A growth hormone secretagogue and GHS-R1a agonist
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Macimorelin (acetate)

Item No. 41886

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-methylalanyl-N-[(1R)-1-(formylamino)-2-(1H-indol-3-yl)ethyl]-D-typtophanamide, acetate
CAS Number
945212-59-9
Synonyms
  • AEZS-130
  • Aib-D-Trp-D-gTrp-CHO
  • Aib-D-Trp-D-gTrp-formyl
  • D 87575
  • EP 1572
  • JMV1843
Molecular Formula
C26H30N6O3 • C2H4O2
Formula Weight
534.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
CC(O)=O.O=CN[C@@H](CC1=CNC2=CC=CC=C12)NC([C@H](NC(C(C)(N)C)=O)CC3=CNC4=CC=CC=C34)=O
InChi Code
InChI=1S/C26H30N6O3.C2H4O2/c1-26(2,27)25(35)31-22(11-16-13-28-20-9-5-3-7-18(16)20)24(34)32-23(30-15-33)12-17-14-29-21-10-6-4-8-19(17)21;1-2(3)4/h3-10,13-15,22-23,28-29H,11-12,27H2,1-2H3,(H,30,33)(H,31,35)(H,32,34);1H3,(H,3,4)/t22-,23-;/m1./s1
InChi Key
WVDSKQXKCDZXLH-OHIDFYLOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $160

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    10 mg

    $288

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    25 mg

    $519

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    50 mg

    $798

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    Product Description

    Macimorelin is a growth hormone secretagogue and agonist of growth hormone secretagogue receptor 1a (GHS-R1a).1 It binds to GHS-R1a (IC50 = 123 nM for the human receptor). Oral administration of macimorelin (1 mg/kg) increases plasma growth hormone levels in dogs. It decreases gastric acid secretion in pylorus-ligated rats when administered intracerebroventricularly at doses of 0.01 or 1 nmol/animal.2 Macimorelin (10 mg/kg) increases acute food intake and body weight in mice.3 It decreases the number and total duration of seizures in mice induced with dopamine D1 receptor kindling using SKF 81297.4 Formulations containing macimorelin have been used in the diagnosis of adult growth hormone deficiency.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Guerlavais, V., Boeglin, D., Mousseaux, D., et al. New active series of growth hormone secretagogues. J. Med. Chem. 46(7), 1191-1203 (2003).

    2. Sibilia, V., Muccioli, G., Deghenghi, R., et al. Evidence for a role of the GHS-R1a receptors in ghrelin inhibition of gastric acid secretion in the rat. J. Neuroendocrinol. 18(2), 122-128 (2006).

    3. Holubová, M., Spolcová, A., Demianová, Z., et al. Ghrelin agonist JMV 1843 increases food intake, body weight and expression of orexigenic neuropeptides in mice. Physiol. Res. 62(4), 435-444 (2013).

    4. Buckinx, A., Van Den Herrewegen, Y., Pierre, A., et al. Differential effects of a full and biased ghrelin receptor agonist in a mouse kindling model. Int. J. Mol. Sci. 20(10), 2480 (2019).