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，Kd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 subfamilyRho GTPasesinhibitor. Rhosin hydrochloride specifically binds to RhoA to inhibit RhoA-GEF interaction with aKdof ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cellapoptosis[1][2]. Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability[3]. |
| IC50& Target | |
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[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[3].
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[3].
| 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 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | 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 | 1 mM | 2.5325 mL | 12.6627 mL | 25.3254 mL | | 5 mM | 0.5065 mL | 2.5325 mL | 5.0651 mL | | 10 mM | 0.2533 mL | 1.2663 mL | 2.5325 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.33 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.33 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.33 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
|
m.cnreagent.com