Censavudine - 98%, high purity , Reverse transcriptase inhibitor, CAS No.634907-30-5, Reverse transcriptase inhibitor

  • ≥98%
Item Number
C648939
Grouped product items
SKUSizeAvailabilityPrice Qty
C648939-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$620.90
C648939-10mg
10mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$980.90
C648939-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$1,950.90

Basic Description

SynonymsCensavudine | 4'-ethynyl stavudine | Censavudine (USAN) | CS-0012405 | 4'-Ethynyl D4T | OSYWBJSVKUFFSU-SKDRFNHKSA-N | UNII-6IE83O6NGA | BMS-986001 | CHEMBL124363 | 1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2,5-dihydrofuran-2-yl]-5-methylpyrimidine-2,4(1H,3H)
Specifications & Purity≥98%
Biochemical and Physiological MechanismsCensavudine (OBP-601; BMS-986001), a nucleoside analog , is a nucleoside reverse transcriptase inhibitor. Censavudine is a potent HIV inhibitor with EC 50 ranges from 30 nM to 81 nM and 450 nM to 890 nM for HIV-2 and HIV-1 , respectively.
Storage TempStore at 2-8°C,Desiccated
Shipped InWet ice
Action TypeINHIBITOR
Mechanism of actionReverse transcriptase inhibitor
Product Description

Censavudine (OBP-601; BMS-986001), a nucleoside analog , is a nucleoside reverse transcriptase inhibitor. Censavudine is a potent HIV inhibitor with EC 50 ranges from 30 nM to 81 nM and 450 nM to 890 nM for HIV-2 and HIV-1 , respectively

In Vitro

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:HIV-2 30-81 nM (EC 50 ) HIV-1 450-890 nM (IC 50 )

Product Properties

ALogP-0.7

Associated Targets(Human)

TK1 Tchem Thymidine kinase, cytosolic (627 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CCRF-CEM (65223 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MT2 (2907 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MT4 (17854 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
RKO (1376 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Human immunodeficiency virus 1 (70413 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name 1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2H-furan-2-yl]-5-methylpyrimidine-2,4-dione
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
InChi Key OSYWBJSVKUFFSU-SKDRFNHKSA-N
Canonical SMILES CC1=CN(C(=O)NC1=O)C2C=CC(O2)(CO)C#C
Isomeric SMILES CC1=CN(C(=O)NC1=O)[C@H]2C=C[C@](O2)(CO)C#C
Alternate CAS 634907-30-5,1097733-37-3
PubChem CID 3008897
Molecular Weight 248.23

Certificates

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Chemical and Physical Properties

SolubilityDMSO : 52 mg/mL (209.48 mM; Need ultrasonic) H2O : 10 mg/mL (40.29 mM; ultrasonic and warming and heat to 60°C)

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