Bropirimine is a synthetic agonist of Toll-like receptor 7 (TLR7). Bropirimine inhibits osteoclast differentiation from osteoclast precursor cells through TLR7-mediated IFN-β production. Bropirimine is an oral active immunomodulator with anticancer activity in transitional cell carcinoma in situ (CIS) of the bladder and upper urinary tract.
| Molecular Weight | 266.09 |
| Formula | C10H8BrN3O |
| CAS Number | 56741-95-8 |
| Solubility (25°C) | DMSO: ≥5 mg/mL (warm DMSO) |
| 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.
[2] M A Wynalda, et al. Characterization of bropirimine O-glucuronidation in human liver microsomes
[4] J A Witjes. Treatment of carcinoma in situ of the urinary bladder with bropirimine
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