An inhibitor of HIV capsid protein-protein interactions
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Lenacapavir

Item No. 41830

Technical Information
Formal Name
(3bS,4aR)-N-[(1S)-1-[3-[4-chloro-3-[(methylsulfonyl)amino]-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl]-6-[3-methyl-3-(methylsulfonyl)-1-butyn-1-yl]-2-pyridinyl]-2-(3,5-difluorophenyl)ethyl]-5,5-difluoro-3b,4,4a,5-tetrahydro-3-(trifluoromethyl)-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazole-1-acetamide
CAS Number
2189684-44-2
Synonyms
  • GS-6207
  • GS-714207
  • GS-CA2
Molecular Formula
C39H32ClF10N7O5S2
Formula Weight
Purity
≥98%
A solid
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
O=C(N[C@H](C1=C(C(C=C2)=C(N3CC(F)(F)F)C(C(NS(C)(=O)=O)=N3)=C2Cl)C=CC(C#CC(C)(C)S(C)(=O)=O)=N1)CC4=CC(F)=CC(F)=C4)CN5N=C(C(F)(F)F)C6=C5C(F)(F)[C@@]7([H])[C@]6([H])C7
InChi Code
InChI=1S/C39H32ClF10N7O5S2/c1-36(2,63(3,59)60)10-9-21-5-6-22(23-7-8-26(40)30-32(23)57(17-37(43,44)45)54-35(30)55-64(4,61)62)31(51-21)27(13-18-11-19(41)14-20(42)12-18)52-28(58)16-56-34-29(33(53-56)39(48,49)50)24-15-25(24)38(34,46)47/h5-8,11-12,14,24-25,27H,13,15-17H2,1-4H3,(H,52,58)(H,54,55)/t24-,25+,27-/m0/s1
InChi Key
BRYXUCLEHAUSDY-WEWMWRJBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Lenacapavir is an inhibitor of the protein-protein interaction between HIV capsid protein and various HIV proteins involved in viral replication.1 It inhibits viral replication in HIV-1-infected primary human CD4+ T cells and macrophages (mean IC50s = 32 and 56 pM, respectively), two HIV-2 clinical isolates (mean IC50 = 885 pM), and 23 HIV-1 clinical isolates (mean IC50 = 50 pM). Lenacapavir (25 mg/kg, s.c.) prevents simian-tropic HIV-1 (stHIV-A19) infection in pigtail macaques.2 Formulations containing lenacapavir have been used in the treatment of HIV-1.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Link, J.O., Rhee, M.S., Tse, W.C., et al. Clinical targeting of HIV capsid protein with a long-acting small molecule. Nature 584(7822), 614-618 (2020).

    2. Swanstrom, A.E., Gorelick, R.J., Welker, J.L., et al. Long-acting lenacapavir protects macaques against intravenous challenge with simian-tropic HIV. EBioMedicine 95, 104764 (2023).