Astemizole
Astemizole 是一种强效的抗组胺药（H1 受体拮抗剂，IC50 = 4 nM），显示出对多巴胺、5-HT 和毒蕈碱型乙酰胆碱受体的选择性。该化合物已显示出强大的 hERG K+ 通道阻断活性（IC50 = 0.9 nM），在体外对多药耐药性疟疾菌株具有抗疟疾活性（IC50 = 227 - 734 nM），并已被用作伴侣分子来纠正某些突变形式的 hERG 通道的折叠缺陷并恢复蛋白质功能。
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生物活性
| Discription | Astemizole is a potent antihistamine (H1-receptor antagonist, IC50 = 4 nM) that displays selectivity over dopamine, 5-HT, and muscarinic acetylcholine receptors. This compound has shown potent hERG K+ channel blocking activity (IC50 = 0.9 nM), antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM), and has been used as a chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels. | |||||
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产品信息
| 目录号 | A13899 |
|---|---|
| 分子式 | C28H31FN4O |
| 分子量 | 458.57 |
| CAS号 | 68844-77-9 |
| SMILES | COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F |
| 其他名称 | Astemisan, Hismanal, Histamen, Paralergim |
| 储存条件 | Store lyophilized at -20ºC, keep desiccated. |
溶解性数据
| In vitro | DMSO | 91 mg/mL (198.44 mM) | |
| Water | Insoluble | ||
| Ethanol | 9 mg/mL | ||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq 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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Preparing Stock Solutions
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 21.81 mL | 109.03 mL | 218.07 mL |
| 0.5 mM | 4.36 mL | 21.81 mL | 43.61 mL |
| 1 mM | 2.18 mL | 10.9 mL | 21.81 mL |
| 5 mM | 0.44 mL | 2.18 mL | 4.36 mL |
Useful Calculator
Calculate the dilution required to prepare a stock solution. This equation is commonly abbreviated as: C1V1 = C2V2
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| 购买 68844-77-9 | 68844-77-9 供应商 | 68844-77-9 花费 | 68844-77-9 生产商 | 订购 68844-77-9 | 68844-77-9 代理商