Fasudil
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MedKoo CAT#: 584417

CAS#: 103745-39-7 (free base)

Description: Fasudil, a Rho-kinase inhibitor, has been shown to reduce portal venous pressure in cirrhotic rats.

Chemical Structure

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Fasudil
CAS# 103745-39-7 (free base)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 584417
Name: Fasudil
CAS#: 103745-39-7 (free base)
Chemical Formula: C14H17N3O2S
Exact Mass: 291.10
Molecular Weight: 291.369
Elemental Analysis: C, 57.71; H, 5.88; N, 14.42; O, 10.98; S, 11.00

Price and Availability

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10mg USD 485 2 weeks
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Related CAS #: 105628-07-7 (HCl)   103745-39-7 (free base)   186694-02-0 (hydrochloride hydrate)  

Synonym: Fasudil; AT 877; AT-877; AT877; HA 1077; HA-1077; HA1077

IUPAC/Chemical Name: 1H-1,4-Diazepine, hexahydro-1-(5-isoquinolinylsulfonyl)-

InChi Key: NGOGFTYYXHNFQH-UHFFFAOYSA-N

InChi Code: InChI=1S/C14H17N3O2S/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

SMILES Code: O=S(N1CCNCCC1)(C2=CC=CC3=C2C=CN=C3)=O

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

More Info:

Product Data:
Product Data
Instruction:
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Biological target: Fasudil (HA-1077; AT877), 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

Preparing Stock Solutions

The following data is based on the product molecular weight 291.37 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: 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. 2. 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.
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.

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1: Li YH, Liu CY, Zhang PJ, Yu JZ, Ji N, Yan YY, Feng L, Zhang HF, Xiao BG, Ma CG. [Effect of Fasudil on miroglia and astrocytes in experimental autoimmune encephalomyelitis mice]. Xi Bao Yu Fen Zi Mian Yi Xue Za Zhi. 2012 Dec;28(12):1242-5. Chinese. PubMed PMID: 23232512.

2: Zeng P, Pi RB, Li P, Chen RX, Lin LM, He H, Zhou SY. Fasudil hydrochloride, a potent ROCK inhibitor, inhibits corneal neovascularization after alkali burns in mice. Mol Vis. 2015 Jun 12;21:688-98. eCollection 2015. PubMed PMID: 26120273; PubMed Central PMCID: PMC4463969.

3: Fukuda T, Narahara Y, Kanazawa H, Matsushita Y, Kidokoro H, Itokawa N, Kondo C, Atsukawa M, Nakatsuka K, Sakamoto C. Effects of fasudil on the portal and systemic hemodynamics of patients with cirrhosis. J Gastroenterol Hepatol. 2014 Feb;29(2):325-9. doi: 10.1111/jgh.12360. PubMed PMID: 24033356.

4: Ma ZP, Jiang R, Cheng Y, Yang HF, Chen F. [Fasudil improves erectile function of hypertensive rats]. Zhonghua Nan Ke Xue. 2012 Jan;18(1):11-5. Chinese. PubMed PMID: 22295842.

5: Watanabe G, Yamaguchi S, Tomita S, Nishida Y. Fasudil Is an Effective Graft Vasodilator for Gastroepiploic Artery in Coronary Artery Bypass Grafting. Innovations (Phila). 2015 Jul-Aug;10(4):268-72; discussion 272. doi: 10.1097/IMI.0000000000000178. PubMed PMID: 26360979.

6: Tatenhorst L, Tönges L, Saal KA, Koch JC, Szegő ÉM, Bähr M, Lingor P. Rho kinase inhibition by fasudil in the striatal 6-hydroxydopamine lesion mouse model of Parkinson disease. J Neuropathol Exp Neurol. 2014 Aug;73(8):770-9. doi: 10.1097/NEN.0000000000000095. PubMed PMID: 25003236.

7: Wu N, Zhang X, Jia D. High dose fasudil preconditioning and postconditioning attenuate myocardial ischemia reperfusion injury in hypercholesterolemic rats. Mol Med Rep. 2014 Feb;9(2):560-6. doi: 10.3892/mmr.2013.1818. Epub 2013 Nov 20. PubMed PMID: 24271017.

8: Fava A, Wung PK, Wigley FM, Hummers LK, Daya NR, Ghazarian SR, Boin F. Efficacy of Rho kinase inhibitor fasudil in secondary Raynaud's phenomenon. Arthritis Care Res (Hoboken). 2012 Jun;64(6):925-9. doi: 10.1002/acr.21622. Epub 2012 Jan 24. PubMed PMID: 22275160; PubMed Central PMCID: PMC3343172.

9: Guo R, Su Y, Yan J, Sun H, Wu J, Liu W, Xu Y. Fasudil improves short-term echocardiographic parameters of diastolic function in patients with type 2 diabetes with preserved left ventricular ejection fraction: a pilot study. Heart Vessels. 2015 Jan;30(1):89-97. doi: 10.1007/s00380-013-0458-3. Epub 2014 Jan 5. PubMed PMID: 24390764.

10: Jiang X, Wang YF, Zhao QH, Jiang R, Wu Y, Peng FH, Xu XQ, Wang L, He J, Jing ZC. Acute hemodynamic response of infused fasudil in patients with pulmonary arterial hypertension: a randomized, controlled, crossover study. Int J Cardiol. 2014 Nov 15;177(1):61-5. doi: 10.1016/j.ijcard.2014.09.101. Epub 2014 Sep 28. PubMed PMID: 25499341.

11: Qi XJ, Ning W, Xu F, Dang HX, Fang F, Li J. Fasudil, an inhibitor of Rho-associated coiled-coil kinase, attenuates hyperoxia-induced pulmonary fibrosis in neonatal rats. Int J Clin Exp Pathol. 2015 Oct 1;8(10):12140-50. eCollection 2015. PubMed PMID: 26722398; PubMed Central PMCID: PMC4680343.

12: Nahar K, Absar S, Gupta N, Kotamraju VR, McMurtry IF, Oka M, Komatsu M, Nozik-Grayck E, Ahsan F. Peptide-coated liposomal fasudil enhances site specific vasodilation in pulmonary arterial hypertension. Mol Pharm. 2014 Dec 1;11(12):4374-84. doi: 10.1021/mp500456k. Epub 2014 Nov 4. PubMed PMID: 25333706; PubMed Central PMCID: PMC4255731.

13: Miyamoto C, Maehata Y, Ozawa S, Ikoma T, Kubota E, Izukuri K, Kato Y, Hata R, Lee MC. Fasudil suppresses fibrosarcoma growth by stimulating secretion of the chemokine CXCL14/BRAK. J Pharmacol Sci. 2012;120(3):241-9. Epub 2012 Oct 26. PubMed PMID: 23099322.

14: Guan SJ, Ma ZH, Wu YL, Zhang JP, Liang F, Weiss JW, Guo QY, Wang JY, Ji ES, Chu L. Long-term administration of fasudil improves cardiomyopathy in streptozotocin-induced diabetic rats. Food Chem Toxicol. 2012 Jun;50(6):1874-82. doi: 10.1016/j.fct.2012.03.006. Epub 2012 Mar 10. PubMed PMID: 22429817.

15: Satoh S, Kawasaki K, Hitomi A, Ikegaki I, Asano T. Fasudil protects cultured N1E-115 cells against lysophosphatidic acid-induced neurite retraction through inhibition of Rho-kinase. Brain Res Bull. 2011 Feb 1;84(2):174-7. doi: 10.1016/j.brainresbull.2010.11.013. Epub 2010 Nov 30. PubMed PMID: 21126559.

16: Kushiyama T, Oda T, Yamamoto K, Higashi K, Watanabe A, Takechi H, Uchida T, Oshima N, Sakurai Y, Miura S, Kumagai H. Protective effects of Rho kinase inhibitor fasudil on rats with chronic kidney disease. Am J Physiol Renal Physiol. 2013 Jun 1;304(11):F1325-34. doi: 10.1152/ajprenal.00447.2012. Epub 2013 Apr 3. PubMed PMID: 23552860.

17: Ma Z, Zhang J, Ji E, Cao G, Li G, Chu L. Rho kinase inhibition by fasudil exerts antioxidant effects in hypercholesterolemic rats. Clin Exp Pharmacol Physiol. 2011 Oct;38(10):688-94. doi: 10.1111/j.1440-1681.2011.05561.x. PubMed PMID: 21711379.

18: Watanabe G, Noda Y, Takagi T, Tomita S, Yamaguchi S, Kiuchi R. Fasudil is a superior vasodilator for the internal thoracic artery in coronary surgery. Ann Thorac Surg. 2013 Aug;96(2):543-7. doi: 10.1016/j.athoracsur.2013.04.039. Epub 2013 Jun 15. PubMed PMID: 23773733.

19: Iwabuchi S, Yokouchi T, Hayashi M, Sato K, Saito N, Hirata Y, Harashina J, Nakayama H, Akahata M, Ito K, Kimura H, Aoki K. Intra-arterial Administration of Fasudil Hydrochloride for Vasospasm Following Subarachnoid Haemorrhage: Experience of 90 Cases. Acta Neurochir Suppl. 2011;110(Pt 2):179-81. doi: 10.1007/978-3-7091-0356-2_33. PubMed PMID: 21125468.

20: Jin J, Peng C, Wu SZ, Chen HM, Zhang BF. Blocking VEGF/Caveolin-1 signaling contributes to renal protection of fasudil in streptozotocin-induced diabetic rats. Acta Pharmacol Sin. 2015 Jul;36(7):831-40. doi: 10.1038/aps.2015.23. Epub 2015 May 4. PubMed PMID: 25937636; PubMed Central PMCID: PMC4648118.