GSK205

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GSK205

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1263068-83-2

GSK205 是一种高效的，选择性的TRPV4拮抗剂，IC₅₀值为 4.19 μM，可抑制TRPV4介导的 Ca²⁺内流。

生物活性

GSK205 is a potent, selectiveTRPV4antagonist with anIC₅₀of 4.19 μM for inhibitingTRPV4-mediated Ca²⁺influx^[1]^[2].

IC₅₀& Target

IC50: 4.19 μM (TRPV4)^[2]

体外研究
(In Vitro)

GSK205 (100 μM) potently antagonizes TRPV4 in 3T3-F442A adipocytes, as it effectively blocks the calcium influx caused by TRPV4 agonist^[1].
GSK205 (5 μM; 4 days; T3-F442A adipocytes) treatment results in increases expression of thermogenic genes (Mcp1, Mip1α, Mcp3, Rantes and Vcam, et al.) and is also accompanied by a decrease in the proinflammatory gene program. This shift resembles the gene expression changes seen in TRPV4-deficient adipocytes^[1].

RT-PCR^[1]

Cell Line:	T3-F442A adipocytes
Concentration:	5 μM
Incubation Time:	4 days
Result:	Resulted in increased expression of thermogenic genes and is also accompanied by a decrease in the proinflammatory gene program.

体内研究
(In Vivo)

GSK205 (10 mg/kg; intraperitoneal injection; twice daily; for 7 days; for 4 weeks; male C57BL/6J mice) treatment shows significantly increases expression of thermogenic genes such as Ucp1, Pgc1a, Cidea and Cox8b. GSK205 treatment causes a reduced expression of the proinflammatory chemokines, macrophage marker and Tnfa in the EPI fat. GSK205 treatment significantly improves glucose tolerance in diet-induced obese (DIO) mice. There are no apparent sign of sickness or weight loss^[1].
GSK205 has a relatively short half-life of 2 hours in the plasma and adipose tissues^[1].

Animal Model:	Male C57BL/6J mice with high-fat diet^[1]
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; twice daily; for 7 days
Result:	Caused a reduced expression of the proinflammatory chemokines, macrophage marker and Tnfa in the EPI fat. Significantly improved glucose tolerance in diet-induced obese (DIO) mice.

分子量

481.45

性状

Solid

Formula

C₂₄H₂₅BrN₄S

CAS 号

1263068-83-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 250 mg/mL(519.26 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.0771 mL	10.3853 mL	20.7706 mL
5 mM	0.4154 mL	2.0771 mL	4.1541 mL
10 mM	0.2077 mL	1.0385 mL	2.0771 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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 40%PEG300 5%Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.32 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
2.
请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline)
Solubility: ≥ 2.08 mg/mL (4.32 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (4.32 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 900 μL20% 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

*以上所有助溶剂都可在本网站选购。