VU0119498

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VU0119498

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:

79183-37-2

VU0119498 是一种泛 G_qmAChR M1，M3，M5的正变构调节剂 (PAM)，EC₅₀值分别为 6.04，6.38 和 4.08 μM。VU0119498 具有抗糖尿病活性。

生物活性

VU0119498 is a pan G_qmAChRM1, M3, M5positive allosteric modulator (PAM), withEC₅₀s of 6.04, 6.38, and 4.08 μM, respectively. VU0119498 has antidiabetic activity^[1]^[2]^[3].

体外研究
(In Vitro)

VU0119498 (0.01-30 μM; 150 s) potentiates Ach responses in M1, M3, and M5-expressing CHO cells, with EC₅₀s of 6.04, 6.38, and 4.08 μM, respectively^[1].
VU0119498 (3-20 μM) augments ACh-mediated increasing in insulin secretion and intracellular calcium levels in MIN6-K8 cells^[3].
VU0119498 (20 μM; 90 min) enhances ACh-induced insulin release in mouse and human pancreatic islets^[3].

体内研究
(In Vivo)

VU0119498 (0.1-2 mg/kg; a single i.p.) improves glucose tolerance and insulin secretion in mice in a β-cell M3R-dependent fashion^[3].
VU0119498 (0.5 mg/kg; a single i.p.) improves glucose tolerance and insulin secretion in obese, glucose-intolerant mice^[3].

Animal Model:	Male WT mice (12 weeks)^[3]
Dosage:	0.1, 0.5, 2 mg/kg
Administration:	A single i.p.
Result:	Caused a significant improvement in glucose tolerance at the dose of 0.5 mg/kg. Significantly augmented GSIS at the dose of 0.5 mg/kg.

分子量

316.15

性状

Solid

Formula

C₁₅H₁₀BrNO₂

CAS 号

79183-37-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 50 mg/mL(158.15 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.1631 mL	15.8153 mL	31.6306 mL
5 mM	0.6326 mL	3.1631 mL	6.3261 mL
10 mM	0.3163 mL	1.5815 mL	3.1631 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。