Bioactivity | BMS-707035 is a potent orally active HIV-1 integrase strand transfer inhibitor (INSTI). BMS-707035 has enzyme inhibitory with an IC50 value of 3 nM. BMS-707035 also has weak CYP inhibiton and antiviral activity. BMS-707035 can be used for the research of human immunodeficiency virus-1 (HIV-1)[1]. | ||||||||||||
Invitro | BMS-707035 has antiviral activity with EC50 values of 2 nM and 17 nM in the presence of 10% FBS and 15 mg/mL human serum albumin, respectively[1].BMS-707035 has high plasma protein binding and not overtly cytotoxicy to several cell lines, with CC50 value of ≥45 μM[1].BMS-707035 has a relatively weak CYP inhibiton with IC50 value of ≥40 μM[1]. | ||||||||||||
In Vivo | BMS-707035 has a low clearance effect in the rat, dog and monkey with moderate to long elimination half-lives in all species[1].Pharmacokinetic Parameters of BMS-707035 in rat, dog and monkey (IV)[1]. | ||||||||||||
Name | BMS-707035 | ||||||||||||
CAS | 729607-74-3 | ||||||||||||
Formula | C17H19FN4O5S | ||||||||||||
Molar Mass | 410.42 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. B Narasimhulu Naidu, et al. The discovery and preclinical evaluation of BMS-707035, a potent HIV-1 integrase strand transfer inhibitor. Bioorg Med Chem Lett. 2018 Jul 1;28(12):2124-2130. |