FESTINAVIR

FESTINAVIR化学性质

熔点 :207-209℃
密度 :1.42±0.1 g/cm3(Predicted)
储存条件 :4°C, away from moisture
溶解度 :DMSO : 52 mg/mL (209.48 mM; Need ultrasonic)
酸度系数(pKa) :9.47±0.10(Predicted)
形态 :Solid
颜色 :Light yellow to yellow
InChI :InChI=1S/C12H12N2O4/c1-3-12(7-15)5-4-9(18-12)14-6-8(2)10(16)13-11(14)17/h1,4-6,9,15H,7H2,2H3,(H,13,16,17)/t9-,12+/m1/s1
InChIKey :OSYWBJSVKUFFSU-SKDRFNHKSA-N
SMILES :OC[C@@]1(C#C)O[C@@H](N2C=C(C)C(=O)NC2=O)C=C1

FESTINAVIR性质、用途与生产工艺

生物活性 Censavudine (OBP-601; BMS-986001)，一种核苷类似物，是一种核苷逆转录酶 (nucleoside reverse transcriptase) 抑制剂。Censavudine 是一种有效的 HIV 抑制剂，对 HIV-2 和 HIV-1 的 EC50 范围分别为 30-81 nM 和 450-890 nM。
靶点

HIV-2

30-81 nM (EC ₅₀ )

HIV-1

450-890 nM (IC ₅₀ )
体外研究

BMS-986001 shows greater activity against HIV-2 _ROD9 than against HIV-1 _NL4-3 ; the mean EC ₅₀ s for BMS-986001 are 74 nM for HIV-2 _ROD9 and 890 nM for HIV-1 _NL4-3 in the single-cycle assay. HIV-2 _ROD9 also showes greater sensitivity to BMS-986001 in 4-day infections of an immortalized T cell line (CEMss), with the mean EC ₅₀ for HIV-2 _ROD9 (EC ₅₀ of 0.14 nM) being 30-fold lower than that for HIV-1 _NL4-3 (EC ₅₀ 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.
体内研究

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 _max for 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.

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FESTINAVIR 试剂级价格

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