Rhosin hydrochloride|cas:1281870-42-5|西域试剂

Rhosin hydrochloride,99.93%

产品编号：Bellancom-12646| CAS NO：1281870-42-5| 分子式：C₂₀H₁₉ClN₆O| 分子量：394.86

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货号	价格	库存与货期
Bellancom-12646	￥2330.00	杭州北京（现货）
Bellancom-12646	￥2900.00	杭州北京（现货）
Bellancom-12646	￥4450.00	杭州北京（现货）

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Rhosin hydrochloride

产品介绍

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.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	D1-GFP or D2-GFP hemizygote mice on a C57BL/6J background
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	D1-GFP or D2-GFP hemizygote mice on a C57BL/6J background
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.

性状

Solid

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

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
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。