ICI-118551(ICI 118,551)|cas 72795-01-8|DC Chemicals

Cas No.:	72795-01-8
Chemical Name:	ICI 118,551 hydrochloride
Synonyms:	2-Butanol,1-[(2,3-dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-,hydrochloride, (2R,3R)-rel- (9CI);ICI 118551 Hydrochloride;(2R,3S)-1-[(7-methyl-2,3-dihydro-1H-inden-4-yl)oxy]-3-(propan-2-ylamino)butan-2-ol,hydrochloride;2-Butanol,1-[(2,3-dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-,hydrochloride,...;ICI 118551 (hydrochloride);ICI-118551 hydrochloride;(2R,3R)-rel-3-isopropylamino-1-(7-methylindan-4-yloxy)-butan-2-ol hydrochloride;(2R,3R)-rel-1-[(2,3-Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol hydrochloride (1:1);ICI 118,551 hydrochloride;ICI 111581;(2R,3S)-1-[(7-methyl-2,3-dihydro-1H-inden-4-yl)oxy]-3-(propan-2-ylamino)butan-2-ol;hydrochloride;MLS002153415;SMR001230791;ICI 118,551 hydrochloride, >=98% (HPLC), powder;(2R,3S)-rel-1-[(2,3-Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol Hydrochloride;(R,S)-()-1-[(2,3-Dihydro-7-methyl
SMILES:	Cl.CC(C)N[C@@H](C)[C@@H](O)COC1=C2C(CCC2)=C(C)C=C1
Formula:	C₁₇H₂₈ClNO₂
M.Wt:	313.8627
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

ICI 118551 Hcl is a highly selective β2 adrenergic receptor antagonist (Ki values are 1.2, 120 and 257 nM at β2, β1 and β3 receptors respectively). IC50 Value: 1.2 nM (Ki) Target: beta 2 adrenoceptor in vitro: ICI-118551 inhibited cAMP accumulation by 50% (IC50 = 1.5 microM and 1.7 microM, respectively . Pharmacological experiments proved that the right shift of the norepinephrine dose-response curve by ICI 118551 was mediated via a beta(2)-adrenoceptor/G(i/o) protein-dependent pathway enhancing NO production in the endothelium; these results were corroborated in beta-adrenoceptor and endothelial NO synthase knockout mice where ICI 118551 had no effect. ICI 118551 increased vascular lumen diameter in lung sections and reduced pulmonary arterial pressure under normoxia and under hypoxia in the isolated perfused lung model . Transgenic mice with high beta(2)AR number and increased G(i) levels had normal basal contractility but showed a similar negative inotropic response to ICI 118,551. Overexpression of human beta(2)AR in rabbit myocytes using adenovirus potentiated the negative inotropic effect of ICI 118,551. In human, rabbit, and mouse myocytes, the negative inotropic effects were blocked after treatment of cells with pertussis toxin to inactivate G(i), and overexpression of G(i)alpha(2) induced the effect de novo in normal rat myocytes . in vivo: After 1 week of treatment ICI 118,551 had no effect on the beta 1-receptor mediated shortening of electromechanical systole (QS2I), the rise in systolic pressure and rise in renin, whereas these responses were blocked by a dose factor of eight after propranolol. ICI 118,551 and propranolol equally blocked the beta 2-receptor mediated fall in diastolic pressure and the rise in noradrenaline . For the detailed information about the solubility of ICI-118551 in water, the solubility of ICI-118551 in DMSO, the solubility of ICI-118551 in PBS buffer, the animal experiment（test） of ICI-118551,the in vivo,in vitro and clinical trial test of ICI-118551,the cell experiment（test） of ICI-118551,the IC50, EC50 and Affinity of ICI-118551, please contact DC Chemicals.

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2018-0101
2018-0101

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