1. Anti-infection
    Cell Cycle/DNA Damage
  2. HIV
    Reverse Transcriptase
    Nucleoside Antimetabolite/Analog
  3. Censavudine

Censavudine (Synonyms: OBP-601; BMS-986001)

Cat. No.: HY-16776
Handling Instructions

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.

For research use only. We do not sell to patients.

Censavudine Chemical Structure

Censavudine Chemical Structure

CAS No. : 634907-30-5

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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].

IC50 & Target[1]

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].

Molecular Weight

248.23

Formula

C₁₂H₁₂N₂O₄

CAS No.

634907-30-5

SMILES

C#C[[email protected]@]1(O[[email protected]](N(C=C2C)C(NC2=O)=O)([H])C=C1)CO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

CensavudineOBP-601BMS-986001OBP601OBP 601BMS986001BMS 986001HIVReverse TranscriptaseNucleoside Antimetabolite/AnalogHuman immunodeficiency virusHIV-2transcriptaseHIV-1replicationnucleosideinfectionInhibitorinhibitorinhibit

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