An MC4R antagonist
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HS-024 (trifluoroacetate salt)

Item No. 41557

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
cyclic (1→9)-disulfide, N-acetyl-L-cysteinyl-L-norleucyl-L-arginyl-L-histidyl-3-(2-naphthalenyl)-D-alanyl-L-tryptophylglycyl-L-cysteinamide, trifluoroacetate salt
Synonyms
  • Ac-Cys-Nle-Arg-His-D-Nal-Arg-Trp-Gly-Cys-NH2
  • cyclic [AcCys3,Nle4,Arg5,D-Nal7,Cys-NH211]α-MSH-(3–11)
Molecular Formula
C58H79N19O10S2 • XCF3COOH
Formula Weight
1266.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mEthanol: Soluble: ≥10 mg/mlPBS (pH 7.2): Soluble: ≥10 mg/ml
SMILES
O=C([C@@H](NC([C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@H](CSSC[C@H](NC(CNC1=O)=O)C(N)=O)NC(C)=O)=O)CCCC)=O)CCCNC(N)=N)=O)CC2=CN=CN2)=O)CC3=CC4=C(C=CC=C4)C=C3)=O)CCCNC(N)=N)N[C@H]1CC5=CNC6=CC=CC=C56.O=C(O)C(F)(F)F
InChi Code
InChI=1S/C58H79N19O10S2.C2HF3O2/c1-3-4-14-40-51(82)72-41(16-9-20-65-57(60)61)53(84)77-45(25-37-27-64-31-69-37)55(86)75-43(23-33-18-19-34-11-5-6-12-35(34)22-33)54(85)73-42(17-10-21-66-58(62)63)52(83)76-44(24-36-26-67-39-15-8-7-13-38(36)39)50(81)68-28-48(79)71-46(49(59)80)29-88-89-30-47(56(87)74-40)70-32(2)78;3-2(4,5)1(6)7/h5-8,11-13,15,18-19,22,26-27,31,40-47,67H,3-4,9-10,14,16-17,20-21,23-25,28-30H2,1-2H3,(H2,59,80)(H,64,69)(H,68,81)(H,70,78)(H,71,79)(H,72,82)(H,73,85)(H,74,87)(H,75,86)(H,76,83)(H,77,84)(H4,60,61,65)(H4,62,63,66);(H,6,7)/t40-,41-,42-,43+,44-,45-,46-,47-;/m0./s1
InChi Key
KFPPOAMKLLTSNH-KMPRNXRMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    500 µg

    $230

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    1 mg

    $437

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    5 mg

    $1,725

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    Product Description

    HS-024 is a cyclic peptide antagonist of melanocortin receptor 4 (MC4R; Ki = 0.29 nM).1 It is selective for MC4R over MC1R, MC3R, and MC5R (Kis = 18.6, 5.45, and 3.29 nM, respectively). HS-024 (100 nM) inhibits cAMP accumulation induced by α-melanocyte-stimulating hormone (α-MSH; Item No. 29923) in COS-1 cells expressing human MC1R, MC3R, MC4R, or MC5R. It increases food intake in rats when administered at doses of 0.3, 1, or 3 nmol/animal. Intrathecal administration of HS-024 (1.5 nmol/animal) inhibits mechanical allodynia at 30 minutes post-injection in a rat model of spinal nerve ligation-induced neuropathic pain.2 It reduces stress-induced reinstatement of nicotine seeking in the foot shock test in rats.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kask, A., Mutulis, F., Muceniece, R., et al. Discovery of a novel superpotent and selective melanocortin-4 receptor antagonist (HS024): Evaluation in vitro and in vivo. Endocrinology 139(12), 5006-5014 (1998).

    2. Bertorelli, R., Fredduzzi, S., Tarozzo, G., et al. Endogenous and exogenous melanocortin antagonists induce anti-allodynic effects in a model of rat neuropathic pain. Behav. Brain Res. 157(1), 55-62 (2005).

    3. Qi, X., Yamada, H., Corrie, L.W., et al. A critical role for the melanocortin 4 receptor in stress-induced relapse to nicotine seeking in rats. Addict. Biol. 20(2), 324-335 (2015).