TUG-770 - CAS:1402601-82-4

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TUG-770

目录号 : KM9254 CAS No. : 1402601-82-4 纯度 : 98%

Data Sheet 产品使用指南

TUG-770 是一种有效的，选择性的，具有口服活性的 GPR40/FFA1 激动剂，对人 FFA1 的 EC₅₀ 为 6 nM。TUG-770 对 FFA1 的选择性高于 FFA2，FFA3，FFA4，PPARγ，其他受体，转运蛋白和酶。TUG-770 可用于 2 型糖尿病研究。

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5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

TUG-770 is a potent, selective and orally active GPR40/FFA1 agonist with an EC₅₀ of 6 nM for human FFA1. TUG-770 shows a high selectivity for FFA1 over FFA2, FFA3, FFA4, PPARγ, other receptors, transporters, and enzymes. TUG-770 can be uesd for type 2 diabetes research.

体外研究

TUG-770 (Compound 22) displays excellent physicochemical and in vitro ADME properties, with good aqueous solubility, good chemical stability, low lipophilicity, and decreased plasma protein binding (PPB). TUG-770 shows excellent stability toward human liver microsomes (HLM), and good permeability in the Caco-2 cell assay.
TUG-770 exhibits lower potency on the rodent orthologs (mFFA1, pEC₅₀ = 6.83; rFFA1, pEC₅₀ = 6.49).
In the rat INS-1E cell line, TUG-770 significantly increases insulin secretion (10.75% of total content with 10 μM 22 vs 8.74 with vehicle) at high glucose concentration (12.4 mM) and, no effect (4.14% of total content with 10 μM 22 vs 4.02 with vehicle) at low glucose concentration (2.8 mM).

体内研究

TUG-770 (Compound 22; 20 mg/kg; oral administration; daily; for 28 days) treatment significantly improves glucose tolerance, and has no effect on food intake, body weight, body composition or plasma leptin concentration. TUG-770 also significantly improves the insulin sensitivity index (plasma glucose x plasma insulin) .

Animal Model:	C56B1/6 male mice (5-6 weeks of age) fed on the 60% fat diet D12492
Dosage:	20 mg/kg
Administration:	Oral administration; daily; for 28 days
Result:	Significantly improved glucose tolerance.

分子式

C₁₉H₁₄NO₂F

分子量

307.32

CAS号

1402601-82-4

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 : ≥ 100 mg/mL (325.39 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2539 mL	16.2697 mL	32.5394 mL
5 mM	0.6508 mL	3.2539 mL	6.5079 mL
10 mM	0.3254 mL	1.6270 mL	3.2539 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 (8.13 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.13 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。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.13 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.13 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。