TCMCB07 (trifluoroacetate salt)

TCMCB07 is a peptide antagonist of melanocortin receptor 1 (MC1R), MC3R, MC4R, and MC5R (IC50s = 19.5, 0.59, 13.58, and 8.07 nM, respectively, for the human receptors). It is also an antagonist of dog MC1R, MC3R, MC4R, and MC5R receptors (IC50s = 53.64, 1.46, 7.14, and 11.22 nM, respectively). TCMCB07 (10 mg/kg) increases food intake and body weight in a rat model of LPS-induced cachexia. It increases body weight, muscle mass, blood levels of urea nitrogen, and mean heart rate in dogs with cachexia when administered at a dose of 0.75 mg/kg per day.Formal Name: N-acetyl-L-norleucyl-L-alpha-aspartyl-L-prolyl-3-(2-naphthalenyl)-D-alanyl-L-arginyl-L-tryptophyl-L-lysyl-D-valyl-D-prolinamide, (2->7)-lactam, trifluoroacetate salt. Synonyms: Ac-Nle-Asp-Pro-D-2Nal-Arg-Trp-Lys-D-Val-D-Pro-NH2, Mifomelatide. Molecular Formula: C63H87N15O11 . XCF3COOH. Formula Weight: 1230.5. Purity: >98%. Formulation: (Request formulation change), A solid. Peptide Sequence: Ac-XDPzRWKvp-NH2 (X = norisoleucine, z = 3-(2-naphalyl)-D-alanine). Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: Soluble: >10 mg/ml. SMILES: O=C([C@@H](NC([C@H](NC([C@@]1([H])N(CCC1)C([C@H](CC(NCCCC[C@H](NC2=O)C(N[C@H](C(C)C)C(N3[C@H](CCC3)C(N)=O)=O)=O)=O)NC([C@H](CCCC)NC(C)=O)=O)=O)=O)CC4=CC5=C(C=CC=C5)C=C4)=O)CCCNC(N)=N)N[C@H]2CC6=CNC7=CC=CC=C67.OC(C(F)(F)F)=O. InChi Code: InChI=1S/C63H87N15O11.C2HF3O2/c1-5-6-19-44(70-37(4)79)55(82)75-49-34-52(80)67-27-12-11-21-45(57(84)76-53(36(2)3)62(89)77-29-14-23-50(77)54(64)81)71-59(86)48(33-41-35-69-43-20-10-9-18-42(41)43)73-56(83)46(22-13-28-68-63(65)66)72-58(85)47(74-60(87)51-24-15-30-78(51)61(49)88)32-38-25-26-39-16-7-8-17-40(39)31-38,3-2(4,5)1(6)7/h7-10,16-18,20,25-26,31,35-36,44-51,53,69H,5-6,11-15,19,21-24,27-30,32-34H2,1-4H3,(H2,64,81)(H,67,80)(H,70,79)(H,71,86)(H,72,85)(H,73,83)(H,74,87)(H,75,82)(H,76,84)(H4,65,66,68),(H,6,7)/t44-,45-,46-,47+,48-,49-,50+,51-,53+,/m0./s1. InChi Key: MSNXMNKRZUHQHJ-PNSCJSEPSA-N.