GPR81 agonist 1|cas:1620992-67-7|西域试剂

GPR81 agonist 1,99.78%

产品编号：Bellancom-135982| CAS NO：1620992-67-7| 分子式：C₂₂H₃₀N₄O₂S₂| 分子量：446.63

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货号	价格	库存与货期
Bellancom-135982	￥4000.00	杭州北京（现货）
Bellancom-135982	￥6800.00	杭州北京（现货）
Bellancom-135982	￥19500.00	杭州北京（现货）
Bellancom-135982	￥29000.00	杭州北京（现货）

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GPR81 agonist 1

产品介绍

GPR81 agonist 1 是一种高效、高选择性的 GPR81 激动剂，对人和小鼠 GPR81 的EC₅₀ 分别为 58 nM 和 50 nM。GPR81 agonist 1 抑制分化的 3T3-L1 脂肪细胞的脂解。GPR81 agonist 1 抑制小鼠的脂解并不会造成皮肤潮红。GPR81 agonist 1 对 GPR81 的选择性高于 GPR109a。

生物活性

GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC₅₀s of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a.

体外研究

GPR81 agonist 1 (compound 2) (1-1000 nM) inhibits lipolysis in differentiated 3T3-L1 adipocytes.

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

体内研究

GPR81 agonist 1 (100 mg/kg; i.p.) suppresses lipolysis in mice without cutaneous flushing.
GPR81 agonist 1 (10 mg/kg; i.p.) shows good bioavailability (71%) and C_max (6.3 μM).

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

Animal Model:	Nine-week-old male C57/Bl6 mice (fed and fasted mice)
Dosage:	100 mg/kg
Administration:	I.p.
Result:	Reduced plasma FFA content of fed and fasted mice by approximately 50% and 35%, respectively, at 15 min postdose when intraperitoneally administered at a dose of 100 mg/kg.

Animal Model:	Male C57/Bl6 mice
Dosage:	10 mg/kg (Pharmacokinetic Analysis)
Administration:	I.p.(Pharmacokinetic Analysis)
Result:	Showed good bioavailability (71%) and C_max (6.3 μM).

体内研究

GPR81 agonist 1 (100 mg/kg; i.p.) suppresses lipolysis in mice without cutaneous flushing.
GPR81 agonist 1 (10 mg/kg; i.p.) shows good bioavailability (71%) and C_max (6.3 μM).

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

Animal Model:	Nine-week-old male C57/Bl6 mice (fed and fasted mice)
Dosage:	100 mg/kg
Administration:	I.p.
Result:	Reduced plasma FFA content of fed and fasted mice by approximately 50% and 35%, respectively, at 15 min postdose when intraperitoneally administered at a dose of 100 mg/kg.

Animal Model:	Male C57/Bl6 mice
Dosage:	10 mg/kg (Pharmacokinetic Analysis)
Administration:	I.p.(Pharmacokinetic Analysis)
Result:	Showed good bioavailability (71%) and C_max (6.3 μM).

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (111.95 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2390 mL	11.1949 mL	22.3899 mL
5 mM	0.4478 mL	2.2390 mL	4.4780 mL
10 mM	0.2239 mL	1.1195 mL	2.2390 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.60 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.60 mM，饱和度未知) 的澄清溶液。
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