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Bictegravir (GS-9883) is a novel, potent inhibitor of HIV-1 integrase with an IC50 of 7.5 nM.
| Molecular Weight | 449.38 |
| Formula | C21H18F3N3O5 |
| CAS Number | 1611493-60-7 |
| Solubility (25°C) | DMSO: ≥ 60 mg/mL (Need ultrasonic and warming) |
| 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] No authors listed. Bictegravir
[3] Emma D Deeks. Bictegravir/Emtricitabine/Tenofovir Alafenamide: A Review in HIV-1 Infection
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| Bictegravir Sodium
Bictegravir (GS-9883) Sodium is a novel and potent inhibitor of HIV-1 integrase, specifically targets IN strand transfer activity with an IC50 of 7.5 nM. |
| Lavendustin B
Lavendustin B inhibits HIV-1 integrase (IN) interaction with its cognate cellular cofactor lens epithelium-derived growth factor (LEDGF/p75). Lavendustin B is an inhibitor of Tyrosine Kinase and also a competitive inhibitor of glucose transporter 1 (Glut1). |
| Dolutegravir
Dolutegravir (GSK1349572) is a two-metal-binding HIV integrase inhibitor with IC50 of 2.7 nM, modest activity against raltegravir-resistant signature mutants Y143R, Q148K, N155H, and G140S/Q148H. |
| MK-2048
MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively. |
| Raltegravir
Raltegravir (MK-0518) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively. |
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