1-(4-BROMOBENZYL)INDOLE-2,3-DIONE
1-(4-BROMOBENZYL)INDOLE-2,3-DIONE Basic information
- Product Name:
- 1-(4-BROMOBENZYL)INDOLE-2,3-DIONE
- Synonyms:
-
- 1-(4-BROMOBENZYL)INDOLE-2,3-DIONE
- VU0119498
- 1-(4-bromobenzyl)-1H-indole-2,3-dione
- 1H-Indole-2,3-dione, 1-[(4-bromophenyl)methyl]-
- antidiabetic,VU 0119498,Inhibitor,VU0119498,inhibit,VU-0119498,mAChR,pan,Muscarinic acetylcholine receptor
- VU0119498, M1 muscarinic receptor agonist and pan mAChR M3, M5 PAM
- VU0119498, 10 mM in DMSO
- 1-[(4-Bromophenyl)methyl]indole-2,3-dione
- CAS:
- 79183-37-2
- MF:
- C15H10BrNO2
- MW:
- 316.15
- Mol File:
- 79183-37-2.mol
1-(4-BROMOBENZYL)INDOLE-2,3-DIONE Chemical Properties
- Melting point:
- 178-180 °C
- Boiling point:
- 469.2±47.0 °C(Predicted)
- Density
- 1.604±0.06 g/cm3(Predicted)
- storage temp.
- Sealed in dry,Room Temperature
- solubility
- DMSO: 50 mg/mL (158.15 mM)
- form
- A solid
- pka
- -2.61±0.20(Predicted)
- color
- Orange to red
1-(4-BROMOBENZYL)INDOLE-2,3-DIONE Usage And Synthesis
Uses
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 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. |
References
[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. DOI:10.1021/jm900286j
[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. DOI:10.1016/j.bmcl.2010.01.109
[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. DOI:10.1073/pnas.1904943116
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