鹽酸松香(Rhosin hydrochloride)
Rhosin hydrochloride 是一種有效的，特異性的 RhoA 亞家族 Rho GTPases 抑制劑，能特異性的結合 RhoA，抑制 RhoA-GEF 相互作用，Kd 值 ~ 0.4 uM，但不與 Cdc42 或 Rac1，GEF，LARG 相互作用。Rhosin hydrochloride 可誘導細胞凋亡。Rhosin hydrochloride 通過增強 D1 中棘神經元的可塑性和降低過度興奮性來促進應激恢復。
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 Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin hydrochloride induces cell apoptosis[1][2]. Rhosin hydrochloride promotes stress resiliency through enhancing D1-MSN plasticity and reducing hyperexcitability[3].
IC50 & Target
Kd: 0.4 uM (RhoA)[1]
體外研究(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].
體內研究(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].
MCE 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[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：394.86
Formula：C20H19ClN6O
CAS 號：1281870-42-5
運輸條件：Room temperature in continental US; may vary elsewhere.
儲存方式
4°C, sealed storage, away from moisture
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性數據
DMSO : 50 mg/mL (126.63 mM; Need ultrasonic)
H2O : 16.67 mg/mL (42.22 mM; Need ultrasonic)
| 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 |
請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 儲存時，請在 6 個月內使用，-20°C 儲存時，請在 1 個月內使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議您現用現配，當天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution
- 2.
請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution
- 3.
請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution
參考文獻
[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. [Content Brief]
[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. [Content Brief]
[3]. Francis TC, et al. The Selective RhoA Inhibitor Rhosin Promotes Stress Resiliency Through Enhancing D1-Medium Spiny Neuron Plasticity and Reducing Hyperexcitability. Biol Psychiatry. 2019;85(12):1001-1010. [Content Brief]
注：產品僅用于科研
采購中心
