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參考價:2330

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型號
HY-12646
品牌
MCE
廠商性質(zhì)
代理商
所在地
杭州市

規(guī)格

2mg 2330元 10000支可售

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CAS號	1281870-42-5	產(chǎn)地	國產(chǎn)
規(guī)格	2mg	級別	化工級
證書	ISO系列證書

CAS號

1281870-42-5

產(chǎn)地

國產(chǎn)

規(guī)格

2mg

級別

化工級

證書

ISO系列證書

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(jié)合 RhoA，抑制 RhoA-GEF 相互作用，K_d 值 ~ 0.4 uM，但不與 Cdc42 或 Rac1，GEF，LARG 相互作用。Rhosin hydrochloride 可誘導(dǎo)細(xì)胞凋亡。Rhosin hydrochloride 通過增強(qiáng) D1 中棘神經(jīng)元的可塑性和降低過度興奮性來促進(jìn)應(yīng)激恢復(fù)。

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^[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(nèi)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(yùn)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(shù)據(jù)

In Vitro:

DMSO : 50 mg/mL (126.63 mM; Need ultrasonic)

H₂O : 16.67 mg/mL (42.22 mM; Need ultrasonic)

配制儲備液

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

請根據(jù)產(chǎn)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(fù)凍融造成的產(chǎn)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?jiān)?6 個月內(nèi)使用，-20°C 儲存時，請?jiān)?1 個月內(nèi)使用。

In Vivo:

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(shí)驗(yàn)結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)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(xiàn)沉淀、析出現(xiàn)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(xiàn)

[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(chǎn)品僅用于科研