BMS-986001

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

一种胸苷类似物核苷逆转录酶抑制剂 (NRTI)，可抑制从未治疗过的个体中分离出的 HIV-2，EC50 为 30-81 nM。

A thymidine analogue nucleoside reverse transcriptase inhibitor (NRTI) that inhibits HIV-2 isolates from treatment-naive individuals with EC50 of 30-81 nM; inhibits isolates of HIV-1 with EC50 of 450-890 nM, also exhibits full activity against HIV-2 variants whose genomes encoded the single amino acid changes K65R and Q151M in reverse transcriptase.HIV Infection Phase 2 Clinical.

BMS-986001 shows greater activity against HIV-2ROD9 than against HIV-1NL4-3; the mean EC50s for BMS-986001 are 74 nM for HIV-2ROD9 and 890 nM for HIV-1NL4-3 in the single-cycle assay. HIV-2ROD9 also showes greater sensitivity to BMS-986001 in 4-day infections of an immortalized T cell line (CEMss), with the mean EC50 for HIV-2ROD9 (EC50 of 0.14 nM) being 30-fold lower than that for HIV-1NL4-3 (EC50 of 4.2 nM). BMS-986001 also exhibits full activity against HIV-2 variants whose genomes encoded the single amino acid changes K65R and Q151M in reverse transcriptase.

The pharmacokinetic parameters of Censavudine (BMS-986001; 100-750 mg/kg) generated from the dried blood spot (DBS) assay and the plasma assay is compared. The ratios of the AUC(0-24 h) and C maxfor BMS-986001 in DBS compared to those in plasma are consistent at 0.83-0.91 and 0.81-0.97, respectively, across all dose groups in rats. The T max in rat DBS and plasma are also consistent at about 1 h.

BMS 986001 | Censavudine | Festinavir | OBP-601 | 4'-Ed4T

Microbiology/Virology

HIV

HIV

Infection

HIV Infection

634907-30-5

248.238

C12H12N2O4

>98% (HPLC)

In Vitro:?DMSO : 52 mg/mL (209.48 mM)

O=C1NC(C(C)=CN1[C@@H]2O[C@@](CO)(C#C)C=C2)=O

1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2,5-dihydrofuran-2-yl]-5-methylpyrimidine-2,4(1H,3H)-dione

(-20℃)

With Ice Pack

≥ 2 years