634907-30-5

634907-30-5 structure

Name: Censavudine
Chemical Name: 1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2H-furan-2-yl]-5-methylpyrimidine-2,4-dione
CAS Number: 634907-30-5
Molecular Formula: C₁₂H₁₂N₂O₄
Molecular Weight: 248.23500
Catalog: Signaling Pathways Anti-infection HIV
Create Date: 2016-08-02 07:54:46
Modify Date: 2024-01-11 22:00:21
Censavudine (OBP-601; BMS-986001), a nucleoside analog, is a nucleoside reverse transcriptase inhibitor. Censavudine is a potent HIV inhibitor with EC50 ranges from 30 nM to 81 nM and 450 nM to 890 nM for HIV-2 and HIV-1, respectively[1][2].

Name	1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2H-furan-2-yl]-5-methylpyrimidine-2,4-dione
Synonyms	UNII-6IE83O6NGA Censavudine 4'-ethynylstavudine 4'-Ed4T 4'-Ethynyl-d4T Ed4T OBP-601 Festinavir BMS-986001

Description	Censavudine (OBP-601; BMS-986001), a nucleoside analog, is a nucleoside reverse transcriptase inhibitor. Censavudine is a potent HIV inhibitor with EC50 ranges from 30 nM to 81 nM and 450 nM to 890 nM for HIV-2 and HIV-1, respectively[1][2].
Related Catalog	Signaling Pathways >> Anti-infection >> HIV Research Areas >> Infection Signaling Pathways >> Cell Cycle/DNA Damage >> Nucleoside Antimetabolite/Analog Signaling Pathways >> Anti-infection >> Reverse Transcriptase
Target	HIV-2:30-81 nM (EC50) HIV-1:450-890 nM (IC50)
In Vitro	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)[1]. BMS-986001 also exhibits full activity against HIV-2 variants whose genomes encoded the single amino acid changes K65R and Q151M in reverse transcriptase[1].
In Vivo	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[2].
References	[1]. Robert A Smith, et al. The Nucleoside Analog BMS-986001 Shows Greater In Vitro Activity Against HIV-2 Than Against HIV-1. Antimicrob Agents Chemother. 2015 Dec;59(12):7437-46. [2]. Long Yuan, et al. Dried Blood Spot Analysis Without Dilution: Application to the LC-MS/MS Determination of BMS-986001 in Rat Dried Blood Spot. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Oct 1;1002:201-9.

Molecular Formula	C₁₂H₁₂N₂O₄
Molecular Weight	248.23500
Exact Mass	248.08000
PSA	84.58000

Hazard Codes	Xi

1158522-08-7	940364-43-2
134104-43-1	131615-57-1
1713477-38-3	2230200-71-0
6906-52-1	930439-75-1
1018584-77-4	1375289-11-4