Rhosin hydrochloride|1281870-42-5|-陌孚医药/Medlife

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Rhosin hydrochloride

目录号: PL10875 纯度: ≥99%

CAS No. :1281870-42-5

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中文名称	Rhosin hydrochloride
中文别名	Rhosin hydrochloride;(R,E)-2-氨基-3-(1H-吲哚-3-基)-N'-(喹喔啉-6-基亚甲基)丙酰肼盐酸盐
英文名称	Rhosin hydrochloride
英文别名	Rhosin hydrochloride;Rhosin (hydrochloride);D-Tryptophan (2E)-2-(6-quinoxalinylmethylene)hydrazide hydrochloride;(R,E)-2-amino-3-(1H-indol-3-yl)-N'-(quinoxalin-6-ylmethylene)propanehydrazide hydrochloride
Cas No.	1281870-42-5
分子式	C₂₀H₁₉ClN₆O
分子量	394.86
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情	Rhosin hydrochloride 是一种有效的，特异性的 RhoA 亚家族 Rho GTPases 抑制剂，能特异性的结合 RhoA，抑制 RhoA-GEF 相互作用，K_d 值 ~ 0.4 uM，但不与 Cdc42 或 Rac1，GEF，LARG 相互作用。Rhosin hydrochloride 可诱导细胞凋亡。Rhosin hydrochloride 通过增强 D1 中棘神经元的可塑性和降低过度兴奋性来促进应激恢复。
生物活性	Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with a K d of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis. Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability.
性状	Solid
IC50 & Target[1][2]	Kd: 0.4 uM (RhoA)
体外研究(In Vitro)	Rhosin hydrochloride dose-dependently reduces RhoA and p-MLC1 activities of MCF7 cell-derived mammospheres with an EC50 ~30-50 μM, and causes decreased size and reduced number of mammospheres in MCF7 cells. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Rhosin (40 mg/kg; i.p.) treatment prevents social avoidance caused by social defeat stress. Rhosin also blocks sucrose preference deficits induced by defeat in C57Bl6/J (Jackson) mice. Rhosin (30 μM; bilateral, intra- Nucleus Accumbens (NAc) infusions) attenuates stress-induced social avoidance. Rhosin blocks stress-induced hyperexcitability in NAc dopamine 1 receptor medium spiny neurons (D1-MSNs). Rhosin prevents decreased excitatory transmission on NAc D1-MSNs. Rhosin enhances spine density in defeat mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献	[1]. Shang X, et al. Rational design of small molecule inhibitors targeting RhoA subfamily Rho GTPases. Chem Biol. 2012 Jun 22;19(6):699-710. [2]. Shang X, et al. Small-molecule inhibitors targeting G-protein-coupled Rho guanine nucleotide exchange factors. Proc Natl Acad Sci U S A. 2013 Feb 19;110(8):3155-60.

溶解度数据	In Vitro: DMSO : 50 mg/mL (126.63 mM; Need ultrasonic)H₂O : 16.67 mg/mL (42.22 mM; Need ultrasonic)配制储备液

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