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ICI 118,551 hydrochloride (ICI 118551 hydrochloride) 是高度选择性的β2 adrenergic receptor 拮抗剂,能够结合 β2 肾上腺素能受体(Ki=0.7 nM)、β1 肾上腺素能受体 (Ki=49.5 nM) 和 β3 肾上腺素能受体 (Ki=611 nM)。
ICI 118,551 hydrochloride (ICI 118551 hydrochloride) 是高度选择性的β2 adrenergic receptor 拮抗剂,能够结合 β2 肾上腺素能受体(Ki=0.7 nM)、β1 肾上腺素能受体 (Ki=49.5 nM) 和 β3 肾上腺素能受体 (Ki=611 nM)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 173 | 现货 | |
5 mg | ¥ 383 | 现货 | |
10 mg | ¥ 699 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 677 | 现货 |
产品描述 | ICI 118,551 hydrochloride (ICI 118551 hydrochloride) is a highly selective β2 adrenergic receptor antagonist (Kis: 0.7, 49.5, and 611 nM for β2, β1, and β3 receptors). |
靶点活性 | β3-adrenoceptor:611 nM (ki), β2-adrenoceptor:ki:0.7nM , β1-adrenoceptor:49.5 nM (ki) |
体外活性 | ICI 118551 (10 μM) induces a prominent vasorelaxation of norepinephrine (NE)-precontracted PA but not AO [2]. ICI 118551 inhibits cAMP accumulation in IMCD cells (IC50: 1.7 μM) [1]. In the failing human heart, ICI 118551 has significant effects on beat duration, with time-to-peak contraction and time-to-90% relaxation reduced compared with basal contraction. Negative Inotropic Effect of ICI 118551 Is Not cAMP-Related. Overexpression of β2AR in rabbit myocytes enhances the negative inotropic effects of ICI 118551 [3]. |
体内活性 | ICI 118551 (0.2 mg/kg) injected into the jugular vein of the mice, strongly reduces systolic pressure in the pulmonary circuit but not systemic arterial pressure in vivo[2]. |
别名 | ICI 118551 hydrochloride |
分子量 | 313.86 |
分子式 | C17H28ClNO2 |
CAS No. | 72795-01-8 |
Smiles | Cl.CC(C)N[C@@H](C)[C@@H](O)COc1ccc(C)c2CCCc12 |
密度 | no data available |
存储 | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 20 mg/mL (63.72 mM), Sonication is recommended. H2O: 11 mg/mL (35.05 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
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