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L-692429

Catalog No. T11798 CAS 145455-23-8

Synonyms: MK-0751

L-692429 (MK-0751) is a potent nonpeptidyl growth hormone secretagogue (GHS) agonist, a benzolactam derivative, which reverses the inhibition of GH secretion by glucocorticoids.L-692429 has a high affinity for the G protein-coupled receptor and can be used in the study of acromegaly and obesity. L-692429 has a high affinity for G protein-coupled receptor and can be used to study acromegaly and obesity.

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L-692429, CAS 145455-23-8

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1 mg	In stock	$ 249.00

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Purity: 99.9%

Biological Description

Chemical Properties

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Description	L-692429 (MK-0751) is a potent nonpeptidyl growth hormone secretagogue (GHS) agonist, a benzolactam derivative, which reverses the inhibition of GH secretion by glucocorticoids.L-692429 has a high affinity for the G protein-coupled receptor and can be used in the study of acromegaly and obesity. L-692429 has a high affinity for G protein-coupled receptor and can be used to study acromegaly and obesity.
Targets&IC50	intracellular calcium:26 nM (EC50), BRET:58 nM (EC50), inositol phosphate (IP) turnover:47 nM (EC50), Serum-responsive element activity:63 nM (EC50), CREB:60 nM (EC50)
In vitro	L-692429, a chemical compound, activates various cellular mechanisms, including 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]. In experiments involving HeLa-T4 cells, those transiently expressing flag epitope-tagged growth hormone secretagogue (GHS) receptor and treated with L-692429 show a measurable increase in intracellular calcium, as detected by fluorometry using fluo-3/AM calcium indicator dye. This response is absent in untransfected HeLa-T4 cells, indicating the specificity of L-692429 for GHS receptor-expressing cells. Moreover, L-692429 treatment significantly enhances luciferase activity in these cells, suggesting that GHS receptor activation triggers the MAPK pathway[1].
In vivo	In anesthetized Wistar rats, L-756867 dose-dependently suppresses GH secretion stimulated by L-692429 (100 μg/kg), with complete inhibition achieved at an intravenous dose of 100 μg/kg of L-756867[3].

Synonyms	MK-0751
Molecular Weight	509.614
Formula	C29H31N7O2
CAS No.	145455-23-8

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 40 mg/mL (78.49 mM), Sonication is recommended.

References and Literature

1. Cheng K, et al. Inhibition of L-692,429-stimulated rat growth hormone release by a weak substance P antagonist: L-756,867. J Endocrinol. 1997 Jan;152(1):155-8. 2. Holst B, et al. Nonpeptide and peptide growth hormone secretagogues act both as ghrelin receptor agonist and as positive or negative allosteric modulators of ghrelin signaling. Mol Endocrinol. 2005 Sep;19(9):2400-11. 3. Cunha SR, et al. Ghrelin and growth hormone (GH) secretagogues potentiate GH-releasing hormone (GHRH)-induced cyclic adenosine 3',5'-monophosphate production in cells expressing transfected GHRH and GH secretagogue receptors. Endocrinology. 2002 Dec;143(12):4570-82.

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Keywords

L-692429 145455-23-8 GPCR/G Protein GHSR GPCR19 MK 0751 L692429 MK0751 MK-0751 L 692429 inhibitor inhibit

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