| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| K408590-1ml |
1ml |
现货  |
|
| 英文别名 | 1-(4-(4-(((2R,4S)-2-((1H-imidazol-1-yl)methyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl)methoxy)phenyl)piperazin-1-yl)ethanone |
|---|---|
| 规格或纯度 | Moligand™, 2mM in DMSO |
| 英文名称 | Ketoconazole (R 41400) |
| 生化机理 | 酮康唑（R 41400）可抑制环孢素氧化酶和睾酮 6 β-羟化酶，其 IC50 分别为 0.19 mM 和 0.22 mM。酮康唑是一种雄激素生物合成抑制剂。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | CYP3A4 抑制剂；K v1.8 通道阻断剂 |
| 产品介绍 |
Information Ketoconazole (R 41400) inhibitscyclosporine oxidaseandtestosterone 6 beta-hydroxylasewithIC50of 0.19 mM and 0.22 mM, respectively. Ketoconazole is anandrogenbiosynthesis inhibitor. Ketoconazole interacts with androgen receptors in a competitive fashion in intact human foreskin fibroblasts. Ketoconazole competes for [3H]dexamethasone binding to fibroblast glucocorticoid receptors with IC50 of 0.3 mM. Ketoconazole reduces cell proliferation and [3H]thymidine incorporation with IC50 of 2.5 mM in the serum independent HT29-S-B6 colon cell clone. Ketoconazole inhibits the incorporation of [3H]thymidine with IC50 of 2 μM and 13 μM in the Evsa-T cell line and MDA-MB-231 cell line, respectively. Ketoconazole induces a decrease of the number of cells in S phase and a corresponding increase of the percentage of cells in Go-G1 in HT29-S-B6 cells. Ketoconazole is susceptable to several Malassezia species with minimum inhibitory concentrations (MICs) of 0.03 µg/mL. In vivo Ketoconazole (25 mg/kg, i.p.) significantly decreases plasma corticosterone and reduces low dose cocaine self-administration without affecting food-reinforced responding in rats. Ketoconazole raises the AUC of orally administered digoxin from 63 mg x h/L to 411 mg x h/L in rats. Ketoconazole raises the AUC of intravenously administered digoxin from 93 mg × h/L to 486 mg × h/L in rats. Ketoconazole increases digoxin bioavailability from 0.68 to 0.84 in rats, while mean absorption time is reduced from 1.1 hours to 0.3 hour. cell lines： Concentrations：25 μM Incubation Time：72 hours Powder Purity:≥99% |
| IC50 | Cyclosporine oxidase, IC50: 0.19 mM |
|---|---|
| ALogP | 3.61 |
| hba_count | 5 |
| Rotatable Bond | 7 |
| Canonical SMILES | CC(=O)N1CCN(CC1)C2=CC=C(OCC3COC(C[N]4C=CN=C4)(O3)C5=CC=C(Cl)C=C5Cl)C=C2 |
|---|---|
| 分子量 | 531.43 |
| Reaxy-Rn | 634785 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=634785&ln= |
| 溶解性 | Solubility (25°C) In vitro DMSO: 56 mg/mL (197.02 mM); |
|---|---|
| DMSO(mg / mL) Max Solubility | 5 |
| DMSO(mM) Max Solubility | 9.41 |
| Water(mg / mL) Max Solubility | <1 |
| Reaxy-Rn | 634785 |
|---|---|
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=634785&ln= |
| Concentration(Compounding value) | 1.96-2.04(mmol/L) |
|---|---|
| Appearance(K408590) | Colorless Transparent Liquid |
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