Stavudine (d4T)

製品コードS1398 バッチS139803

化学情報

	Synonyms	BMY-27857, Sanilvudine, NSC 163661,d4T	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₀H₁₂N₂O₄
	分子量	224.21	CAS No.	3056-17-5
Solubility (25°C)*	体外	DMSO	49 mg/mL (218.54 mM)
		Ethanol	24 mg/mL (107.04 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

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

プロトコル(参考用のみ)

参考

[4] Gaou I, et al. J Pharmacol Exp Ther, 2001, 297(2), 516-523.

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Condensin-mediated restriction of retrotransposable elements facilitates brain development in Drosophila melanogaster. [ bioRxiv, 2024, 10.1101/2024.01.22.576652]	PubMed: none
Seasonal coronavirus infections trigger NLRP3 inflammasome activation in macrophages but is therapeutically targetable [ Antiviral Res, 2023, 216:105674]	PubMed: 37459896
Reverse Transcriptase Inhibition Disrupts Repeat Element Life Cycle in Colorectal Cancer [ Cancer Discov, 2022, candisc.1117.2021]	PubMed: 35320348
The antiretroviral agents azidothymidine, stavudine, and didanosine have the identical mutational fingerprint in the rpoB region of Escherichia coli [ Environ Mol Mutagen, 2022, 3(7):329-335.]	PubMed: 36066544
Reverse transcriptase inhibition potentiates target therapy in BRAF-mutant melanomas: effects on cell proliferation, apoptosis, DNA-damage, ROS induction and mitochondrial membrane depolarization [ Cell Commun Signal, 2020, 18(1):150]	PubMed: 32933538
Altered Gut Microbiome under Antiretroviral Therapy: Impact of Efavirenz and Zidovudine [ ACS Infect Dis, 2020, 10.1021/acsinfecdis.0c00536]	PubMed: 33346662
How to Control HTLV-1-Associated Diseases: Preventing de Novo Cellular Infection Using Antiviral Therapy. [ Front Microbiol, 2018, 9:278]	PubMed: 29593659

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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