoter activity at concentrations from 0.1 to 100 μM.


In Vivo

Hydroxyfasudil (10 mg/kg, i.p.) significantly increases both the average and maximal voided volumes in SD rats. Hydroxyfasudil also significantly decreases the maximal detrusor pressure. Hydroxyfasudil (3 mg/kg, i.p) inhibits hypercontractility induced by norepinephrine in spontaneously hypertensive rats (SHRs). Furthermore, Hydroxyfasudil (3, 10 mg/kg, i.p) significantly ameliorates decreased penile cGMP contents in rats.





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  1. Hinderling PH, Karara AH, Tao B, Pawula M, Wilding I, Lu M. Systemic availability of the active metabolite hydroxy-fasudil after administration of fasudil to different sites of the human gastrointestinal tract. J Clin Pharmacol. 2007 Jan;47(1):19-25. PubMed PMID: 17192498.


  1. Scherer EQ, Arnold W, Wangemann P. Pharmacological reversal of endothelin-1 mediated constriction of the spiral modiolar artery: a potential new treatment for sudden sensorineural hearing loss. BMC Ear Nose Throat Disord. 2005 Nov 29;5:10. PubMed PMID: 16316469; PubMed Central PMCID: PMC1315339.


Products are for research use only. Not for human use.

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