Art. -Nr.: HY-114933

VU0119498

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

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Reinheit: 98.76%
CAS. Nr.: 79183-37-2
Formel: C₁₅H₁₀BrNO₂
Molecular Weight:316.15

Speicherung:

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

VU0119498 Chemical Structure

CAS. Nr.: 79183-37-2

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

VU0119498 is a pan G_q 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].

IC₅₀ & Target

mAChR1

mAChR3

mAChR5

Alle mAChR Isoform-spezifische Produkte anzeigen :

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	>30 μM Compound: 1	Agonist activity at rat muscarinic M2 expressed in CHO cells assessed as stimulation of calcium mobilization Agonist activity at rat muscarinic M2 expressed in CHO cells assessed as stimulation of calcium mobilization	[PMID: 20004578]
CHO	EC₅₀	>30 μM Compound: 1	Agonist activity at rat muscarinic M4 expressed in CHO cells assessed as stimulation of calcium mobilization Agonist activity at rat muscarinic M4 expressed in CHO cells assessed as stimulation of calcium mobilization	[PMID: 20004578]
CHO	EC₅₀	4.08 μM Compound: 113, (VU0119498)	Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization	[PMID: 19438238]
CHO	EC₅₀	4.1 μM Compound: 1	Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization Agonist activity at human muscarinic M5 expressed in CHO cells assessed as stimulation of calcium mobilization	[PMID: 20004578]
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	6.04 μM Compound: 113, (VU0119498)	Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization Activation of rat muscarinic M1 receptor expressed in CHO cells co-expressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization	[PMID: 19438238]
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	6.1 μM Compound: 1	Agonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilization Agonist activity at rat muscarinic M1 expressed in CHO cells assessed as stimulation of calcium mobilization	[PMID: 20004578]
CHO	EC₅₀	6.38 μM Compound: 113, (VU0119498)	Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization Activation of human muscarinic M3 receptor expressed in CHO cells coexpressing Gq protein assessed as potentiation of acetylcholine-induced intracellular Ca2+ mobilization	[PMID: 19438238]
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]
CHO	EC₅₀	6.4 μM Compound: 1	Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization Agonist activity at human muscarinic M3 expressed in CHO cells assessed as stimulation of calcium mobilization	[PMID: 20004578]

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].

MedChemExpress (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].

MedChemExpress (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.

Chemical Information

CAS. Nr. 79183-37-2
Appearance Solid
Molecular Weight 316.15
Formel C₁₅H₁₀BrNO₂
Color Orange to red
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (1)

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Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (158.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Bridges TM, et, al. Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins. J Med Chem. 2009 Jun 11;52(11):3445-8. [Content Brief]

[2]. Bridges TM, et, al. Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM. Bioorg Med Chem Lett. 2010 Mar 15;20(6):1972-5. [Content Brief]

[3]. Zhu L, et, al. Allosteric modulation of β-cell M 3 muscarinic acetylcholine receptors greatly improves glucose homeostasis in lean and obese mice. Proc Natl Acad Sci U S A. 2019 Sep 10;116(37):18684-18690. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	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

Keywords

VU0119498

1 Cited Publications

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VU0119498

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Covalent Screening Library

Anti-diabetic Compound Library

Neurotransmitter Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Allosteric Modulators (AMs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) VU0119498

Alle mAChR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

VU0119498

GPCR/G Protein Compound Library

Neuronal Signaling Compound Library

Covalent Screening Library

Anti-diabetic Compound Library

Neurotransmitter Receptor Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Allosteric Modulators (AMs) Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) VU0119498

Alle mAChR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

VU0119498 Related Classifications

HY-114933 Related Classifications