BMS-986163 a Negative Allosteric Modulator of GluN2B with Potential Utility in Major Depressive Disorder. BMS-986163 is a water-soluble intravenous prodrug BMS-986163 and its active parent molecule BMS-986169, which demonstrated high binding affinity for the GluN2B allosteric site (Ki = 4.0 nM) and selective inhibition of GluN2B receptor function (IC50 = 24 nM) in cells. The conversion of prodrug BMS-986163 to parent BMS-986169 was rapid in vitro and in vivo across preclinical species. The prodrug BMS-986163 has demonstrated an acceptable safety and toxicology profile and was selected as a preclinical candidate for further evaluation in major depressive disorder.
MedKoo Cat#: 555230
Name: BMS-986163
CAS#: 1801151-09-6
Chemical Formula: C23H28FN2O5P
Exact Mass: 462.1720
Molecular Weight: 462.46
Elemental Analysis: C, 59.74; H, 6.10; F, 4.11; N, 6.06; O, 17.30; P, 6.70
The following data is based on the product molecular weight 462.46 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
