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Y-27632 dihydrochloride Y-27632双盐酸盐 CAS:129830-38-2


CAS:129830-38-2

C14357

Y-27632双盐酸盐

Product Name:Y-27632 dihydrochloride 

Synonyms:Y-27632 2HCl

Chemical Name:trans-4-[(1R)-1-Aminoethyl]-N-4-pyridinylcyclohexanecarboxamide dihydrochloride

Molecular Formula:C14H21N3O.2HCl

Formula Weight:320.26

Purity:>99% 

Appearance:White to pale yellow solid

Short Term Storage:+4°C

Long Term Storage:-20°C

Solubility: Soluble to 100 mM in water

Use/Stability:Stable for at least 2 years after receipt when stored at -20°C. Stock solutions are stable for at least 3 months when stored at -20°C

Biological Activity:
Selective p160ROCK inhibitor (Ki values are 0.14, 26, 25 and > 250 μM for p160ROCK, PKC, PKA and MLCK respectively). Also inhibits PRK2 (IC50 = 600 nM). Smooth muscle relaxant and orally active in vivo. Increases survival rate of human embryonic stem (hES) cells undergoing cryopreservation. Also optimizes naïve human pluripotent stem cell growth and viability following naïve cell derivation from primed ESCs and iPSCs using naïve human stem cell medium (NHSM).

References:
1.Calcium sensitization of smooth muscle mediated by a Rho-associated protein kinase in hypertension: M. Uehata, et al.; Nature 389, 990 (1997)
2.An essential part for Rho-associated kinase in the transcellular invasion of tumor cells: K. Itoh, et al.; Nat. Med. 5, 221 (1999)
3.Use and properties of ROCK-specific inhibitor Y-27632: S. Narumiya, et al.; Meth. Enzymol. 325, 273 (2000)
4.Specificity and mechanism of action of some commonly used protein kinase inhibitors: S.P. Davies, et al.; Biochem. J. 351, 95 (2000)
5.Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases: T. Ishizaki, et al.; Mol. Pharmacol. 57, 976 (2000)
6.Y-27632 potentiates relaxant effects of beta 2-adrenoceptor agonists in bovine tracheal smooth muscle: T. Nakahara, et al.; Eur. J. Pharmacol. 389, 103 (2000)
7.A p160ROCK-specific inhibitor, Y-27632, attenuates rat hepatic stellate cell growth: H. Iwamoto, et al.; J. Hepatol. 32, 762 (2000)
8.Inhibition of intrahepatic metastasis of human hepatocellular carcinoma by Rho-associated protein kinase inhibitor Y-27632: M. Takamura, et al.; Hepatology 33, 577 (2001)
9.Rho-kinase inhibitor, Y-27632, has an antinociceptive effect in mice: K. Buyukafsar, et al.; Eur. J. Pharmacol. 541, 49 (2006)
10.Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities: C. Doe, et al.; JPET 320, 89 (2007)
11.A ROCK inhibitor permits survival of dissociated human embryonic stem cells: K. Watanabe, et al.; Nat. Biotechnol. 25, 681 (2007)
12.The ROCK inhibitor Y-27632 enhances the survival rate of human embryonic stem cells following cryopreservation: X. Li, et al.; Stem Cells Dev. 17, 1079 (2008)
13.Effect of Rho-associated kinase (ROCK) inhibitor Y-27632 on the post-thaw viability of cryopreserved human bone marrow-derived mesenchymal stem cells: B.C. Heng; Tissue Cell 41, 376 (2009)
14.Effect of ROCK inhibitor Y-27632 on normal and variant human embryonic stem cells (hESCs) in vitro: its benefits in hESC expansion: K. Gauthaman, et al.; Stem Cell Rev. 6, 86 (2010)
15.Pharmacological inhibition of Rho-kinase signaling with Y-27632 blocks melanoma tumor growth: A. Routhier, et al.; Oncol. Rep. 23, 861 (2010)
16.The ROCK inhibitor Y-27632 improves recovery of human embryonic stem cells after fluorescence-activated cell sorting with multiple cell surface markers: N. Emre, et al.; PLoS One 5, e12148 (2010)

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发布日期:2017/3/15 14:22:23