Didanosine

製品コードS1702 バッチS170201

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₀H₁₂N₄O₃
	分子量	236.23	CAS No.	69655-05-6
Solubility (25°C)*	体外	DMSO	47 mg/mL (198.95 mM)
		Water	Insoluble
		Ethanol	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	Didanosine is a reverse transcriptase inhibitor with an IC50 of 0.49 μM.
in vitro	Didanosine induces cytoplasmic lipid droplet accumulations, increases lactate production and decreases activities of COX (complex IV) and SDH (part of complex II) in cultured human muscle cells. ^[1] Didanosine is converted to its active moiety, dideoxyadenosine-5'-triphosphate (ddATP), which inhibits HIV reverse transcriptase and terminates viral DNA growth in the target cell for HIV. ^[2] Didanosine induces dose-dependent decreases in neurite number, length of the longest neurite in each neuron, and total neurite length per neuron in dissociated DRG cell cultures with 3 days treatment. Didanosine induces a neurite retraction or neurite loss in a dose-dependent manner in dissociated DRG neurons, suggesting that Didanosine may partially contribute to developing peripheral neuropathy. ^[3] Didanosine potentiates the mutagenicity of Zidovudine in the thymidine kinase (TK) gene of cultured human TK6 lymphoblastoid cells. Didanosine combined with Zidovudine causes a significant increase in micronucleated PCEs and induces a significant increase in Tk mutants, which is associated with loss of the wild-type Tk+ allele. ^[4] Didanosine depletes mitochondrial DNA (mtDNA) in cultured hepatocytes, this mtDNA depletion is associated with an increased in vitro production of lactate. ^[5]

製品説明

Didanosine is a reverse transcriptase inhibitor with an IC50 of 0.49 μM.

in vitro

Didanosine induces cytoplasmic lipid droplet accumulations, increases lactate production and decreases activities of COX (complex IV) and SDH (part of complex II) in cultured human muscle cells. ^[1] Didanosine is converted to its active moiety, dideoxyadenosine-5'-triphosphate (ddATP), which inhibits HIV reverse transcriptase and terminates viral DNA growth in the target cell for HIV. ^[2] Didanosine induces dose-dependent decreases in neurite number, length of the longest neurite in each neuron, and total neurite length per neuron in dissociated DRG cell cultures with 3 days treatment. Didanosine induces a neurite retraction or neurite loss in a dose-dependent manner in dissociated DRG neurons, suggesting that Didanosine may partially contribute to developing peripheral neuropathy. ^[3] Didanosine potentiates the mutagenicity of Zidovudine in the thymidine kinase (TK) gene of cultured human TK6 lymphoblastoid cells. Didanosine combined with Zidovudine causes a significant increase in micronucleated PCEs and induces a significant increase in Tk mutants, which is associated with loss of the wild-type Tk+ allele. ^[4] Didanosine depletes mitochondrial DNA (mtDNA) in cultured hepatocytes, this mtDNA depletion is associated with an increased in vitro production of lactate. ^[5]

プロトコル(参考用のみ)

参考

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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：

Biological and Structural Analyses of New Potent Allosteric Inhibitors of HIV-1 Integrase [ Antimicrob Agents Chemother, 2023, 67(7):e0046223]	PubMed: 37310224
Piperacetazine Directly Binds to the PAX3::FOXO1 Fusion Protein and Inhibits Its Transcriptional Activity [ Cancer Res Commun, 2023, 3(10):2030-2043]	PubMed: 37732905
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
PARP1 depletion induces RIG-I-dependent signaling in human cancer cells [ PLoS One, 2018, 13(3):e0194611]	PubMed: 29590171
Repression of Stress-Induced LINE-1 Expression Protects Cancer Cell Subpopulations from Lethal Drug Exposure. [ Cancer Cell, 2017, 32(2):221-237]	PubMed: 28781121

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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