VU0119498
VU0119498
CAS: 79183-37-2
Molecular Formula: C15H10BrNO2
VU0119498 - Names and Identifiers
| Name | VU0119498 |
| Synonyms | VU0119498 1-(4-BROMOBENZYL)INDOLE-2,3-DIONE 1-(4-bromobenzyl)-1H-indole-2,3-dione 1H-Indole-2,3-dione, 1-[(4-bromophenyl)methyl]- |
| CAS | 79183-37-2 |
VU0119498 - Physico-chemical Properties
| Molecular Formula | C15H10BrNO2 |
| Molar Mass | 316.15 |
| Density | 1.604±0.06 g/cm3(Predicted) |
| Melting Point | 178-180 °C |
| Boling Point | 469.2±47.0 °C(Predicted) |
| Solubility | Soluble in DMSO |
| pKa | -2.61±0.20(Predicted) |
| Storage Condition | Sealed in dry,Room Temperature |
| Use | VU0119498 is a M1 muscarinic receptor agonist (EC50 = 3.1 μM) and pan mAChR M3, M5 positive allosteric modulator (PAM). VU0119498 is a neuroprotective agent. |
| Target | M1 muscarinic receptor : 3.1 μM(EC50), muscarinic receptor, M1 : 3.1 μM(EC50), |
| In vitro study | VU0119498 (0.01-30 μM; 150 s) potentiates Ach responses in M1, M3, and M5-expressing CHO cells, with EC 50 s of 6.04, 6.38, and 4.08 µM, respectively. VU0119498 (3-20 μM) augments ACh-mediated increasing in insulin secretion and intracellular calcium levels in MIN6-K8 cells. VU0119498 (20 μM; 90 min) enhances ACh-induced insulin release in mouse and human pancreatic islets. |
VU0119498 - Reference
| Reference Show more | 1: Bridges TM, Kennedy JP, Hopkins CR, Conn PJ, Lindsley CW. Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5617-22. doi: 10.1016/j.bmcl.2010.08.042. Epub 2010 Aug 12. PubMed PMID: 20801651; PubMed Central PMCID: PMC3179183. 2: Bridges TM, Phillip Kennedy J, Noetzel MJ, Breininger ML, Gentry PR, Conn PJ, Lindsley CW. 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. doi: 10.1016/j.bmcl.2010.01.109. Epub 2010 Feb 1. PubMed PMID: 20156687; PubMed Central PMCID: PMC2834874. 3: Bridges TM, Kennedy JP, Cho HP, Breininger ML, Gentry PR, Hopkins CR, Conn PJ, Lindsley CW. Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. Bioorg Med Chem Lett. 2010 Jan 15;20(2):558-62. doi: 10.1016/j.bmcl.2009.11.089. Epub 2009 Nov 22. PubMed PMID: 20004578; PubMed Central PMCID: PMC3177601. 4: Bridges TM, Marlo JE, Niswender CM, Jones CK, Jadhav SB, Gentry PR, Plumley HC, Weaver CD, Conn PJ, Lindsley CW. 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. doi: 10.1021/jm900286j. PubMed PMID: 1943 |
VU0119498 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.163 ml | 15.815 ml | 31.63 ml |
| 5 mM | 0.633 ml | 3.163 ml | 6.326 ml |
| 10 mM | 0.316 ml | 1.582 ml | 3.163 ml |
| 5 mM | 0.063 ml | 0.316 ml | 0.633 ml |
Last Update：2024-01-02 23:10:35
VU0119498 - Reference Information
| biological activity | VU0119498 is a kind of pan-Gq musamino acroline receptor (mAChR) M1,M3, the EC50 values of the positive allosteric modulator (PAM) of M5 were 6.1 μm, 6.4 μm and 4.1 μm, respectively. |
| Target | Value |
| mAChR M5 (Cell-free assay) | 4.1 μM |
| mAChR M1 (Cell-free assay) | 6.1 μM |
| mAChR M3 (Cell-free assay) | 6.4 μM |
| Animal Model: | Male WT mice (12 weeks) |
| 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. |
Last Update：2024-04-09 02:00:14
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