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Cat.No.S1398
| Related Targets | Integrase Bacterial Antibiotics Anti-infection Fungal Antiviral COVID-19 Parasite HIV HCV Protease |
|---|---|
| Other Reverse Transcriptase Inhibitors | Dapivirine (TMC120) Salicylanilide Fangchinoline Bifendate 3'-Fluoro-3'-deoxythymidine (Alovudine) Ulonivirine Lersivirine (UK-453061) 4-Chloro-2-(trifluoroacetyl)aniline hydrochloride |
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In vitro |
DMSO
: 49 mg/mL
(218.54 mM)
Ethanol : 24 mg/mL Water : Insoluble |
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In vivo |
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| Molecular Weight | 224.21 | Formula | C10H12N2O4 |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 3056-17-5 | Download SDF | Storage of Stock Solutions |
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| Synonyms | BMY-27857, Sanilvudine, NSC 163661,d4T | Smiles | CC1=CN(C(=O)NC1=O)C2C=CC(O2)CO | ||
| Targets/IC50/Ki |
Reverse transcriptase
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|---|---|
| In vitro |
Stavudine (d4T) alters 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. It drives 5-10% of 3T3-F442A cells towards apoptosis, and reduces the lipid content and survival of differentiated 3T3-L1 adipocytes. This compound increases mitochondrial mass by two to fourfold, and lowers the mitochondrial membrane potential (JC-1 stain). It inhibits p24 antigen production by HIV-I in PBMC with EDsos ranging from 0.04 μM to 0.2 μM. It also 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. Its treatment elevates mitochondrial reactive oxygen species (ROS), enhances mitochondrial oxidative stress, and contributes mechanistically to NRTI-induced toxicity.
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| In vivo |
Stavudine (d4T) (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. It can decrease hepatic and muscle mtDNA in lean mice and can also cause ketoacidosis during fasting without altering mtDNA. This compound depletes WAT mtDNA only in obese mice.
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References |
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(data from https://clinicaltrials.gov, updated on 2024-05-22)
| 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 |
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