Formulation: A crystalline solid
Formal Name: 1-[1-(3-methyl-L-histidyl-O-methyl-D-tyrosyl)-4-phenyl-4-piperidinyl]-1-butanone, dihydrochloride
Purity: ≥98%
Formula Markup: C32H41N5O4 • 2HCl
Formula Weight: 632,6
Shelf life (days): 730
CAS Number: 2341796-82-3
Notes: BMS 470539 is an agonist of melanocortin receptor 1 (MC1R).{38259} It induces cAMP accumulation in B16/F10 murine melanoma cells and in CHO cells overexpressing human MC1R (EC50s = 11.6 and 16.8 nM, respectively). It inhibits TNF-α-induced NF-κB activation in vitro in a concentration-dependent manner. In vivo, BMS 470539 inhibits LPS-induced TNF-α production in mice (ED50 = 10 μmol/kg, s.c.). It reduces LPS-induced leukocyte infiltration and paw swelling in mouse models of lung inflammation and delayed-type hypersensitivity, respectively. BMS 470539 decreases retinal damage in a mouse model of streptozotocin-induced diabetic retinopathy.{38260} It also increases striatal dopamine levels and decreases the number of striatal α-synuclein aggregates in a mouse model of Parkinson’s disease when administered at a dose of 20 mg/kg.{62919}
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