Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMS-984923, a highly potent silent allosteric modulator (SAM) of mGluR5, demonstrates exceptional binding affinity (K i = 0.6 nM). Additionally, this compound possesses favorable oral bioavailability and blood-brain barrier (BBB) penetration. BMS-984923 effectively inhibits the interaction between PrPC and mGluR5, preventing pathological Aβo signaling, while leaving physiological glutamate signaling unaffected.
Description | BMS-984923, a highly potent silent allosteric modulator (SAM) of mGluR5, demonstrates exceptional binding affinity (K i = 0.6 nM). Additionally, this compound possesses favorable oral bioavailability and blood-brain barrier (BBB) penetration. BMS-984923 effectively inhibits the interaction between PrPC and mGluR5, preventing pathological Aβo signaling, while leaving physiological glutamate signaling unaffected. |
In vivo | BMS-984923, administered orally at dosages of 7.5 mg/kg or 15 mg/kg, demonstrates effective oral bioavailability and penetration of the blood-brain barrier (BBB) [1]. This assessment was conducted using C57Bl6J male mice [1], with the pharmacokinetic analysis revealing that plasma concentrations surpassed 2 μM at 10 hours post-administration. Notably, brain concentrations approached those of plasma levels three hours following a single 7.5 mg/kg dose, indicating significant cerebral distribution. |
Molecular Weight | 374.82 |
Formula | C22H15ClN2O2 |
CAS No. | 1375752-78-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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BMS-984923 1375752-78-5 BMS984923 BMS 984923 inhibitor inhibit