GSK2193874|cas:1336960-13-4|西域试剂

GSK2193874,99.74%

产品编号：Bellancom-100720| CAS NO：1336960-13-4| 分子式：C₃₇H₃₈BrF₃N₄O| 分子量：691.62

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-100720	￥550.00	杭州北京（现货）
Bellancom-100720	￥770.00	杭州北京（现货）
Bellancom-100720	￥1350.00	杭州北京（现货）
Bellancom-100720	￥2450.00	杭州北京（现货）
Bellancom-100720	￥4650.00	杭州北京（现货）

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GSK2193874

产品介绍

GSK2193874 是具有口服活性的有效的选择性 TRPV4 拮抗剂，作用于 rTRPV4 和 hTRPV4，IC₅₀ 分别为 2 nM 和 40 nM。

生物活性

GSK2193874 is an orally active, potent, and selective TRPV4 antagonist with IC₅₀s of 2 nM and 40 nM for rTRPV4 and hTRPV4.

体外研究

GSK2193874 is profiled against TRP channels and is selective against TRPV1, TRPA1, TRPC3, TRPC6, and TRPM8 (IC₅₀>25 μM). GSK2193874 is a selective, orally active TRPV4 blocker that inhibits Ca²⁺ influx through recombinant TRPV4 channels and native endothelial TRPV4 currents. In whole-cell patch-clamp studies, GSK2193874 inhibits activation of recombinant TRPV4 currents when applied to the extracellular solution at 3 nM and above but is ineffective at up to 10 μM when applied to the inside of the cell by inclusion in the intracellular pipette solution.

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

体内研究

The pharmacokinetic (PK) properties for GSK2193874 are evaluated in both rat and dog and found to have half-lives and oral exposure suitable for oral dosing in chronic animal models (Rat PK: iv CL=7.3 mL/min/kg, po t_1/2=10 h, %F=31. Dog PK: iv CL=6.9 mL/min/kg, po t_1/2=31 h, %F=53). In addition, GSK2193874 shows no blood pressure or heart rate effect in rats when dose up to 30 mg/kg. GSK2193874 is the first-in-class orally bioavailable TRPV4 inhibitor that demonstrated ability to improve pulmonary functions in a number of heart failure models. GSK2193874 shows low clearance (7.3 mL/min/kg) and good rat oral bioavailability (31%).

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 : 100 mg/mL (144.59 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4459 mL	7.2294 mL	14.4588 mL
5 mM	0.2892 mL	1.4459 mL	2.8918 mL
10 mM	0.1446 mL	0.7229 mL	1.4459 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： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (3.61 mM); Suspended solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.01 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.01 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.01 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.01 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。