1. GPCR/G Protein
  2. GHSR
  3. L-692429

L-692429 (Synonyms: MK-0751)

Cat. No.: HY-10957
Handling Instructions

L-692429 (MK-0751) is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 binds to G protein-coupled receptor with a Ki of 63 nM.

For research use only. We do not sell to patients.

L-692429 Chemical Structure

L-692429 Chemical Structure

CAS No. : 145455-23-8

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Description

L-692429 (MK-0751) is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 binds to G protein-coupled receptor with a Ki of 63 nM[1][2].

IC50 & Target

Growth hormone secretagogue (GHS)[1][3]

In Vitro

L-692429 stimulates intracellular calcium release, inositol phosphate (IP) turnover, cAMP-responsive element binding protein (CREB) activity, serum-responsive element activity and bioluminescence resonance energy transfer (BRET) activity with EC50 values of 26 nM, 47 nM, 60 nM, 63 nM and 58 nM, respectively[2].
HeLa-T4 cells transiently expressing the flag epitope-tagged growth hormone secretagogue (GHS) receptor are treated with L-692429. The release of intracellular calcium is measured using fluorometry with the calcium indicator dye fluo-3/AM. Untransfected HeLa-T4 cells are unresponsive to L-692429 treatment, whereas HeLa-T4 cells transiently expressing GHS receptors demonstrate an increase in fluorescent emission after L-692429 treatment. A significant increase in luciferase activity after L-692429 treatment is seen, suggesting that activation of the GHS receptor stimulates the MAPK pathway[3].

In Vivo

When tested in anesthetized rats (Wistar rats), L-756867 inhibits L-692429 (100 μg/kg)-stimulated GH secretion in a dose-dependent manner. Complete inhibition is observed at an i.v. dose of 100 μg/kg of L-756867[1].

Molecular Weight

509.60

Formula

C₂₉H₃₁N₇O₂

CAS No.

145455-23-8

SMILES

CC(C)(N)CC(N[[email protected]]1C(N(CC2=CC=C(C3=CC=CC=C3C4=NNN=N4)C=C2)C5=CC=CC=C5CC1)=O)=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

L-692429MK-0751L692429L 692429MK0751MK 0751GHSRGrowth hormone secretagogue receptorBenzolactamnonpeptidylGHsecretagogueCREBBRETSREIPMAPKInhibitorinhibitorinhibit

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L-692429
Cat. No.:
HY-10957
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