Stavudine (d4T)

Synonyms: BMY-27857, Sanilvudine, NSC 163661,d4T

Stavudine (d4T, BMY-27857, Sanilvudine, NSC 163661) is a nucleoside analog reverse transcriptase inhibitor (NARTI) active against HIV.

Stavudine (d4T) Chemical Structure

Stavudine (d4T) Chemical Structure

CAS No. 3056-17-5

Purity & Quality Control

Stavudine (d4T) Related Products

Biological Activity

Description Stavudine (d4T, BMY-27857, Sanilvudine, NSC 163661) is a nucleoside analog reverse transcriptase inhibitor (NARTI) active against HIV.
Targets
Reverse transcriptase [1]
In vitro
In vitro Stavudine alteres the lipid phenotype, decreasing the lipid content and expression of markers involved in lipid metabolism, namely C/EBPalpha, peroxisome proliferator-activated receptor gamma, adipocyte lipid binding protein 2, fatty acid synthase and acetyl-coenzyme A carboxylase. Stavudine drives 5-10% of 3T3-F442A cells towards apoptosis, and reduces the lipid content and survival of differentiated 3T3-L1 adipocytes. Stavudine increases mitochondrial mass by two to fourfold, and loweres the mitochondrial membrane potential (JC-1 stain). [1] stavudine inhibits p24 antigen production by HIV-I in PBMC with EDsos ranging from 0.04 μM to 0.2 μM. [2] Stavudine produces significant mitochondrial dysfunction with a 1.5-fold increase in cellular lactate to pyruvate ratios. Stavudine causes a dose-dependent decrease in mtDNA amplification and a correlative increase in abundance of markers of mitochondrial oxidative stress. Stavudine treatment elevates mitochondrial reactive oxygen species (ROS), enhances mitochondrial oxidative stress, and contributes mechanistically to NRTI-induced toxicity. [3]
In Vivo
In vivo Stavudine (500 mg/kg/day) results in lack of significant oxidative mtDNA lesions (as assessed by long polymerase chain reaction experiments), and normal blood lactate/pyruvate ratios in lean mice. Stavudine (500 mg/kg/day) can decrease hepatic and muscle mtDNA in lean mice and can also cause ketoacidosis during fasting without altering mtDNA. Stavudine (500 mg/kg/day) depletes WAT mtDNA only in obese mice. [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01178684 Completed
HIV
SEARCH Research Foundation|University of Hawaii
May 2010 --
NCT00455585 Completed
HIV Infections
Makerere University|Department of Foreign Affairs Ireland
January 2007 Phase 4
NCT00235222 Unknown status
HIV
Groupe Hospitalier Pitie-Salpetriere|Bristol-Myers Squibb
June 2004 Phase 4
NCT00116116 Completed
HIV Infections|AIDS
Bristol-Myers Squibb
March 2002 Phase 4

Chemical Information & Solubility

Molecular Weight 224.21 Formula

C10H12N2O4

CAS No. 3056-17-5 SDF Download Stavudine (d4T) SDF
Smiles CC1=CN(C(=O)NC1=O)C2C=CC(O2)CO
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 45 mg/mL ( (200.7 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 45 mg/mL

Ethanol : 20 mg/mL


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In vivo
Batch:

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In vivo Formulation Calculator

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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