1-(4-BROMOBENZYL)INDOLE-2,3-DIONE
- Product Name
- 1-(4-BROMOBENZYL)INDOLE-2,3-DIONE
- CAS No.
- 79183-37-2
- Chemical Name
- 1-(4-BROMOBENZYL)INDOLE-2,3-DIONE
- Synonyms
- VU0119498;VU0119498 ，S0783;VU0119498, 10 mM in DMSO;1-(4-BROMOBENZYL)INDOLE-2,3-DIONE;1-(4-bromobenzyl)-1H-indole-2,3-dione;1-[(4-Bromophenyl)methyl]indole-2,3-dione;1H-Indole-2,3-dione, 1-[(4-bromophenyl)methyl]-;VU0119498, M1 muscarinic receptor agonist and pan mAChR M3, M5 PAM;antidiabetic,VU 0119498,Inhibitor,VU0119498,inhibit,VU-0119498,mAChR,pan,Muscarinic acetylcholine receptor
- CBNumber
- CB82463915
- Molecular Formula
- C15H10BrNO2
- Formula Weight
- 316.15
- MOL File
- 79183-37-2.mol
1-(4-BROMOBENZYL)INDOLE-2,3-DIONE Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
- Precautionary statements
-
P264Wash hands thoroughly after handling.
P264Wash skin thouroughly after handling.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P332+P313IF SKIN irritation occurs: Get medical advice/attention.
P337+P313IF eye irritation persists: Get medical advice/attention.
P362Take off contaminated clothing and wash before reuse.
N-Bromosuccinimide Price
- Product number
- CS-0064669
- Product name
- VU0119498
- Packaging
- 10mg
- Price
- $60
- Updated
- 2021/12/16
- Product number
- CS-0064669
- Product name
- VU0119498
- Packaging
- 50mg
- Price
- $160
- Updated
- 2021/12/16
- Product number
- 5425CJ
- Product name
- 1-[(4-Bromophenyl)methyl]indole-2,3-dione
- Packaging
- 250mg
- Price
- $203
- Updated
- 2021/12/16
- Product number
- CS-0064669
- Product name
- VU0119498
- Packaging
- 25mg
- Price
- $110
- Updated
- 2021/12/16
- Product number
- CS-0064669
- Product name
- VU0119498
- Packaging
- 100mg
- Price
- $240
- Updated
- 2021/12/16
1-(4-BROMOBENZYL)INDOLE-2,3-DIONE Chemical Properties,Usage,Production
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
1-(4-BROMOBENZYL)INDOLE-2,3-DIONE Preparation Products And Raw materials
Raw materials
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