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Azepexole (B-HT 933) dihydrochloride 是一种有效的选择性α 2肾上腺素受体激动剂,对 α2A-、α2B- 和 α2C- 肾上腺素受体亚型的 pKi 分别为 8.3、7.6 和 7.5。Azepexole dihydrochloride 引起浓度依赖性的蠕动收缩抑制,IC50值为 78.72 nM。
Azepexole (B-HT 933) dihydrochloride 是一种有效的选择性α 2肾上腺素受体激动剂,对 α2A-、α2B- 和 α2C- 肾上腺素受体亚型的 pKi 分别为 8.3、7.6 和 7.5。Azepexole dihydrochloride 引起浓度依赖性的蠕动收缩抑制,IC50值为 78.72 nM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 560 | 35日内发货 | |
5 mg | ¥ 2,430 | 35日内发货 | |
10 mg | ¥ 3,480 | 35日内发货 |
产品描述 | Azepexole dihydrochloride (B-HT 933), a potent and selective alpha 2-adrenoceptor agonist, exhibits affinity for α2A-, α2B-, and α2C-adrenoceptor subtypes with pKis of 8.3, 7.6, and 7.5, respectively [1]. It elicits a concentration-dependent inhibition of peristaltic contractions, evidenced by an IC50 of 78.72 nM. |
体外活性 | In normoglycemic rats, the sympathetically-induced vasopressor responses are dose-dependently inhibited by 1 and 3 μg/kg.min (i.v.) Azepexole dihydrochloride, with 10 and 30 μg/kg.min Azepexole dihydrochloride do not produce further inhibition. In diabetic rats, the electrically-induced vasopressor responses are: (i) unchanged by 1 and 3 μg/kg.min Azepexole dihydrochloride; (ii) significantly inhibited at all frequencies of stimulation by 10 μg/kg.min B-HT 933 dihydrochloride; and (iii) similarly inhibited (i.e. supramaximal inhibition) by 30 μg/kg.min Azepexole dihydrochloride [1]. |
分子量 | 254.16 |
分子式 | C9H17Cl2N3O |
CAS No. | 36067-72-8 |
密度 | 1.126g/cm3 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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