product name Stavudine (d4T)
Description: Stavudine (also known as BMY-27857, Sanilvudine, NSC 163661, and d4T) is a nucleoside analog reverse transcriptase inhibitor (NARTI) active against HIV. 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.
References: AIDS. 2004 Nov 5;18(16):2127-36; Toxicol Appl Pharmacol. 2004 Aug 15;199(1):10-9.
224.21
Formula
C10H12N2O4
CAS No.
3056-17-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 45 mg/mL (200.7 mM)
Water: <1 mg/mL
Ethanol: 15 mg/mL (66.9 mM)
Solubility (In vivo)
0.5% CMC Na: 30mg/mL
Synonyms
BMY-27857, Sanilvudine, NSC 163661
other peoduct :
| In Vitro |
In vitro activity: 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). Stavudine inhibits p24 antigen production by HIV-I in PBMC with EDsos ranging from 0.04 μM to 0.2 μM. 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. Kinase Assay: Cell Assay: |
|---|---|
| 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. |
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| References | IDS. 2004 Nov 5;18(16):2127-36; Toxicol Appl Pharmacol. 2004 Aug 15;199(1):10-9; J Pharmacol Exp Ther. 2001 May;297(2):516-23. |
