Doravirine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Doravirine (MK-1439、MK1439) 是一种新型、高度特异性的 HIV-1 非核苷逆转录酶抑制剂 (NNRTI)，针对 WT、K103N 和 Y181C 逆转录酶 (RT) 突变体的 IC50 分别为 12、9.7 和 9.7 nM。

Doravirine (MK-1439, MK1439) is a novel, highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor (NNRTI) with IC50 of 12, 9.7, and 9.7 nM against WT, K103N, and Y181C reverse transcriptase (RT) mutants, respectively, in a biochemical assay; shows excellent potency in suppressing the replication of WT virus with EC95 of 20 nM, as well as K103N, Y181C, and K103N/Y181C mutant viruses with EC95 of 43, 27, and 55 nM, respectively.HIV Infection Phase 3 Clinical(In Vitro):Selectivity and cytotoxicity studies confirmed that Doravirine is a highly specific nonnucleoside reverse transcriptase inhibitors with minimum off-target activities. In the presence of 50% normal human serum (NHS), Doravirine shows excellent potency in suppressing the replication of WT virus, with a 95% effective concentration (EC95) of 20 nM, as well as K103N, Y181C, and K103N/Y181C mutant viruses with EC9595 of 43, 27, and 55 nM, respectively. Doravirine exhibits similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses).(In Vivo):Administration of 50 mg Doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity and C24 h with no change in Cmax.

Selectivity and cytotoxicity studies confirmed that Doravirine is a highly specific nonnucleoside reverse transcriptase inhibitorswith minimum off-target activities. In the presence of 50% normal human serum (NHS), Doravirine shows excellent potency in suppressing the replication of WT virus, with a 95% effective concentration (EC95) of 20 nM, as well as K103N, Y181C, and K103N/Y181C mutant viruses with EC9595 of 43, 27, and 55 nM, respectively. Doravirine exhibits similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses).

Administration of 50 mg Doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity and C24 h with no change in Cmax.

MK-1439 | MK1439

Microbiology/Virology

HIV

HIV-1

Infection

HIV Infection

1338225-97-0

425.7491

C17H11ClF3N5O3

>98% (HPLC)

DMSO: ≥ 30 mg/mL

N#CC1=CC(OC2=C(C(F)(F)F)C=CN(CC(N3C)=NNC3=O)C2=O)=CC(Cl)=C1

Benzonitrile, 3-chloro-5-[[1-[(4,5-dihydro-4-methyl-5-oxo-1H-1,2,4-triazol-3-yl)methyl]-1,2-dihydro-2-oxo-4-(trifluoromethyl)-3-pyridinyl]oxy]-

(-20℃)

With Ice Pack

≥ 2 years