Hydroxyfasudil HCl
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MedKoo CAT#: 333182

CAS#: 155558-32-0 (HCl)

Description: 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.


Price and Availability

Size
Price

50mg
USD 190
500mg
USD 1250
5g
USD 6450
Size
Price

100mg
USD 350
1g
USD 2150
Size
Price

200mg
USD 650
2g
USD 3750

Hydroxyfasudil HCl, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 333182
Name: Hydroxyfasudil HCl
CAS#: 155558-32-0 (HCl)
Chemical Formula: C14H18ClN3O3S
Exact Mass:
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: Hydroxyfasudil HCl, HA-1100 HCl; HA1100; HA 1100; Hydroxyfasudil hydrochloride

IUPAC/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).

Harmonized System Code:
2934990300


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.

2: 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.

3: 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.

4: 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.

5: 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.

6: Tratsiakovich Y, Kiss A, Gonon AT, Yang J, Sjöquist PO, Pernow J. Inhibition of Rho kinase protects from ischaemia-reperfusion injury via regulation of arginase activity and nitric oxide synthase in type 1 diabetes. Diab Vasc Dis Res. 2017 May;14(3):236-245. doi: 10.1177/1479164116687935. Epub 2017 Feb 9. PubMed PMID: 28183205.

7: Mao Z, Wu Y, Li Q, Wang X, Liu Y, Di X. Aldehyde oxidase-dependent species difference in hepatic metabolism of fasudil to hydroxyfasudil. Xenobiotica. 2018 Feb;48(2):170-177. doi: 10.1080/00498254.2017.1292016. Epub 2017 Mar 2. PubMed PMID: 28166443.

8: Huang L, Li Q, Wen R, Yu Z, Li N, Ma L, Feng W. Rho-kinase inhibitor prevents acute injury against transient focal cerebral ischemia by enhancing the expression and function of GABA receptors in rats. Eur J Pharmacol. 2017 Feb 15;797:134-142. doi: 10.1016/j.ejphar.2017.01.021. Epub 2017 Jan 18. PubMed PMID: 28109911.

9: Chen Y, Huang W, Jiang W, Wu X, Ye B, Zhou X. HIV-1 Tat Regulates Occludin and Aβ Transfer Receptor Expression in Brain Endothelial Cells via Rho/ROCK Signaling Pathway. Oxid Med Cell Longev. 2016;2016:4196572. doi: 10.1155/2016/4196572. Epub 2016 Aug 2. PubMed PMID: 27563375; PubMed Central PMCID: PMC4985576.

10: Nishimiya K, Matsumoto Y, Uzuka H, Ogata T, Hirano M, Shindo T, Hasebe Y, Tsuburaya R, Shiroto T, Takahashi J, Ito K, Shimokawa H. Beneficial Effects of a Novel Bioabsorbable Polymer Coating on Enhanced Coronary Vasoconstricting Responses After Drug-Eluting Stent Implantation in Pigs in Vivo. JACC Cardiovasc Interv. 2016 Feb 8;9(3):281-291. doi: 10.1016/j.jcin.2015.09.041. PubMed PMID: 26847120.

11: Akin Y, Bozkurt A, Erol HS, Halici M, Celebi F, Kapakin KA, Gulmez H, Ates M, Coban A, Nuhoglu B. Impact of Rho-Kinase Inhibitor Hydroxyfasudil in Protamine Sulphate Induced Cystitis Rat Bladder. Low Urin Tract Symptoms. 2015 May;7(2):108-14. doi: 10.1111/luts.12058. Epub 2014 Apr 17. PubMed PMID: 26663691.

12: Baba I, Egi Y, Utsumi H, Kakimoto T, Suzuki K. Inhibitory effects of fasudil on renal interstitial fibrosis induced by unilateral ureteral obstruction. Mol Med Rep. 2015 Dec;12(6):8010-20. doi: 10.3892/mmr.2015.4467. Epub 2015 Oct 21. PubMed PMID: 26498136; PubMed Central PMCID: PMC4758322.

13: Holmström F, Shimizu S, Shimizu T, Higashi Y, Martin DT, Honda M, Saito M. Protective effect of hydroxyfasudil, a Rho kinase inhibitor, on ventral prostatic hyperplasia in the spontaneously hypertensive rat. Prostate. 2015 Nov;75(15):1774-82. doi: 10.1002/pros.23063. Epub 2015 Aug 19. PubMed PMID: 26286428.

14: Nishimiya K, Matsumoto Y, Shindo T, Hanawa K, Hasebe Y, Tsuburaya R, Shiroto T, Takahashi J, Ito K, Ishibashi-Ueda H, Yasuda S, Shimokawa H. Association of Adventitial Vasa Vasorum and Inflammation With Coronary Hyperconstriction After Drug-Eluting Stent Implantation in Pigs In Vivo. Circ J. 2015;79(8):1787-98. doi: 10.1253/circj.CJ-15-0149. Epub 2015 Jun 1. PubMed PMID: 26027445.

15: Médard G, Pachl F, Ruprecht B, Klaeger S, Heinzlmeir S, Helm D, Qiao H, Ku X, Wilhelm M, Kuehne T, Wu Z, Dittmann A, Hopf C, Kramer K, Kuster B. Optimized chemical proteomics assay for kinase inhibitor profiling. J Proteome Res. 2015 Mar 6;14(3):1574-86. doi: 10.1021/pr5012608. Epub 2015 Feb 20. PubMed PMID: 25660469.

16: Yayama K, Sasahara T, Ohba H, Funasaka A, Okamoto H. Orthovanadate-induced vasocontraction is mediated by the activation of Rho-kinase through Src-dependent transactivation of epidermal growth factor receptor. Pharmacol Res Perspect. 2014 Apr;2(2):e00039. doi: 10.1002/prp2.39. Epub 2014 Apr 1. PubMed PMID: 25505586; PubMed Central PMCID: PMC4184709.

17: Moreau S, DaSilva JN, Valdivia A, Fernando P. N-[(11)C]-methyl-hydroxyfasudil is a potential biomarker of cardiac hypertrophy. Nucl Med Biol. 2015 Feb;42(2):192-7. doi: 10.1016/j.nucmedbio.2014.09.008. Epub 2014 Sep 30. PubMed PMID: 25451216.

18: Cheng CI, Chen PH, Lin YC, Kao YH. High glucose activates Raw264.7 macrophages through RhoA kinase-mediated signaling pathway. Cell Signal. 2015 Feb;27(2):283-92. doi: 10.1016/j.cellsig.2014.11.012. Epub 2014 Nov 14. PubMed PMID: 25446262.

19: Kiss A, Tratsiakovich Y, Gonon AT, Fedotovskaya O, Lanner JT, Andersson DC, Yang J, Pernow J. The role of arginase and rho kinase in cardioprotection from remote ischemic perconditioning in non-diabetic and diabetic rat in vivo. PLoS One. 2014 Aug 20;9(8):e104731. doi: 10.1371/journal.pone.0104731. eCollection 2014. PubMed PMID: 25140754; PubMed Central PMCID: PMC4139318.

20: Huang L, Zhao LB, Yu ZY, He XJ, Ma LP, Li N, Guo LJ, Feng WY. Long-term inhibition of Rho-kinase restores the LTP impaired in chronic forebrain ischemia rats by regulating GABAA and GABAB receptors. Neuroscience. 2014 Sep 26;277:383-91. doi: 10.1016/j.neuroscience.2014.07.015. Epub 2014 Jul 19. PubMed PMID: 25050822.