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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。
VU0119498图片
CAS NO:79183-37-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
VU0119498 是一种泛 GqmAChR 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 GqmAChRM1, 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°C3 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM3.1631 mL15.8153 mL31.6306 mL
5 mM0.6326 mL3.1631 mL6.3261 mL
10 mM0.3163 mL1.5815 mL3.1631 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。