A peptide agonist of MC4R
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Setmelanotide (trifluoroacetate salt)

Item No. 35564

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
cyclic (2→8)-disulfide N2-acetyl-L-arginyl-L-cysteinyl-D-alanyl-L-histidyl-D-phenylalanyl-L-arginyl-L-tryptophyl-L-cysteinamide, trifluoroacetate salt
Synonyms
  • BIM-22493
  • N-acetyl-RCAHFRWC-NH2
  • RM-493
Molecular Formula
C49H68N18O9S2 • XCF3COOH
Formula Weight
1117.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Water: soluble
SMILES
O=C([C@@H](NC([C@H](NC([C@@H](NC([C@H](NC([C@H](CSSC[C@H](NC1=O)C(N)=O)NC([C@@H](NC(C)=O)CCCNC(N)=N)=O)=O)C)=O)CC2=CN=CN2)=O)CC3=CC=CC=C3)=O)CCCNC(N)=N)N[C@H]1CC4=CNC5=CC=CC=C45.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C49H68N18O9S2.C2HF3O2/c1-26-41(70)63-37(20-30-22-55-25-59-30)46(75)64-35(18-28-10-4-3-5-11-28)44(73)62-34(15-9-17-57-49(53)54)43(72)65-36(19-29-21-58-32-13-7-6-12-31(29)32)45(74)66-38(40(50)69)23-77-78-24-39(47(76)60-26)67-42(71)33(61-27(2)68)14-8-16-56-48(51)52;3-2(4,5)1(6)7/h3-7,10-13,21-22,25-26,33-39,58H,8-9,14-20,23-24H2,1-2H3,(H2,50,69)(H,55,59)(H,60,76)(H,61,68)(H,62,73)(H,63,70)(H,64,75)(H,65,72)(H,66,74)(H,67,71)(H4,51,52,56)(H4,53,54,57);(H,6,7)/t26-,33+,34+,35-,36+,37+,38+,39+;/m1./s1
InChi Key
WLNKAQFYDVNRDO-GZRAWZNHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $62

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    10 mg

    $117

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    25 mg

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    50 mg

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    Setmelanotide is a cyclic peptide agonist of melanocortin receptor 4 (MC4R).1 It increases cAMP production in CHO-K1 cells expressing MC4R, MC1R, MC3R, and MC5R (EC50s = 0.27, 5.8, 5.3, and 1,600 nM, respectively, for the human receptors) but not in cells expressing MC2R (EC50 = >10 µM). Setmelanotide (6.4 µmol/animal) inhibits food intake in MC3R, but not MC4R, knockout mice. It also reduces food intake and hepatosteatosis, induces weight loss, and decreases serum insulin, glucose, and leptin levels in a mouse model of diet-induced obesity when administered at a dose of 300 nmol/kg per day. Formulations containing setmelanotide have been used in chronic weight management due to proopiomelanocortin (POMC), proprotein convertase subtilisin/kexin type 1 (PCSK1), or leptin receptor deficiency.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kumar, K.G., Sutton, G.M., Dong, J.Z., et al. Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice. Peptides 30(10), 1892-1900 (2009).