Home>>BMS 470539 (hydrochloride)

BMS 470539 (hydrochloride)

目录号 : GC42954

An MC1R agonist

BMS 470539 (hydrochloride) Chemical Structure

Cas No.:2341796-82-3

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5mg
¥1,782.00
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10mg
¥2,772.00
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25mg
¥6,237.00
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50mg
¥11,385.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

BMS 470539 is an agonist of melanocortin receptor 1 (MC1R) with EC50 values of 16.8 and 11.6 nM for human and murine MC1R, respectively, in a cAMP accumulation assay. [1] It inhibits TNF-α-induced NF-κB activation in vitro in a dose-dependent manner. In vivo, subcutaneous administration of BMS 470539 inhibits LPS-induced TNF-α production in wild-type mice (ED50 = 10 μmol/kg). It reduces LPS-induced leukocyte infiltration and paw swelling in mouse models of lung inflammation and delayed-type hypersensitivity, respectively. BMS 470539 administration also decreases retinal damage in a mouse model of streptozotocin-induced diabetic retinopathy. [2]

Reference:
[1]. Kang, L., McIntyre, K.W., Gillooly, K.M., et al. A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice. J. Leukoc. Biol. 80(4), 897-904 (2006).
[2]. Rossi, S., Maisto, R., Gesualdo, C., et al. Activation of melanocortin receptors MC1 and MC5 attenuates retinal damage in experimental diabetic retinopathy. Mediators Inflamm.

Chemical Properties

Cas No. 2341796-82-3 SDF
化学名 1-[1-(3-methyl-L-histidyl-O-methyl-D-tyrosyl)-4-phenyl-4-piperidinyl]-1-butanone, dihydrochloride
Canonical SMILES O=C([C@@H](CC1=CC=C(OC)C=C1)NC([C@@H](N)CC2=CN=CN2C)=O)N3CCC(C4=CC=CC=C4)(C(CCC)=O)CC3.Cl.Cl
分子式 C32H41N5O4•2HCl 分子量 632.6
溶解度 DMF: 25 mg/ml, DMSO: 10 mg/ml, Ethanol: 20 mg/ml 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 1.5808 mL 7.9039 mL 15.8078 mL
5 mM 0.3162 mL 1.5808 mL 3.1616 mL
10 mM 0.1581 mL 0.7904 mL 1.5808 mL
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