Bioactivity | Lenacapavir (GS-6207) is a HIV-1 capsid inhibitor. Lenacapavir shows anti-HIV activity with an EC50 of 100 pM in MT-4 cells. Lenacapavir displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs)[1]. | ||||||||||||
Target | EC50: 100 pM (anti-HIV; in MT-4 cells) | ||||||||||||
Invitro | Lenacapavir (GS-6207) is a potent capsid-targeting inhibitor of HIV replication. Lenacapavir shows sub-nanomolar potency in target cells (EC50=23 pM), in a full-cycle assay (EC50=25 pM) and in producer cells (EC50=439 pM). Lenacapavir interferes with both the early and late stages of HIV-1 replication but exhibits greater potency against the early stage[2]. | ||||||||||||
Name | Lenacapavir | ||||||||||||
CAS | 2189684-44-2 | ||||||||||||
Formula | C39H32ClF10N7O5S2 | ||||||||||||
Molar Mass | 968.28 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Singh K, et al. GS-CA Compounds: First-In-Class HIV-1 Capsid Inhibitors Covering Multiple Grounds. Front Microbiol. 2019 Jun 20;10:1227. [2]. John O Link, et al. Clinical targeting of HIV capsid protein with a long-acting small molecule. Nature. 2020 Jul 1. |