BMS-470539|BMS 470539;BMS470539

Cas No.:	457893-92-4
Chemical Name:	1-[1-(3-Methyl-L-histidyl-O-methyl-D-tyrosyl)-4-phenyl-4-piperidinyl]-1-butanone dihydrochloride
Synonyms:	BMS 470539;BMS470539
SMILES:	C(C(C1=CC=CC=C1)1CCN(C(=O)[C@H](CC2C=CC(OC)=C(C)C=2)NC(=O)[C@@H](CC2N=CNC=2)N)CC1)(=O)CCC.[H]Cl.[H]Cl
Formula:	C₃₂H₄₁N₅O₄^.₂HCl
M.Wt:	632.62
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

A potent, selective, full agonist of human and murine MC1R with EC50 of 16.8 and 11.6 nM, respectively; dose-dependently inhibits TNFα-induced activation of a NF-kappaB transcriptional reporter in human melanoma cells; inhibits LPS-induced TNFα production in BALB/c mice (EC50=10 uM/kg); inhibits leucocyte trafficking in the inflamed vasculature.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101

Cat. No.	Product name	Field of application
DC47573	α-MSH free acid	α-MSH (free acid) is a MC3R and MC4R agonist with an EC50 of 0.16±0.09 nM and 5.6±6.8 nM, respectively. α-MSH (free acid) activates cAMP generation at MC3R and MC4R.
DC46845	MCL0020	MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake.
DC46586	MSG606 TFA	MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses morphine-induced hyperalgesia in female mice, with no effect in male mice.
DC46548	JKC363 TFA	JKC363 TFA, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC363 TFA blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect.
DC46340	CCZ01048	CCZ01048, a α-melanocyte-stimulating hormone (α-MSH) analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma.
DC46339	CCZ01048 TFA	CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma.
DC44951	γ-1-Melanocyte Stimulating Hormone (MSH), amide	γ-1-Melanocyte Stimulating Hormone (MSH), amide is a 11-amino acid peptide. γ-1-Melanocyte Stimulating Hormone (MSH) regulates sodium (Na+) balance and blood pressure through activation of the melanocortin receptor 3 (MC3-R).
DC44950	α-Melanocyte-Stimulating Hormone (MSH), amide TFA	α-Melanocyte-Stimulating Hormone (MSH), amide TFA is an endogenous neuropeptide, with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC), acts as an endogenous melanocortin receptor 4 (MC4R) agonist.
DC44949	JKC363	JKC363, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC-363 blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect.
DC44948	MSG606	MSG606 is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 exhibits binding affinity for A375 melanoma cells in vitro. MSG606 reverses morphine-induced hyperalgesia in female mice, with no effect in male mice.