BMS-751324
- Catalog NO.:A902840
- CAS No. : 948842-66-8
- Molecular Formula:C32H35N6O10P
- Molecular Weight: 694.64
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Product Details
CAS Number | 948842-66-8 | Appearance | |
Catalog Number | A902840 | MDL Number | |
Molecular Formula | C32H35N6O10P | Molecular Weight | 694.64 |
Boiling Point | Melting Point | ||
Flash Point | Density | ||
Synonyms | (((4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyl)oxy)methyl 2-(4-(phosphonooxy)phenyl)acetate;(((4-((5-(cyclopropylcarbamoyl)-2-methylphenyl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazine-6-carbonyl)(propyl)carbamoyl)oxy)methyl 2-(4-(phosphonooxy)phenyl)acetate | ||
Storage Condition | Store in a tightly closed container,in a cool and dry place |
Safety
GHS Pictogram | |||
Signal Word | Warning | UN Number | |
Hazard Statements | Class | ||
Precautionary Statements | Packing Group |
Description
BMS-751324 is a clinical prodrug of p38α MAP kinase inhibitor. BMS-751324 is prodrug of BMS-582949. BMS-751324 was designed to address the issue of pH-dependent solubility and exposure associated with BMS-582949, a phase II clinical p38α MAP kinase inhibitor. BMS-751324 is featured with a carbamoylmethylene linked promoiety containing hydroxyphenyl acetic acid (HPA) derived ester and phosphate functionalities. BMS-751324 was not only stable but also water-soluble under both acidic and neutral conditions. BMS-751324 was effectively bioconverted into parent drug BMS-582949 in vivo by alkaline phosphatase and esterase in a stepwise manner, providing higher exposure of BMS-582949 compared to its direct administration, especially within higher dose ranges. In a rat LPS-induced TNFα pharmacodynamic model and a rat adjuvant arthritis model, BMS-751324 demonstrated similar efficacy to BMS-582949. Most importantly, it was shown in clinical studies that prodrug BMS-582949 was indeed effective in addressing the pH-dependent absorption issue associated with BMS-582949. |