SR7826

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

SR7826  纯度: 98.74%

SR7826 是一类由双芳基脲衍生的有效，选择性和具有口服活性的 LIM 激酶 (LIMK) 抑制剂，对于 LIMK1 的 IC50 为 43 nM。SR7826 对 LIMK1 的选择性比 ROCK 和 JNK 激酶高 100 倍以上。

SR7826

SR7826 Chemical Structure

CAS No. : 1219728-20-7

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5 mg ￥2600 In-stock
10 mg ￥3800 In-stock
25 mg ￥8000 In-stock
50 mg ￥12800 In-stock
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生物活性

SR7826 is a class of bis-aryl urea derived potent, selective and orally active LIM kinase (LIMK) inhibitor with an IC50 of 43 nM for LIMK1. SR7826 is >100-fold more selective for LIMK1 than ROCK and JNK kinases[1].

IC50 & Target

LIMK1

43 nM (IC50)

ROCKI

5536 nM (IC50)

ROCKII

6565 nM (IC50)

体外研究
(In Vitro)

In the profiling against a panel of 61 kinases, SR7826 (compound 18b) at 1 μM inhibits only Limk1 and STK16 with ≥80% inhibition. SR7826 is highly efficient in inhibiting cell-invasion/migration in PC-3 cells. SR7826 (compound 18b) inhibits cofilin phosphorylation in A7r5 (IC50 = 470 nM) and PC-3 cells (IC50 < 1 µM)[1].
SR7826 (1 μM) inhibits contractions of prostate strips, which were induced by electrical field stimulation and inhibits cofilin phosphorylation in prostate tissues and cultured stromal cells (WPMY-1). In WPMY-1 cells, SR7826 causes breakdown of actin filaments and reduced viability[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

SR7826 (10 mg/kg; oral gavage; once daily; for 11 days; hAPPJ20 mice) treatment significantly reduces the phosphorylation of cofilin at Ser3. SR7826 also increases both apical and basal thin spine density significantly in hAPPJ20 mice over mock-treated animals[2].
The plasma pharmacokinetics studies on rats are investigated. After intravenous injection, the PK properties of SR7826 (compound 18b; 1mg/kg) with a Cl of 5.2 mL/min/kg, a T1/2 of 2.2h, an AUC of 8.4 μM*h and a Cmax of 7.7 μM, and has 36% oral bioavailability in rats (oral administration; 2mg/kg)[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: hAPPJ20 mice (6-mouth-old)[2]
Dosage: 10 mg/kg
Administration: Oral gavage; once daily; for 11 days
Result: Significantly reduced the phosphorylation of cofilin at Ser3, a LIMK1 substrate.

分子量

387.43

Formula

C22H21N5O2
CAS 号

1219728-20-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Yan Yin, et al. Bis-aryl urea derivatives as potent and selective LIM kinase (Limk) inhibitors. J Med Chem. 2015 Feb 26;58(4):1846-61.

    [2]. Benjamin W Henderson, et al. Pharmacologic inhibition of LIMK1 provides dendritic spine resilience against β-amyloid. Sci Signal. 2019 Jun 25;12(587):eaaw9318.

    [3]. Qingfeng Yu, et al. Inhibition of human prostate smooth muscle contraction by the LIM kinase inhibitors, SR7826 and LIMKi3. Br J Pharmacol. 2018 Jun;175(11):2077-2096.

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