D77 is anti-HIV-1 inhibitor targeting the interaction between integrase and cellular LEDGF/p75. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells). IC50 value: 23.8 μg/ml (EC50, in MT-4 cell ), 5.03 μg/ml (EC50, in C8166 cell) Target: HIV-1 in vitro: D77 exhibits a highly specific binding affinity to HIV-1 integrase catalytic core domain.D77 induces a dramatic concentration-dependent decrease of α-galactosidase activity compared to the D77-untreated cells. D77 reveals a significant inhibition activity against the interaction of IN with IBD.
Molecular Weight | 596.45 |
Formula | C28H22BrNO7S |
CAS Number | 497836-10-9 |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
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.
[1] Tobias Madl. Acta Crystallogr D Struct Biol. Intracellular drug binding affinities by NMR
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