L-692429

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.

Product information

CAS Number: 145455-23-8

Molecular Weight: 509.60

Formula: C29H31N7O2

Chemical Name: 3-amino-3-methyl-N-[(3R)-2-oxo-1-{[2'-(2H-1,2,3,4-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl]methyl}-2,3,4,5-tetrahydro-1H-1-benzazepin-3-yl]butanamide

Smiles: CC(C)(N)CC(=O)N[C@@H]1CCC2=CC=CC=C2N(CC2C=CC(=CC=2)C2=CC=CC=C2C2=NNN=N2)C1=O

InChiKey: SBJLJOFPWOYATP-XMMPIXPASA-N

InChi: InChI=1S/C29H31N7O2/c1-29(2,30)17-26(37)31-24-16-15-21-7-3-6-10-25(21)36(28(24)38)18-19-11-13-20(14-12-19)22-8-4-5-9-23(22)27-32-34-35-33-27/h3-14,24H,15-18,30H2,1-2H3,(H,31,37)(H,32,33,34,35)/t24-/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 50 mg/mL (98.12 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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. 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.

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.

Products are for research use only. Not for human use.