Hydroxy-Fasudil


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

Description

Cas:105628-72-6

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:

5-(1,4-diazepan-1-ylsulfonyl)-2H-isoquinolin-1-one

 

InChi Key: 

ZAVGJDAFCZAWSZ-UHFFFAOYSA-N

 

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:

O=C1NC=CC2=C1C=CC=C2S(=O)(N3CCNCCC3)=O

 

 

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.

 

 

References

 

  1. Ray P, Wright J, Adam J, Boucharens S, Black D, Brown AR, Epemolu O, Fletcher D, Huggett M, Jones P, Laats S, Lyons A, de Man J, Morphy R, Sherborne B, Sherry L, Straten Nv, Westwood P, York M. Optimisation of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors. Bioorg Med Chem Lett. 2011 Feb 15;21(4):1084-8. doi: 10.1016/j.bmcl.2010.12.104. Epub 2010 Dec 28. PubMed PMID: 21251828.

 

  1. Maeda A, Yano T, Itoh Y, Kakumori M, Kubota T, Egashira N, Oishi R. Down-regulation of RhoA is involved in the cytotoxic action of lipophilic statins in HepG2 cells. Atherosclerosis. 2010 Jan;208(1):112-8. doi: 10.1016/j.atherosclerosis.2009.07.033. Epub 2009 Jul 23. PubMed PMID: 19683239.

 

  1. Huang L, Li Q, Li H, He Z, Cheng Z, Chen J, Guo L. Inhibition of intracellular Ca2+ release by a Rho-kinase inhibitor for the treatment of ischemic damage in primary cultured rat hippocampal neurons. Eur J Pharmacol. 2009 Jan 14;602(2-3):238-44. doi: 10.1016/j.ejphar.2008.11.053. Epub 2008 Dec 3. PubMed PMID: 19070614.

 

  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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