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.
货号:ajcx18146
CAS:N/A
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
纯度：98%
存储：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]

参考文献:
[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.