SR7826|cas:1219728-20-7|西域试剂

SR7826,98.74%

产品编号：Bellancom-19353| CAS NO：1219728-20-7| 分子式：C₂₂H₂₁N₅O₂| 分子量：387.43

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-19353	￥2000.00	杭州北京（现货）
Bellancom-19353	￥3200.00	杭州北京（现货）
Bellancom-19353	￥6500.00	杭州北京（现货）
Bellancom-19353	￥10200.00	杭州北京（现货）

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SR7826

产品介绍

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。

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.

体外研究

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).
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.

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

体内研究

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.
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 T_1/2 of 2.2h, an AUC of 8.4 μM*h and a C_max of 7.7 μM, and has 36% oral bioavailability in rats (oral administration; 2mg/kg).

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

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

体内研究

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

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (258.11 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5811 mL	12.9056 mL	25.8111 mL
5 mM	0.5162 mL	2.5811 mL	5.1622 mL
10 mM	0.2581 mL	1.2906 mL	2.5811 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。-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 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (6.45 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (6.45 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.45 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。