Hydroxyfasudil HCl


Catalog No. size PriceQuantity
M6872-2 2mg solid $122
M6872-10 10mg solid $488

Description

Cas:155558-32-0 (HCl)

Product Information

Hydroxyfasudil, aslo known as HA1100, is a cell-permeable hydroxylated metabolite of HA-1077, is a potent inhibitor of Rho-associated kinase (ROCK) (Ki = 150 nM). Hydroxyfasudil alleviates demyelination through the inhibition of MOG antibody and microglia activation in cuprizone mouse model.

 

Chemical Formula: C14H18ClN3O3S

 

Molecular Weight: 343.826

 

Elemental Analysis: C, 48.91; H, 5.28; Cl, 10.31; N, 12.22; O, 13.96; S, 9.32

 

Related CAS #: 155558-32-0 (HCl)   105628-72-6 (free base)    

 

Synonym: 

 

HA-1100 HCl

HA 1100

Hydroxyfasudil hydrochloride

 

Chemical Name:

1-(1-Hydroxy-5-isoquinolinesulfonyl)homopiperazine hydrochloride

 

InChi Key:

XWWFOUVDVJGNNG-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C14H17N3O3S.ClH/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);1H

 

Smiles Code:

O=S(N1CCNCCC1)(C2=CC=CC3=C2C=CN=C3O)=O.[H]Cl

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: >3 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 hydrochloride 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. Wang J, Sui RX, Miao Q, Wang Q, Song LJ, Yu JZ, Li YH, Xiao BG, Ma CG. Hydroxyfasudil alleviates demyelination through the inhibition of MOG antibody and microglia activation in cuprizone mouse model. Clin Immunol. 2019 Apr;201:35-47. doi: 10.1016/j.clim.2019.01.006. Epub 2019 Jan 17. PubMed PMID: 30660624.

 

  1. Antolín AA, Mestres J. Dual Inhibitors of PARPs and ROCKs. ACS Omega. 2018 Oct 31;3(10):12707-12712. doi: 10.1021/acsomega.8b02337. Epub 2018 Oct 5. PubMed PMID: 30411017; PubMed Central PMCID: PMC6210072.

 

  1. Bozkurt A, Budak H, Erol HS, Can S, Mercantepe T, Akin Y, Ozbey I, Cankaya M, Halici MB, Coban TA. A novel therapeutics agent: antioxidant effects of hydroxylfasudil on rat kidney and liver tissues in a protamine sulphate-induced cystitis rat model; preliminary results. Artif Cells Nanomed Biotechnol. 2018;46(sup2):9-14. doi: 10.1080/21691401.2018.1449120. Epub 2018 Mar 9. PubMed PMID: 29523028.

 

  1. Vieira GM, Roberto GM, Lira RC, Engel EE, Tone LG, Brassesco MS. Prognostic value and functional role of ROCK2 in pediatric Ewing sarcoma. Oncol Lett. 2018 Feb;15(2):2296-2304. doi: 10.3892/ol.2017.7571. Epub 2017 Dec 8. PubMed PMID: 29434937; PubMed Central PMCID: PMC5777092.

 

  1. Cheng CI, Lee YH, Chen PH, Lin YC, Chou MH, Kao YH. Cobalt chloride induces RhoA/ROCK activation and remodeling effect in H9c2 cardiomyoblasts: Involvement of PI3K/Akt and MAPK pathways. Cell Signal. 2017 Aug;36:25-33. doi: 10.1016/j.cellsig.2017.04.013. Epub 2017 Apr 21. PubMed PMID: 28435089.

 

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

 

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