GSK726701A|cas:945721-87-9|西域试剂

GSK726701A,98.72%

产品编号：Bellancom-112152| CAS NO：945721-87-9| 分子式：C₂₄H₂₂FNO₅| 分子量：423.43

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-112152		￥5000.00	杭州北京（现货）
Bellancom-112152		￥8500.00	杭州北京（现货）

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GSK726701A

产品介绍

GSK726701A是前列腺素E2受体4 (EP4)的部分激动剂，pEC₅₀为7.4。

生物活性

GSK726701A is a novel prostaglandin E2 receptor 4 (EP4) partial agonist with a pEC₅₀ of 7.4.

体外研究

GSK726701A has high selectivity (>100-fold) against a set of other prostaglandin receptors (EP1-3 , DP1 , FP, IP, TP) and no significant activity against a wider panel of targets. It demonstrates EP4 agonist activity with similar potency and intrinsic activity (pEC₅₀=8.2) in a human whole blood (HWB) assay on the inhibition of LPS-mediated TNFα induction.

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

体内研究

GSK726701A has good pharmacokinetic file in rat, dog and monkey. GSK726701A has robust activity in a range of animal models of inflammatory and neuropathic pain GSK726701A demonstrates a time-dependant, full reversal of CCI-induced mechanical allodynia at 3mg/kg, equivalent to the clinical gold standard gabapentin (30mg/kg). GSK726701A has an ED₅₀ of 0.2mg/kg in the FCA acute rat model of inflammatory pain.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (59.04 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3617 mL	11.8083 mL	23.6167 mL
5 mM	0.4723 mL	2.3617 mL	4.7233 mL
10 mM	0.2362 mL	1.1808 mL	2.3617 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% corn oil
Solubility: ≥ 2.5 mg/mL (5.90 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.90 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。