Dapivirine


CAS No. : 244767-67-7

(Synonyms: TMC120; R147681)

244767-67-7
Price and Availability of CAS No. : 244767-67-7
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Cat. No. : HY-14266
M.Wt: 329.41
Formula: C20H19N5
Purity: >98 %
Solubility: DMSO : ≥ 47 mg/mL
Introduction of 244767-67-7 :

Dapivirine (TMC120), the prototype of diarylpyrimidines (DAPY), is an orally active and nonnucleoside reverse transcriptase inhibitor (NRTI). Dapivirine (TMC120) binds directly to HIV-1 reverse transcriptase. Dapivirine (TMC120) regulates autophagy and induced Akt, Bad and SAPK/JNK activations[1][2]. In Vitro: Dapivirine (4-64 μM, 24, 48, 72, 96 and 120 hours) inhibits proliferation of glioma cells and induces apoptosis (16 μM, 12-48 h)[1].
Dapivirine (8 and 16 μM, 12 h) enhances invasion of glioma cells[1].
Dapivirine (16 μM, 12 h, 24 h and 48 h) promotes autophagy in U87 cells[1].
Dapivirine (TMC120-R147681) apparently blocks infection in the primary cultures at a 10 nM concentration, but secondary cultures revealed that a 100 nM concentration was needed to completely prevent proviral integration[3].
In Vivo: Dapivirine (16 mg/kg, once every 3 days for 12 days) exhibits potent antitumor activity in human glioblastoma models in mice[1].
Dapivirine has been shown to have a half-life in the range of 65 to 90 h[4].

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