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L-692429

SKU: orb1709298

Description

L-692429 (MK-0751) is a potent, nonpeptidyl benzolactam growth hormone secretagogue (GHS) receptor agonist. It effectively reverses glucocorticoid-induced suppression of GH secretion and is utilized in research models for studying acromegaly, obesity, and related metabolic disorders in both in vitro and in vivo experimental settings.

Research Area

Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number145455-23-8
MW509.614
Purity99.90%
FormulaC29H31N7O2
SMILESCC(C)(N)CC(=O)N[C@@H]1CCc2ccccc2N(Cc2ccc(cc2)-c2ccccc2-c2nn[nH]n2)C1=O
TargetGPCR19,GHSR
SolubilityDMSO:40 mg/mL (78.49 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.92 mM)

Bioactivity

Target IC50
CREB:60 nM (EC50)|BRET:58 nM (EC50)|Serum-responsive element activity:63 nM (EC50)|inositol phosphate (IP) turnover:47 nM (EC50)|intracellular calcium:26 nM (EC50)
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.
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. 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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Growth hormone secretagogue (GHS), GHSR, G protein-coupled Bile Acid Receptor 1, L692429, L-692429, MK 0751, MK0751, MK-0751, L 692429

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Key Properties

No computed properties available.

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Protocol Information

L-692429 (orb1709298)

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% DMSO +
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% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 2,600.00
5 mg
¥ 5,720.00
1 ml x 10 mM (in DMSO)
¥ 6,370.00
10 mg
¥ 8,190.00
25 mg
¥ 12,870.00
50 mg
¥ 17,160.00
100 mg
¥ 22,880.00
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