Ac-(D-Arg)-CEH-(D-Phe)-RWC-NH2 (trifluoroacetate salt)

Ac-(D-Arg)-CEH-(D-Phe)-RWC-NH2 is a cyclic peptide and an agonist of melanocortin receptor 4 (MC4R). It induces cAMP release in HEK293 cells expressing human MC4R (EC50 = 0.28 nM). Ac-(D-Arg)-CEH-(D-Phe)-RWC-NH2 is selective for MC4R over MC1R, MC3R, and MC5R (Kis = 0.55, 16.78, 56.79, and >500 nM, respectively). It decreases food intake and body weight in a rat model of diet-induced obesity when administered at doses of 0.075 or 0.299 µmol/kg.Formal Name: 3-((4R,7S,10S,13R,16S,19S,22R)-16-((1H-imidazol-5-yl)methyl)-7-((1H-indol-3-yl)methyl)-22-((R)-2-acetamido-5-guanidinopentanamido)-13-benzyl-4-carbamoyl-10-(3-guanidinopropyl)-6,9,12,15,18,21-hexaoxo-1,2-dithia-5,8,11,14,17,20-hexaazacyclotricosan-19-yl)propanoic acid, trifluorocetate salt. Synonyms: Ac-dR[CEHdFRWC]-NH2. Molecular Formula: C51H70N18O11S2 . XCF3COOH. Formula Weight: 1175.4. Purity: >98%. Formulation: (Request formulation change), A solid. Peptide Sequence: Ac-rCEHfRWC-NH2. Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: Soluble: >10 mg/ml, PBS (pH 7.2): Soluble: >10 mg/ml. SMILES: O=C(N[C@@H](CSSC[C@@H](C(N[C@H](C(N[C@H](C(N[C@@H](C(N[C@H]1CCCNC(N)=N)=O)CC2=CC=CC=C2)=O)CC3=CN=CN3)=O)CCC(O)=O)=O)NC([C@@H](CCCNC(N)=N)NC(C)=O)=O)C(N)=O)[C@H](CC4=CNC5=CC=CC=C54)NC1=O.O=C(O)C(F)(F)F. InChi Code: InChI=1S/C51H70N18O11S2.C2HF3O2/c1-27(70)62-33(13-7-17-58-50(53)54)43(74)69-40-25-82-81-24-39(42(52)73)68-47(78)37(20-29-22-60-32-12-6-5-11-31(29)32)66-44(75)34(14-8-18-59-51(55)56)63-46(77)36(19-28-9-3-2-4-10-28)65-48(79)38(21-30-23-57-26-61-30)67-45(76)35(64-49(40)80)15-16-41(71)72,3-2(4,5)1(6)7/h2-6,9-12,22-23,26,33-40,60H,7-8,13-21,24-25H2,1H3,(H2,52,73)(H,57,61)(H,62,70)(H,63,77)(H,64,80)(H,65,79)(H,66,75)(H,67,76)(H,68,78)(H,69,74)(H,71,72)(H4,53,54,58)(H4,55,56,59),(H,6,7)/t33-,34+,35+,36-,37+,38+,39+,40+,/m1./s1. InChi Key: UTZVAVDKLIBFTA-MBRWJLABSA-N.