Rhosin

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Rhosin

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1173671-63-0

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

Rhosin 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 可诱导细胞凋亡 (apoptosis)。Rhosin 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 is a potent, specific RhoA subfamilyRho GTPasesinhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with aK_dof ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cellapoptosis^[1]^[2]. Rhosin promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability^[3].

IC₅₀& Target

Kd: 0.4 uM (RhoA)^[1]

体外研究
(In Vitro)

Rhosin 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^[1].

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^[1].
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^[1].

Animal Model:	D1-GFP or D2-GFP hemizygote mice on a C57BL/6J background^[3]
Dosage:	40 mg/kg
Administration:	i.p.
Result:	Rhosin was systemically administered 15 min prior to defeat to block RhoA activation. While defeat significantly reduced the time that experimental mice spent interacting with a novel mouse, Rhosin administration suppressed this effect without affecting locomotor behaviors.

分子量

358.40

Formula

C₂₀H₁₈N₆O

CAS 号

1173671-63-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.