An MC1R agonist and MC4R antagonist
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SHU9119 (trifluoroacetate salt)

Item No. 24152

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-acetyl-L-norleucyl-L-α-aspartyl-L-histidyl-3-(2-naphthalenyl)-D-alanyl-L-arginyl-L-tryptophyl-L-lysinamide, (2→7)-lactam, trifluoroacetate salt
CAS Number
168482-23-3
Molecular Formula
C54H71N15O9 • XCF3COOH
Formula Weight
1074.2
Purity
≥95%
Formulation
A lyophilized powder
Solubility(Learn about Variance in Solubility)
Water: 1 mg/ml
SMILES
O=C([C@@H](NC([C@H](CCCC)NC(C)=O)=O)C1)N[C@@H](CC2=CN=CN2)C(N[C@H](CC3=CC=C(C=CC=C4)C4=C3)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC5=CNC6=C5C=CC=C6)C(N[C@H](C(N)=O)CCCCNC1=O)=O)=O)=O)=O.FC(F)(C(O)=O)F
InChi Code
InChI=1S/C54H71N15O9.C2HF3O2/c1-3-4-15-40(63-31(2)70)48(73)69-45-27-46(71)59-21-10-9-17-39(47(55)72)64-51(76)43(25-35-28-61-38-16-8-7-14-37(35)38)67-49(74)41(18-11-22-60-54(56)57)65-50(75)42(24-32-19-20-33-12-5-6-13-34(33)23-32)66-52(77)44(68-53(45)78)26-36-29-58-30-62-36;3-2(4,5)1(6)7/h5-8,12-14,16,19-20,23,28-30,39-45,61H,3-4,9-11,15,17-18,21-22,24-27H2,1-2H3,(H2,55,72)(H,58,62)(H,59,71)(H,63,70)(H,64,76)(H,65,75)(H,66,77)(H,67,74)(H,68,78)(H,69,73)(H4,56,57,60);(H,6,7)/t39-,40-,41-,42+,43-,44-,45-;/m0./s1
InChi Key
UIYQACCNXSQAGQ-YHJYRULISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    1 mg

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    SHU9119 is an agonist of melanocortin receptor 1 (MC1R) and antagonist of MC4R (IC50s = 1.2 and 2.9 nM, respectively, for displacement of melanocortin).1 It induces cAMP formation in HEK293 cells expressing human MC1R (EC50 = 1.11 nM), but inhibits cAMP formation in cells expressing human MC4R.1 In rats, SHU9119 (24 nmol, i.c.v. per day for seven days) increases food intake, body weight, fat mass, and lean mass, with concomitant increases in blood glucose, insulin, and leptin levels via disrupted melanocortin signaling.2 Similarly, mice treated with SHU9119 (5 nmol/day, i.c.v.) exhibit food intake-independent increases in body weight and fat mass consequent to MC4R inhibition and subsequent brown adipose tissue dysfunction.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yang, Y., Chen, M., Lai, Y., et al. Molecular determinants of human melanocortin-4 receptor responsible for antagonist SHU9119 selective activity. The Journal of Biological Chemisty 277(23), 20328-20335 (2002).

    2. Nogueiras, R., Wiedmer, P., Perez-Tilve, D., et al. The central melanocortin system directly controls peripheral lipid metabolism. J. Clin. Invest. 117(11), 3475-3488 (2007).

    3. Kooijman, S., Boon, M.R., Parlevliet, E.T., et al. Inhibition of the central melanocortin system decreases brown adipose tissue activity. J. Lipid Res. 55(10), 2022-2032 (2014).