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Tocris/ICI 118,551 hydrochloride/0821/50/50 mg

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货号: 0821/50

品牌: Tocris

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Description: Very selective β₂ antagonist/inverse agonist

Chemical Name: (±)-erythro-(S*,S*)-1-[2,3-(Dihydro-7-methyl-1H-inden-4-yl)oxy]-3-[(1-methylethyl)amino]-2-butanol hydrochloride

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Very selective β₂ adrenergic antagonist/inverse agonist (K_i values are 1.2, 120 and 257 nM for β₂, β₁ and β₃ receptors respectively). Active in vivo. Also available as part of the β-Adrenoceptor Antagonist Tocriset™.

Licensing Information

Sold with the permission of AstraZeneca UK Ltd.

Technical Data

M. Wt	313.87
Formula	C₁₇H₂₇NO₂.HCl
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	72795-01-8
PubChem ID	46704341
InChI Key	KBXMBGWSOLBOQM-MELYUZJYSA-N
Smiles	CC1=C(CCC2)C2=C(OC[C@@H](O)[C@H](C)NC(C)C)C=C1.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	3.14	10
	water	3.14	10

Preparing Stock Solutions

The following data is based on the product molecular weight 313.87. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	3.19 mL	15.93 mL	31.86 mL
5 mM	0.64 mL	3.19 mL	6.37 mL
10 mM	0.32 mL	1.59 mL	3.19 mL
50 mM	0.06 mL	0.32 mL	0.64 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Bilski et al (1983) The pharmacology of a β2-selective adrenoceptor antagonist (ICI-118,551). J.Cardiovasc.Pharmacol. 5 430 PMID: 6191142

Cook et al (1993) β-Adrenoceptor subtypes and the opening of plasmalemmal K⁺-channels in trachealis muscle: electrophysiological and mechanical studies in guinea-pig tissue. Br.J.Pharmacol. 109 1140 PMID: 8104643

Strosberg and Pietri-Rouxel (1996) Function and regulation of the β₃-adrenoceptor. TiPS 17 373 PMID: 8979772

Ten Berge et al (1995) β₂-but not β₃-adrenoceptors mediate prejunctional inhibition of non-adrenergic non cholinergic contraction of guinea pig main bronchi. Eur.J.Pharmacol. 275 199 PMID: 7796855

Bond et al (1995) Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the β₂-adrenoceptor. Nature 374 272 PMID: 7885448

Keywords: ICI 118,551 hydrochloride, supplier, selective, β2-adrenoceptors, α2-adrenoceptor, beta2-adrenoceptors, b2-adrenoceptors, b2-adrenergic, β2-adrenergic, α2-adrenergic, beta2-adrenergic, antagonists, Receptors, ICI118551, hydrochloride, AstraZeneca, inverse, agonist, agonism, Adrenergic, Beta-2, Receptors, Adrenergic, Beta-2, Receptors, Tocris Bioscience

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