| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| 25mg | |||
| Other Sizes |
| Targets |
L-692429 targets the growth hormone secretagogue receptor (GHSR), also known as the ghrelin receptor. GHSR is a G protein-coupled receptor that is activated by ghrelin, a peptide hormone produced in the stomach. Activation of GHSR stimulates the release of growth hormone from the pituitary gland and has effects on appetite, metabolism, and energy balance. L-692429 is a non-peptidyl agonist that binds to GHSR with a Ki of 63 nM.
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| ln Vitro |
With EC50 values of 26 nM, 47 nM, 60 nM, 63 nM, and 58 nM, respectively, L-692429 stimulates intracellular calcium release, inositol phosphate (IP) turnover, cAMP response element binding protein (CREB) activity, serum response element activity, and bioluminescence resonance energy transfer (BRET) activity[2]. L-692429 was applied to HeLa-T4 cells that were transiently expressing the epitope-tagged growth hormone secretagogue (GHS) receptor. Calcium release within cells is measured by a fluorometric technique employing the calcium indicator dye Fluo-3/AM. L-692429 treatment had no effect on untransfected HeLa-T4 cells, however it did boost the fluorescence emission of HeLa-T4 cells that were transiently expressing GHS receptors. Following L-692429 administration, luciferase activity dramatically increased, suggesting that GHS receptor activation activates the MAPK pathway [3].
In vitro, L-692429 binds to the GHS receptor with high affinity (Ki = 63 nM). The compound stimulates growth hormone release from pituitary cells in culture, as measured by radioimmunoassay or ELISA. L-692429 activates GHSR-mediated signaling pathways, including the Gq/11-phospholipase C pathway, leading to increased intracellular calcium and the release of growth hormone. The compound's non-peptidyl nature makes it a valuable tool for studying GHSR pharmacology. |
| ln Vivo |
L-756867 demonstrated a dose-dependent inhibition of L-692429 (100 μg/kg)-stimulated GH production in Wistar rats under anesthesia. At an intravenous dosage of 100 μg/kg, L-756867 showed complete inhibition [1].
In vivo, L-692429 stimulates growth hormone release in animal models. Administration of the compound to rats or other species results in a rapid and dose-dependent increase in plasma growth hormone levels. L-692429 has been studied for its potential in the research of growth hormone deficiency and other conditions. However, specific in vivo efficacy data are limited in the available literature. |
| Enzyme Assay |
The non-cellular assay for L-692429 involves measuring its binding affinity for the GHS receptor using radioligand binding assays. Membrane preparations from cells expressing the GHS receptor are incubated with a radiolabeled GHS receptor ligand (such as [¹²⁵I]-ghrelin or [³H]-L-692429) and varying concentrations of unlabeled L-692429. The inhibition of radioligand binding is measured, and the Ki is determined from competition curves.
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| Cell Assay |
The cellular assay for L-692429 involves treating cells expressing the GHS receptor with the compound and measuring its effects on receptor-mediated signaling. Cells are loaded with a calcium-sensitive dye, and the increase in intracellular calcium in response to L-692429 stimulation is measured using fluorescence microscopy or a plate reader. The EC50 for receptor activation is determined from concentration-response curves. Growth hormone release from pituitary cells is measured by immunoassay.
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| Animal Protocol |
In the in vivo efficacy study, L-692429 is administered to rodents by intravenous injection or oral gavage. Blood samples are collected at various time points, and plasma growth hormone levels are measured by radioimmunoassay or ELISA. The compound's ability to stimulate growth hormone release is assessed, and the dose-response relationship is determined. The effects on food intake and body weight may also be evaluated.
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| ADME/Pharmacokinetics |
L-692429 has a molecular weight of 509.6 and a molecular formula of C₂₉H₃₁N₇O₂. The compound is soluble in DMSO. It should be stored as a powder at -20°C, protected from light and moisture. The compound has a purity of ≥98%. L-692429 should be handled with appropriate laboratory safety precautions.
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| Toxicity/Toxicokinetics |
The toxicological profile of L-692429 has not been extensively characterized in the published literature. As a GHS receptor agonist, it may have effects on growth hormone release, appetite, and metabolism. Comprehensive toxicology data are limited, and L-692429 is not approved for clinical use. The compound should be handled with appropriate laboratory safety precautions.
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| References |
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| Additional Infomation |
L-692429 is a non-peptidyl growth hormone secretagogue receptor agonist that has been used as a research tool to study the GHS receptor and growth hormone regulation. Its high affinity (Ki = 63 nM) and non-peptidyl nature make it a valuable tool for investigating the pharmacology of the ghrelin receptor and for developing new therapeutic strategies for growth hormone deficiency and metabolic disorders. The compound is not approved for clinical use and is strictly a research tool.
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| Molecular Formula |
C29H31N7O2
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|---|---|
| Molecular Weight |
509.6021
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| Exact Mass |
509.254
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| CAS # |
145455-23-8
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| Related CAS # |
169188-19-6 (HCl);145455-23-8;145455-80-7 (TFA);
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| PubChem CID |
121879
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| Appearance |
White to off-white solid powder
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| Density |
1.33g/cm3
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| Index of Refraction |
1.678
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| LogP |
5.23
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
38
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| Complexity |
815
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)(CC(=O)N[C@@H]1CCC2=CC=CC=C2N(C1=O)CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)N
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| InChi Key |
SBJLJOFPWOYATP-XMMPIXPASA-N
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| InChi Code |
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
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| Chemical Name |
3-amino-3-methyl-N-[(3R)-2-oxo-1-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-4,5-dihydro-3H-1-benzazepin-3-yl]butanamide
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| Synonyms |
L-692429L-692,429 L 692429 L 692,429 L692,429 L692429.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~98.12 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9623 mL | 9.8116 mL | 19.6232 mL | |
| 5 mM | 0.3925 mL | 1.9623 mL | 3.9246 mL | |
| 10 mM | 0.1962 mL | 0.9812 mL | 1.9623 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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