BMS-986299 is a first-in-class (first-in-class) NLRP3 inflammatory vesicle agonist that induces IL8 release to activate natural killer (NK) cells with an EC50 of 1.28 μM.
| Molecular Weight | 349.39 |
| Formula | C18H19N7O |
| CAS Number | 2242952-69-6 |
| Solubility (25°C) | DMSO 70 mg/mL Water 17 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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| Antcin A
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| ADS032
ADS032 is a dual inhibitor of NLRP1 and NLRP3 that rapidly, reversibly and stably inhibits inflammasome formation and reduces NLPR1 and NLRP3 activation of human-derived macrophages and bronchial epithelial cells to secrete and mature IL-1β and TNF-α, and reduces NLRP3-induced ASC speck formation. In addition, ADS032 protects mice from the deadly influenza A virus, reduces lung inflammation and improves survival. |
| Emlenoflast sodium
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