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- BMS 470539 (hydrochloride)
BMS 470539 (hydrochloride)
BMS 470539 (hydrochloride)是一种高效的选择性黑皮质素1受体（MC-1R）激动剂，在cAMP积累测定中，对人源和鼠源MC1R的EC50值分别为16.8和11.6nM。
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包装价格促销价数量
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1mg￥857.00600.00- +
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5mg￥1571.001100.00- +
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10mg￥2143.001500.00- +
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25mg￥5714.004000.00- +
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50mg￥8285.005800.00- +
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200mg￥0.000.00- +
- 货号: ajcx18146
- CAS: 2341796-82-3
- 别名: BMS-470539 dihydrochloride
- 分子式: C32H41N5O4.2HCl
- 分子量: 632.6
- 纯度: >98%
- 溶解度: DMF: 25 mg/ml, DMSO: 10 mg/ml, Ethanol: 20 mg/ml
- 储存: Store at -20°C
- 库存: 现货
Background
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.
