2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. VU0119498

VU0119498 是一种泛 Gq mAChR 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。

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VU0119498 Chemical Structure

VU0119498 Chemical Structure

CAS No. : 79183-37-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660
In-stock
5 mg ￥375
In-stock
10 mg ￥600
In-stock
25 mg ￥1100
In-stock
50 mg ￥1600
In-stock
100 mg ￥2400
In-stock
200 mg   询价  
500 mg   询价  

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Customer Review

VU0119498 相关抗体

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查看 mAChR 亚型特异性产品:

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VU0119498 is a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM), with EC50s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 has antidiabetic activity[1][2][3].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
> 30 μM
Compound: 1, VU0119498
Positive allosteric modulation of muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
Positive allosteric modulation of muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
[PMID: 20801651]
CHO EC50
> 30 μM
Compound: 1, VU0119498
Positive allosteric modulation of muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
Positive allosteric modulation of muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
[PMID: 20801651]
CHO EC50
4.6 μM
Compound: 1, VU0119498
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
Positive allosteric modulation of muscarinic M5 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
[PMID: 20801651]
CHO EC50
6.1 μM
Compound: 1, VU0119498
Positive allosteric modulation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
Positive allosteric modulation of muscarinic M1 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
[PMID: 20801651]
CHO EC50
6.4 μM
Compound: 1, VU0119498
Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
Positive allosteric modulation of muscarinic M3 receptor expressed in CHO cells assessed as effect on acetylcholine-induced intracellular calcium mobilization after 1 hr by FLIPR assay
[PMID: 20801651]
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].

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

VU0119498 相关抗体:
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].

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

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

Formula

C15H10BrNO2
CAS 号
性状

固体

颜色

Orange to red

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
细胞实验： 

DMSO 中的溶解度 : 50 mg/mL (158.15 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

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
查看完整储备液配制表

* 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。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.52%

COA (268 KB) HNMR (210 KB) LCMS (96 KB)

产品使用指南 (1538 KB)
参考文献

VU0119498 相关分类

完整储备液配制表

* 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.1631 mL 15.8153 mL 31.6306 mL 79.0764 mL
5 mM 0.6326 mL 3.1631 mL 6.3261 mL 15.8153 mL
10 mM 0.3163 mL 1.5815 mL 3.1631 mL 7.9076 mL
15 mM 0.2109 mL 1.0544 mL 2.1087 mL 5.2718 mL
20 mM 0.1582 mL 0.7908 mL 1.5815 mL 3.9538 mL
25 mM 0.1265 mL 0.6326 mL 1.2652 mL 3.1631 mL
30 mM 0.1054 mL 0.5272 mL 1.0544 mL 2.6359 mL
40 mM 0.0791 mL 0.3954 mL 0.7908 mL 1.9769 mL
50 mM 0.0633 mL 0.3163 mL 0.6326 mL 1.5815 mL
60 mM 0.0527 mL 0.2636 mL 0.5272 mL 1.3179 mL
80 mM 0.0395 mL 0.1977 mL 0.3954 mL 0.9885 mL
100 mM 0.0316 mL 0.1582 mL 0.3163 mL 0.7908 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VU011949879183-37-2VU 0119498VU-0119498mAChRMuscarinic acetylcholine receptorpanGqM1M3M5antidiabeticInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-114933
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