L-692429
Based on 1 Customer Validation
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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.53%
- CAS. Nr.: 145455-23-8
- Formel: C29H31N7O2
- Molecular Weight:509.60
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Pituitary gland cell | ED50 |
0.06 μM
Compound: L-692429
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In vitro growth hormone release in rat pituitary cells assay was determined
In vitro growth hormone release in rat pituitary cells assay was determined
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[PMID: 10576695] |
| Pituitary gland cell | EC50 |
60 nM
Compound: L-692429
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In vitro growth hormone releasing activity was measured in rat pituitary cells
In vitro growth hormone releasing activity was measured in rat pituitary cells
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[PMID: 11741481] |
| Pituitary gland cell | EC50 |
60 nM
Compound: 1
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Effective concentration for their ability to release growth hormone in the rat pituitary cell assay
Effective concentration for their ability to release growth hormone in the rat pituitary cell assay
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[PMID: 12729672] |
| Pituitary gland cell | EC50 |
60 nM
Compound: L692 429
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Stimulation of growth hormone secretion in rat pituitary cells
Stimulation of growth hormone secretion in rat pituitary cells
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[PMID: 35344905] |
| Pituitary gland cell | ED50 |
60 nM
Compound: 1, (L-692429)
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In vitro dose required for stimulation of GH release from rat pituitary cells
In vitro dose required for stimulation of GH release from rat pituitary cells
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[PMID: 8151616] |
| Pituitary gland cell | EC50 |
60 nM
Compound: 2a, (L-692429)
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Effective Concentration for GH secretion from rat pituitary cell was determined
Effective Concentration for GH secretion from rat pituitary cell was determined
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[PMID: 8627599] |
| Pituitary gland cell | ED50 |
60 nM
Compound: 1
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In vitro growth hormone (GH) releasing activity in rat primary pituitary cells.
In vitro growth hormone (GH) releasing activity in rat primary pituitary cells.
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[PMID: 9572898] |
| Pituitary gland cell | EC50 |
60 nM
Compound: L-692429
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In vitro growth hormone release was determined in rat pituitary cell assay
In vitro growth hormone release was determined in rat pituitary cell assay
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[PMID: 9925440] |
| Pituitary gland cell | ED50 |
0.06 μM
Compound: 1
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Effective dose of compound required for in vitro effect on growth hormone release was measured in rat pituitary cell assay
Effective dose of compound required for in vitro effect on growth hormone release was measured in rat pituitary cell assay
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10.1016/0960-894X(95)00209-C |
| Pituitary gland cell | ED50 |
60 nM
Compound: 1, (L-692429)
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In vitro Growth hormone releasing activity in rat pituitary cells
In vitro Growth hormone releasing activity in rat pituitary cells
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10.1016/0960-894X(95)00389-B |
| Pituitary gland cell | EC50 |
60 nM
Compound: L-692429
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In vitro for growth hormone release by using rat pituitary cell assay.
In vitro for growth hormone release by using rat pituitary cell assay.
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10.1016/0960-894X(96)00394-0 |
| Pituitary gland cell | ED50 |
60 nM
Compound: 1, (L-692429)
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Tested in vitro for growth hormone release in rat pituitary cells
Tested in vitro for growth hormone release in rat pituitary cells
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10.1016/S0960-894X(00)80080-3 |
| Pituitary gland cell | ED50 |
0.06 μM
Compound: L-692429
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In vitro effective dose was measured for the growth hormone release in rat pituitary cells
In vitro effective dose was measured for the growth hormone release in rat pituitary cells
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10.1016/S0960-894X(01)80239-0 |
| Pituitary gland cell | ED50 |
0.06 μM
Compound: 2, (L-692429)
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In vitro effective dose for the growth hormone(GH) release in rat pituitary cells
In vitro effective dose for the growth hormone(GH) release in rat pituitary cells
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10.1016/S0960-894X(01)80375-9 |
| Pituitary gland cell | ED50 |
60 nM
Compound: L-692429
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Growth hormone release from rat pituitary cells
Growth hormone release from rat pituitary cells
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10.1016/S0960-894X(01)80702-2 |
| Pituitary gland cell | ED50 |
0.06 μM
Compound: L-692429
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In vitro growth hormone release in rat pituitary cells
In vitro growth hormone release in rat pituitary cells
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10.1016/S0960-894X(96)00566-5 |
| Pituitary gland cell | EC50 |
125 nM
Compound: 2
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The compound was tested in vitro for the growth hormone release in rat pituitary cell assays
The compound was tested in vitro for the growth hormone release in rat pituitary cell assays
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10.1016/S0960-894X(97)00216-3 |
| Pituitary gland cell | EC50 |
60 nM
Compound: L-692429
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Ability to release growth hormone in a rat pituitary cell assay
Ability to release growth hormone in a rat pituitary cell assay
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10.1016/S0960-894X(97)00421-6 |
| Pituitary gland cell | ED50 |
125 nM
Compound: 1
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Compound was evaluated for its potency using rat pituitary cell assay
Compound was evaluated for its potency using rat pituitary cell assay
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10.1016/S0960-894X(97)10115-9 |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 145455-23-8
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Appearance Solid
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Molecular Weight 509.60
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Formel C29H31N7O2
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Color White to off-white
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SMILES
CC(C)(N)CC(N[C@H]1C(N(CC2=CC=C(C3=CC=CC=C3C4=NNN=N4)C=C2)C5=CC=CC=C5CC1)=O)=O
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Synonyms
MK-0751
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (98.12 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[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. [Content Brief]
[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(1 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9623 mL | 9.8116 mL | 19.6232 mL | 49.0581 mL |
| 5 mM | 0.3925 mL | 1.9623 mL | 3.9246 mL | 9.8116 mL | |
| 10 mM | 0.1962 mL | 0.9812 mL | 1.9623 mL | 4.9058 mL | |
| 15 mM | 0.1308 mL | 0.6541 mL | 1.3082 mL | 3.2705 mL | |
| 20 mM | 0.0981 mL | 0.4906 mL | 0.9812 mL | 2.4529 mL | |
| 25 mM | 0.0785 mL | 0.3925 mL | 0.7849 mL | 1.9623 mL | |
| 30 mM | 0.0654 mL | 0.3271 mL | 0.6541 mL | 1.6353 mL | |
| 40 mM | 0.0491 mL | 0.2453 mL | 0.4906 mL | 1.2265 mL | |
| 50 mM | 0.0392 mL | 0.1962 mL | 0.3925 mL | 0.9812 mL | |
| 60 mM | 0.0327 mL | 0.1635 mL | 0.3271 mL | 0.8176 mL | |
| 80 mM | 0.0245 mL | 0.1226 mL | 0.2453 mL | 0.6132 mL |
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