Terbinafine HCl

製品コードS2557 バッチS255702

化学情報

	Synonyms	KWD 201,KWD 2019,TDT 067 hydrochloride	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₁H₂₅N.HCl
	分子量	327.89	CAS No.	78628-80-5
Solubility (25°C)*	体外	DMSO	65 mg/mL (198.23 mM)
		Ethanol	65 mg/mL (198.23 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.

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生物活性

製品説明	Terbinafine HCl (KWD 201,KWD 2019,TDT 067 hydrochloride) inhibits ergosterol synthesis by inhibiting squalene epoxidase, used as an antifungal drug.
in vitro	Terbinafine (50 μM to 100 μM) inhibits only marginally the metabolism of ethoxycoumarin (CYP1A2), tolbutamide (CYP2C9), or ethynylestradiol, CsA, and cortisol. Terbinafine proves to be a potent inhibitor of the CYP2D6-mediated dextromethorphan O-demethylation and bufuralol 1-hydroxylation with IC50values of 0.2 μM and 0.25 μM, respectively. ^[1] Terbinafine is highly activ Aspergillus isolates (minimum inhibitory concentration [MIC] 0.01 to 2 mg/mL) with a primary fungicidal action (minimum fungicidal concentration [MFC] 0.02 to 4 mg/mL). ^[2] Terbinafine inhibits dextromethorphan O-demethylation with an apparent Ki ranging from 28 to 44 nM in human hepatic microsomes and averaging 22.4 nM for the heterologously expressed enzymes. ^[3] Terbinafine shows a very strong activity in vitro against Penicillium spp., Paecilomyces spp., Trichoderma spp., Acremonium spp. and Arthrographis spp. with GMs <1 mg/L. ^[4] Terbinafine decreases the levels of phosphorylated extracellular signal-regulated kinase (ERK). Terbinafine might cause a decrease of MEK, which in turn up-regulates p53 through the inhibition of ERK phosphorylation, and finally causes an increase of p21expression and cell-cycle arrest. ^[5]

製品説明

Terbinafine HCl (KWD 201,KWD 2019,TDT 067 hydrochloride) inhibits ergosterol synthesis by inhibiting squalene epoxidase, used as an antifungal drug.

in vitro

Terbinafine (50 μM to 100 μM) inhibits only marginally the metabolism of ethoxycoumarin (CYP1A2), tolbutamide (CYP2C9), or ethynylestradiol, CsA, and cortisol. Terbinafine proves to be a potent inhibitor of the CYP2D6-mediated dextromethorphan O-demethylation and bufuralol 1-hydroxylation with IC50values of 0.2 μM and 0.25 μM, respectively. ^[1] Terbinafine is highly activ Aspergillus isolates (minimum inhibitory concentration [MIC] 0.01 to 2 mg/mL) with a primary fungicidal action (minimum fungicidal concentration [MFC] 0.02 to 4 mg/mL). ^[2] Terbinafine inhibits dextromethorphan O-demethylation with an apparent Ki ranging from 28 to 44 nM in human hepatic microsomes and averaging 22.4 nM for the heterologously expressed enzymes. ^[3] Terbinafine shows a very strong activity in vitro against Penicillium spp., Paecilomyces spp., Trichoderma spp., Acremonium spp. and Arthrographis spp. with GMs <1 mg/L. ^[4] Terbinafine decreases the levels of phosphorylated extracellular signal-regulated kinase (ERK). Terbinafine might cause a decrease of MEK, which in turn up-regulates p53 through the inhibition of ERK phosphorylation, and finally causes an increase of p21expression and cell-cycle arrest. ^[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：

Genetic screens reveal new targetable vulnerabilities in BAP1-deficient mesothelioma [ Cell Rep Med, 2023, S2666-3791(22)00494-3]	PubMed: 36657447
Antifungal agent Terbinafine restrains tumor growth in preclinical models of hepatocellular carcinoma via AMPK-mTOR axis [ Oncogene, 2021, 10.1038/s41388-021-01934-y]	PubMed: 34247189
Classic and Targeted Anti-Leukaemic Agents Interfere With the Cholesterol Biogenesis Metagene in Acute Myeloid Leukaemia: Therapeutic Implications [ J Cell Mol Med, 2020, 25]	PubMed: 32450611
Drug repositioning as a therapeutic strategy for neurodegenerations associated with OPA1 mutations [ Hum Mol Genet, 2020, ddaa244]	PubMed: 33231680

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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