NLRP3/AIM2-IN-3 is a potent inhibitor that interferes with the interaction of NLRP3 or AIM2 with the bridging protein ASC and inhibits ASC oligomerization, and has different species-specific effects on NLRP3 and AIM2 inflammasome-dependent pyroptosis. In addition, NLRP3/AIM2-IN-3 inhibited LPS/nigericin-stimulated cell pyroptosis in THP-1 macrophages with an IC50 of 0.077 ± 0.008 μM.
| Molecular Weight | 266.29 |
| Formula | C16H14N2O2 |
| CAS Number | 1787787-60-3 |
| Form | Solid |
| Solubility (25°C) | DMSO >100 mg/mL Methanol 50 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
Antcin A is an NLRP3 inhibitor that inhibits the assembly and activation of NLRP3 inflammatory vesicles. In addition, Antcin A inhibits pyroptosis of Kupffer cells and has hepatoprotective activity.Antcin A can be used in inflammation-related studies. |
| 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. |
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