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Formula | C21H25N.HCl |
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Molecular Weight | 327.89 | CAS No. | 78628-80-5 | |
Solubility (25°C)* | In vitro | 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Terbinafine HCl (KWD 201,KWD 2019,TDT 067 hydrochloride) inhibits ergosterol synthesis by inhibiting squalene epoxidase, used as an antifungal drug. | |
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Targets |
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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] |
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 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.