GW-1100

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GW-1100

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:

306974-70-9

包装与价格：

包装	价格(元)
10 mM * 1 mL in DMSO	电议
5mg	电议
10mg	电议
50mg	电议
100mg	电议
200mg	电议

产品介绍

GW-1100是选择性的GPR40拮抗剂，pIC₅₀为6.9。

生物活性

GW-1100 is a selectiveGPR40antagonist with apIC₅₀of 6.9.

IC₅₀& Target

pIC50: 6.9 (GPR40)^[1]

体外研究
(In Vitro)

GW-1100 (GW1100) dose dependently inhibits GPR40-mediated Ca²⁺elevations stimulated by GW9508 and linoleic acid (pIC₅₀values of 5.99±0.03 and 5.99±0.06, respectively). GW-1100 at a concentration of 1 μM produces a significant rightward shift in the concentration-response curve to GW9508 (pEC₅₀=7.17±0.08 in the absence and pEC₅₀=6.79±0.09 in the presence of 1 μM GW-1100; P<0.05; n=3). At concentrations of GW-1100 of 3 μM and higher a significant decrease in the maximal response is observed with a continuing rightward shift in the pEC₅₀response^[2]. GW-1100 (GW1100) reduces FFAR1 ligand-induced intracellular calcium in CHO-K1/bFFAR1 cells and neutrophils. CHO-K1/bFFAR1 cells are incubated for 15 min with 10 μM GW1100 or vehicle (0.1% DMSO) and then stimulated with vehicle, oleic acid, linoleic acid or GW9508. GW-1100 significantly reduces the increase in intracellular calcium induced by 300 μM oleic acid (AUC_{(60-150 s)}, p<0.05), 100 μM linoleic acid (AUC_{(60-150 s)}, p<0.05) and 10 μM GW9508 (AUC_{(60-150 s)}, p<0.05)^[3].

体内研究
(In Vivo)

The intracerebroventricular injection of DHA (50 μg) and GW9508 (1.0 μg), a GPR40-selective agonist, significantly reduces mechanical allodynia and thermal hyperalgesia at day 7, but not at day 1, after CFA injection. These effects are inhibited by intracerebroventricular pretreatment with GW-1100 (10 μg), a GPR40 antagonist^[4].

分子量

520.58

性状

Solid

Formula

C₂₇H₂₅FN₄O₄S

CAS 号

306974-70-9

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

溶解性数据

In Vitro:

DMSO : 50 mg/mL(96.05 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.9209 mL	9.6047 mL	19.2093 mL
5 mM	0.3842 mL	1.9209 mL	3.8419 mL
10 mM	0.1921 mL	0.9605 mL	1.9209 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。-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 50% PBS
Solubility: 5 mg/mL (9.60 mM); Suspended solution; Need ultrasonic
2.
请依序添加每种溶剂： 10% DMSO 90%corn oil
Solubility: ≥ 2.5 mg/mL (4.80 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.80 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。
3.
请依序添加每种溶剂： 1% DMSO 99% saline
Solubility: 0.06 mg/mL (0.12 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。