Fasudil mesylate (Synonyms: HA-1077 mesylate; AT-877 mesylate)

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Fasudil (HA-1077; AT877) mesylate is a nonspecific and orally active RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an K_i 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. Fasudil mesylate is also a potent Ca²⁺ channel antagonist and vasodilator.

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Fasudil mesylate Chemical Structure

CAS No. : 1001206-62-7

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Other In-stock Forms of Fasudil mesylate:

Fasudil Hydrochloride

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15 Publications Citing Use of MCE Fasudil mesylate

: Fasudil mesylate purchased from MedChemExpress. Usage Cited in: Biomed Rep. 2015 May;3(3):361-364. [Abstract]; RhoA and ROCK2 upregulation in the rat hippocampus is involved in memory dysfunction induced by postnatal exposure of Sevoflurane. The expression of RhoA, ROCK2 and cleaved caspase-3 (Cl-Csp3) in the hippocampus of the S3 group significantly increased, compared to that of the C group (P<0.05). There is no difference of the level of RhoA, ROCK2 and Cl-Csp3 between the C and S1 groups (P>0.05). ROCK2 inhibitor Fasudil hydrochloride in the F group clearly decreases the expression of ROCK2 and Cl-Cs

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Description	Fasudil (HA-1077; AT877) mesylate is a nonspecific and orally active RhoA/ROCK inhibitor and also has inhibitory effect on protein kinases, with an K_i 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. Fasudil mesylate is also a potent Ca²⁺ channel antagonist and vasodilator^[1]^[2]^[3]^[4]^[5]^[6].
IC₅₀ & Target	Ki: 0.33 μM (ROCK1)^[1] IC50: 0.158 μM (ROCK2), 4.58 μM (PKA), 12.30 μM (PKC), 1.650 μM (PKG)^[1]
Molecular Weight	387.47
Formula	C₁₅H₂₁N₃O₅S₂
CAS No.	1001206-62-7
SMILES	CS(O)(=O)=O.O=S(C1=CC=CC2=C1C=CN=C2)(N3CCNCCC3)=O
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (279 KB) Handling Instructions (2659 KB)
References	[1]. Chen M, et al. Fasudil and its analogs: a new powerful weapon in the long war against central nervous system disorders? Expert Opin Investig Drugs. 2013 Apr;22(4):537-50. [Content Brief] [2]. Huang XN, et al. The effects of fasudil on the permeability of the rat blood-brain barrier and blood-spinal cordbarrier following experimental autoimmune encephalomyelitis. J Neuroimmunol. 2011 Oct 28;239(1-2):61-7. [Content Brief] [3]. Uehata M, et al. Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension. Nature. 1997 Oct 30;389(6654):990-4. [Content Brief] [4]. Fukushima M, et al. 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. [Content Brief] [5]. Zhang J, et al. 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. [Content Brief] [6]. Sun X, et al. The selective Rho-kinase inhibitor Fasudil is protective and therapeutic in experimental autoimmune encephalomyelitis. J Neuroimmunol. 2006 Nov;180(1-2):126-34. Epub 2006 Sep 22. [Content Brief]

Fasudil mesylate Related Classifications

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Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Fasudil mesylate (Synonyms: HA-1077 mesylate; AT-877 mesylate)

Other Forms of Fasudil mesylate:

Fasudil mesylate Related Antibodies

15 Publications Citing Use of MCE Fasudil mesylate

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•Related Small Molecules:

•Related Proteins:

View All ROCK Isoform Specific Products:

View All PKC Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review