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

VU0119498 

Cat. No.: HY-114933
Handling Instructions

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.

For research use only. We do not sell to patients.

VU0119498 Chemical Structure

VU0119498 Chemical Structure

CAS No. : 79183-37-2

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10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
25 mg USD 110 In-stock
Estimated Time of Arrival: December 31
50 mg USD 160 In-stock
Estimated Time of Arrival: December 31
100 mg USD 240 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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].

In Vitro

VU0119498 (0.01-30 μM; 150s) 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 increases 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.

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.
Molecular Weight

316.15

Formula

C₁₅H₁₀BrNO₂

CAS No.

79183-37-2

SMILES

O=C1N(C2=C(C1=O)C=CC=C2)CC3=CC=C(C=C3)Br

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

VU0119498VU 0119498VU-0119498mAChRMuscarinic acetylcholine receptorpanGqM1M3M5antidiabeticInhibitorinhibitorinhibit

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VU0119498
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