For research use only. Not for therapeutic Use.
Dapivirine (Cat No.:I002825) is a non-nucleoside inhibitor of HIV reverse transcriptase with IC50 of 24 nM, and inhibits multiple different types of HIV-1 isolates, including multiple NNRTI-resistant isolates. If you need, please contact us in time, and we will reply to you as soon as possible within 24 hours.
| Catalog Number | I002825 |
| CAS Number | 244767-67-7 |
| Synonyms | 4-[[4-(2,4,6-trimethylanilino)pyrimidin-2-yl]amino]benzonitrile |
| Molecular Formula | C20H19N5 |
| Purity | ≥95% |
| Target | HIV |
| Solubility | DMSO: ≥ 47 mg/mL |
| Storage | under inert gas (nitrogen or Argon) at 2–8 °C |
| IC50 | 24 nM [1] |
| IUPAC Name | 4-[[4-(2,4,6-trimethylanilino)pyrimidin-2-yl]amino]benzonitrile |
| InChI | InChI=1S/C20H19N5/c1-13-10-14(2)19(15(3)11-13)24-18-8-9-22-20(25-18)23-17-6-4-16(12-21)5-7-17/h4-11H,1-3H3,(H2,22,23,24,25) |
| InChIKey | ILAYIAGXTHKHNT-UHFFFAOYSA-N |
| SMILES | CC1=CC(=C(C(=C1)C)NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C |
| Reference | </br>1:<i>In Vitro</i> Cross-Resistance Profiles of Rilpivirine, Dapivirine and MIV-150: NNRTI Microbicides in Clinical Development for the Prevention of HIV-1 Infection. Giacobbi NS, Sluis-Cremer N.Antimicrob Agents Chemother. 2017 May 15. pii: AAC.00277-17. doi: 10.1128/AAC.00277-17. [Epub ahead of print] PMID: 28507107 </br>2:Packing polymorphism of dapivirine and its impact on the performance of a dapivirine-releasing silicone elastomer vaginal ring. McCoy CF, Murphy DJ, Boyd P, Derrick T, Spence P, Devlin B, Malcolm RK.J Pharm Sci. 2017 Apr 26. pii: S0022-3549(17)30261-7. doi: 10.1016/j.xphs.2017.04.026. [Epub ahead of print] PMID: 28456732 </br>3:Acceptability and use of a dapivirine vaginal ring in a phase III trial. Montgomery ET, van der Straten A, Chitukuta M, Reddy K, Woeber K, Atujuna M, Bekker LG, Etima J, Nakyanzi T, Mayo AJ, Katz A, Laborde N, Grossman CI, Soto-Torres L, Palanee-Phillips T, Baeten JM; MTN-020/ASPIRE Study..AIDS. 2017 May 15;31(8):1159-1167. doi: 10.1097/QAD.0000000000001452. PMID: 28441175 </br>4:Dapivirine Vaginal Ring for HIV-1 Prevention. Winceslaus SJ.N Engl J Med. 2017 Mar 9;376(10):994-5. doi: 10.1056/NEJMc1616546. No abstract available. PMID: 28276229 </br>5:Dapivirine Vaginal Ring for HIV-1 Prevention. Seidman D, Weber S, Aaron E.N Engl J Med. 2017 Mar 9;376(10):995. doi: 10.1056/NEJMc1616546. No abstract available. PMID: 28273024 </br>6:Dapivirine Vaginal Ring for HIV-1 Prevention. Baeten JM, Brown ER, Hillier SL.N Engl J Med. 2017 Mar 9;376(10):995-6. doi: 10.1056/NEJMc1616546. No abstract available. PMID: 28273023 Free Article</br>7:Infection: Dapivirine ring reduces HIV acquisition. Fenner A.Nat Rev Urol. 2017 Feb;14(2):68. doi: 10.1038/nrurol.2016.263. Epub 2016 Dec 20. No abstract available. PMID: 27995936 </br>8:Safety and Efficacy of a Dapivirine Vaginal Ring for HIV Prevention in Women. Nel A, van Niekerk N, Kapiga S, Bekker LG, Gama C, Gill K, Kamali A, Kotze P, Louw C, Mabude Z, Miti N, Kusemererwa S, Tempelman H, Carstens H, Devlin B, Isaacs M, Malherbe M, Mans W, Nuttall J, Russell M, Ntshele S, Smit M, Solai L, Spence P, Steytler J, Windle K, Borremans M, Resseler S, Van Roey J, Parys W, Vangeneugden T, Van Baelen B, Rosenberg Z; Ring Study Team..N Engl J Med. 2016 Dec 1;375(22):2133-2143. PMID: 27959766 Free Article</br>9:Frequent Cross-Resistance to Dapivirine in HIV-1 Subtype C-Infected Individuals after First-Line Antiretroviral Therapy Failure in South Africa. Penrose KJ, Wallis CL, Brumme CJ, Hamanishi KA, Gordon KC, Viana RV, Harrigan PR, Mellors JW, Parikh UM.Antimicrob Agents Chemother. 2017 Jan 24;61(2). pii: e01805-16. doi: 10.1128/AAC.01805-16. Print 2017 Feb. PMID: 27895013 </br>10:Comparison of Dapivirine Vaginal Gel and Film Formulation Pharmacokinetics and Pharmacodynamics (FAME 02B). Robinson JA, Marzinke MA, Bakshi RP, Fuchs EJ, Radebaugh CL, Aung W, Spiegel HM, Coleman JS, Rohan LC, Hendrix CW.AIDS Res Hum Retroviruses. 2017 Apr;33(4):339-346. doi: 10.1089/AID.2016.0040. Epub 2016 Dec 13. PMID: 27809557 |
