HS014 - CAS# 207678-81-7

HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats.

Product information

CAS Number: 207678-81-7

Molecular Weight: 1563.76

Formula: C71H94N20O17S2

Chemical Name: 3-[[2-[[1-[1-[25-acetamido-13-(3-carbamimidamidopropyl)-22-(2-carboxyethyl)-19-(1H-imidazol-4-ylmethyl)-10-(1H-indol-3-ylmethyl)-16-(naphthalen-2-ylmethyl)-6, 9, 12, 15, 18, 21, 24-heptaoxo-1, 2-dithia-5, 8, 11, 14, 17, 20, 23-heptazacyclohexacosane-4-carbonyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-6-aminohexanoyl]amino]-4-amino-4-oxobutanoic acid

Smiles: CC(=O)NC1CSSCC(NC(=O)CNC(=O)C(CC2=CNC3=CC=CC=C23)NC(=O)C(CCCNC(N)=N)NC(=O)C(CC2=CC3=CC=CC=C3C=C2)NC(=O)C(CC2=CNC=N2)NC(=O)C(CCC(O)=O)NC1=O)C(=O)N1CCCC1C(=O)N1CCCC1C(=O)NC(CCCCN)C(=O)NC(CC(O)=O)C(N)=O

InChiKey: BRGDPINZISNYJL-UHFFFAOYSA-N

InChi: InChI=1S/C71H94N20O17S2/c1-38(92)81-53-35-109-110-36-54(69(107)91-26-10-18-56(91)70(108)90-25-9-17-55(90)68(106)85-46(15-6-7-23-72)62(100)86-49(60(73)98)31-59(96)97)82-57(93)34-79-61(99)51(29-42-32-78-45-14-5-4-13-44(42)45)88-63(101)47(16-8-24-77-71(74)75)83-65(103)50(28-39-19-20-40-11-2-3-12-41(40)27-39)87-66(104)52(30-43-33-76-37-80-43)89-64(102)48(84-67(53)105)21-22-58(94)95/h2-5,11-14,19-20,27,32-33,37,46-56,78H,6-10,15-18,21-26,28-31,34-36,72H2,1H3,(H2,73,98)(H,76,80)(H,79,99)(H,81,92)(H,82,93)(H,83,103)(H,84,105)(H,85,106)(H,86,100)(H,87,104)(H,88,101)(H,89,102)(H,94,95)(H,96,97)(H4,74,75,77)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vivo:

The dose-effect curve of morphine for locomotor activity was shifted downwards in C57Bl/6 mice pretreated with HS014 and in A(y) mice. The dose-effect curve of morphine for antinociception is shifted two- and threefold to the left in C57Bl/6 mice pretreated with HS014 and in A(y) mice, respectively. Pretreatment with HS014 blocks the effect of IL-1beta on food intake and respiratory exchange ratio (RER) at later time points (beyond 8 h post injection), as well as the hypoactivity and increases metabolic rate.

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