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L-692,429 is a new, potent nonpeptidyl growth hormone secretagogue (GHS) acting as an agonist of GHS with a Ki of 63 nM for binding to the GPCR.
| 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].
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| 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].
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| References |
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| Molecular Formula |
C29H31N7O2
|
|---|---|
| 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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