L-692585
Based on 1 Customer Validation
L-692585 is a potent and nonpeptidyl growth hormone secretagogue receptor (GHS-R1a) agonist, with a Ki of 0.8 nM. L-692585 acts directly on somatotropes causing GH release.
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- Pureté: 98.94%
- CAS No.: 145455-35-2
- Formule: C32H37N7O3
- Masse moléculaire:567.68
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Ki: 0.8 nM (GHS-R1a)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Pituitary gland cell | ED50 |
3 nM
Compound: 2, (L-692585)
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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 | ED50 |
3 nM
Compound: 7
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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 |
3 μM
Compound: 24, (L-692585)
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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 |
3 nM
Compound: 7
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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 |
0.003 μM
Compound: L-692585
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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 |
3 nM
Compound: 1, (L-692585)
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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 |
L-692585 (10 µM; 2 min) produces a prompt transient increase in [Ca2+]i, following by the sustained decline to a plateau above the basal level in GH cells[2].
L-692585 (0.01-10 µM; 2 min) induces release of growth hormone (GH) in a dose-dependent manner from isolated porcine somatotropes[2].
L-692585 (100 nM) significantly increases the number and size of plaques, and it also causes a significant increase in total secretion index (TSI) [2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
L-692585 (0.005-0.1 mg/kg; a single i.v.) significantly increases peak GH concentrations 4.3-fold at a dose of 0.005 mg/kg, 7-fold at a dose of 0.02 mg/kg, and 21-fold at a dose of 0.10 mg/kg in vivo[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Beagles (1-1.5 years old ; weighting 8.5-16.0 kg)[3]
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Dosage:0.01, 0.1 mg/kg
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Administration:I.v. once daily for 2 weeks
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Result:Increased the peak plasma GH levels and total GH release on days 1, 8 and 15 in a dose-dependent manner, and no desensitization was evident.
Chemical Information
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CAS No. 145455-35-2
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Appearance Solid
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Masse moléculaire 567.68
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Formule C32H37N7O3
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Color White to off-white
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SMILES
CC(C)(NC[C@H](O)C)CC(N[C@H]1C(N(CC2=CC=C(C3=CC=CC=C3C4=NN=NN4)C=C2)C5=CC=CC=C5CC1)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (176.16 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (4.40 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (4.40 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Smith RG, et, al. Peptidomimetic regulation of growth hormone secretion. Endocr Rev. 1997 Oct; 18(5): 621-45. [Content Brief]
[2]. Glavaski-Joksimovic A, et, al. Mechanism of action of the growth hormone secretagogue, L-692,585, on isolated porcine somatotropes. J Endocrinol. 2002 Dec; 175(3): 625-36. [Content Brief]
[3]. Jacks T, et, al. Effects of acute and repeated intravenous administration of L-692,585, a novel non-peptidyl growth hormone secretagogue, on plasma growth hormone, IGF-1, ACTH, cortisol, prolactin, insulin, and thyroxine levels in beagles. J Endocrinol. 1994 Nov; 143(2): 399-406. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7616 mL | 8.8078 mL | 17.6156 mL | 44.0389 mL |
| 5 mM | 0.3523 mL | 1.7616 mL | 3.5231 mL | 8.8078 mL | |
| 10 mM | 0.1762 mL | 0.8808 mL | 1.7616 mL | 4.4039 mL | |
| 15 mM | 0.1174 mL | 0.5872 mL | 1.1744 mL | 2.9359 mL | |
| 20 mM | 0.0881 mL | 0.4404 mL | 0.8808 mL | 2.2019 mL | |
| 25 mM | 0.0705 mL | 0.3523 mL | 0.7046 mL | 1.7616 mL | |
| 30 mM | 0.0587 mL | 0.2936 mL | 0.5872 mL | 1.4680 mL | |
| 40 mM | 0.0440 mL | 0.2202 mL | 0.4404 mL | 1.1010 mL | |
| 50 mM | 0.0352 mL | 0.1762 mL | 0.3523 mL | 0.8808 mL | |
| 60 mM | 0.0294 mL | 0.1468 mL | 0.2936 mL | 0.7340 mL | |
| 80 mM | 0.0220 mL | 0.1101 mL | 0.2202 mL | 0.5505 mL | |
| 100 mM | 0.0176 mL | 0.0881 mL | 0.1762 mL | 0.4404 mL |
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