ICI 118,551 hydrochloride

产品编号 T11607Cas号 72795-01-8

别名 ICI 118551 hydrochloride

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

产品编号 T11607别名 ICI 118551 hydrochlorideCas号 72795-01-8

规格	价格	库存
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

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产品介绍

生物活性

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	β1-adrenoceptor:49.5 nM (ki), β2-adrenoceptor:ki:0.7nM , β3-adrenoceptor:611 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

化学信息

分子量	313.86
分子式	C₁₇H₂₈ClNO₂
CAS No.	72795-01-8

储存&溶解度

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.

溶液配制表

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	3.1861 mL	15.9307 mL	31.8613 mL	159.3067 mL
5 mM	0.6372 mL	3.1861 mL	6.3723 mL	31.8613 mL
10 mM	0.3186 mL	1.5931 mL	3.1861 mL	15.9307 mL
20 mM	0.1593 mL	0.7965 mL	1.5931 mL	7.9653 mL