Ibutamoren
Based on 5 publication(s) in Google Scholar
Ibutamoren (MK-677 free base; MK-0677 free base) is an orally active non-peptide growth hormone secretagogue receptor agonist. Ibutamoren activates signal cascades by mimicking endogenous ligands, triggers pulsatile release of growth hormone from the pituitary gland, and increases serum levels of IGF-1 and insulin-like growth factor-binding protein 3. Ibutamoren not only increases the frequency of growth hormone pulses in male individuals, but also promotes elevated bone formation markers in female individuals with postmenopausal osteoporosis. The combination of Ibutamoren with Alendronate sodium hydrate (HY-11101) significantly increases bone mineral density at the femoral neck. However, Ibutamoren may cause mild, reversible adverse reactions such as increased appetite, fluid retention, and elevated fasting blood glucose. Ibutamoren has been widely used in studies related to idiopathic growth hormone deficiency, sarcopenia, Alzheimer's disease, and osteoporosis.
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- Pureza: 99.84%
- No. CAS: 159634-47-6
- Fòrmula: C27H36N4O5S
- Peso molecular:528.66
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Ibutamoren
More
Actividad biológica
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GHSR1a |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | IC50 |
0.51 nM
Compound: 25
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Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cells
Ability to displace [125I]ghrelin from cloned human Growth hormone secretagogue receptor type I (GSH1a) receptor expressed in COS-7 cells
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[PMID: 12477342] |
| HEK293 | EC50 |
1.43 nM
Compound: MK-677
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Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
Functional potency measured as intracellular calcium elevation in Hek-293 cells expressing hGHSR1a
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[PMID: 11459669] |
| Pituitary gland cell | EC50 |
0.6 nM
Compound: MK-677
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Concentration required for GH release from isolated pituitary cells of rat tested in vitro
Concentration required for GH release from isolated pituitary cells of rat tested in vitro
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[PMID: 11459660] |
| Pituitary gland cell | EC50 |
1 nM
Compound: 2
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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 |
1.3 nM
Compound: 3a(MK-677)
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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 | EC50 |
1.3 nM
Compound: L-163191
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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 | EC50 |
1.3 nM
Compound: MK 0677
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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 | EC50 |
1.3 nM
Compound: MK-0677
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Agonist activity at GHS-R1a in rat pituitary cells
Agonist activity at GHS-R1a in rat pituitary cells
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[PMID: 23816043] |
| Pituitary gland cell | EC50 |
1.3 nM
Compound: MK-677
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Effective concentration for ability to release growth hormone from rat pituitary cells
Effective concentration for ability to release growth hormone from rat pituitary cells
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[PMID: 11708912] |
| Pituitary gland cell | EC50 |
1.3 nM
Compound: MK-677
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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 |
1.5 nM
Compound: MK-0677
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Stimulation of growth hormone in rat pituitary cell
Stimulation of growth hormone in rat pituitary cell
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[PMID: 17482461] |
| Pituitary gland cell | IC50 |
1.3 μM
Compound: 2
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The effective concentration against rat pituitary cell GH release assay
The effective concentration against rat pituitary cell GH release assay
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[PMID: 10636230] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 159634-47-6
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Appearance Solid
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Peso molecular 528.66
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Fòrmula C27H36N4O5S
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Color White to off-white
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SMILES
O=S(N1C2=C(C(CCN3C([C@@H](COCC4=CC=CC=C4)NC(C(C)(C)N)=O)=O)(CC3)C1)C=CC=C2)(C)=O
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Synonyms
MK-677 free base; MK-0677 free base
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Anal Bioanal Chem
Fully automated dried blood spot sample preparation enables the detection of lower molecular mass peptide and non-peptide doping agents by means of LC-HRMS. [Abstract]2020 Jun;412(15):3765-3777. PMID: 32300840 -
Drug Test Anal
An in vitro assay approach to investigate the potential impact of different doping agents on the steroid profile. [Abstract]2021 May;13(5):916-928. PMID: 33283964 -
Drug Test Anal
Recent improvements in sports drug testing concerning the initial testing for peptidic drugs (< 2 kDa) - sample preparation, mass spectrometric detection, and data review. [Abstract]2018 Nov;10(11-12):1755-1760. PMID: 30239151 -
Amino Acids
Novel bioluminescent receptor-binding assays for peptide hormones: using ghrelin as a model. [Abstract]2015 Oct;47(10):2237-43. PMID: 26002812 -
Solvente y solubilidad
DMSO : 62.5 mg/mL (118.22 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 (4.73 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 (4.73 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.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Codner E, et al. Effects of oral administration of ibutamoren mesylate, a nonpeptide growth hormone secretagogue, on the growth hormone-insulin-like growth factor I axis in growth hormone-deficient children. Clin Pharmacol Ther. 2001;70(1):91-98. [Content Brief]
[2]. Sigalos JT, et al. The Safety and Efficacy of Growth Hormone Secretagogues. Sex Med Rev. 2018;6(1):45-53. [Content Brief]
[3]. Murphy MG, et al. Effect of alendronate and MK-677 (a growth hormone secretagogue), individually and in combination, on markers of bone turnover and bone mineral density in postmenopausal osteoporotic women. J Clin Endocrinol Metab. 2001;86(3):1116-1125. [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 | 1.8916 mL | 9.4579 mL | 18.9158 mL | 47.2894 mL |
| 5 mM | 0.3783 mL | 1.8916 mL | 3.7832 mL | 9.4579 mL | |
| 10 mM | 0.1892 mL | 0.9458 mL | 1.8916 mL | 4.7289 mL | |
| 15 mM | 0.1261 mL | 0.6305 mL | 1.2611 mL | 3.1526 mL | |
| 20 mM | 0.0946 mL | 0.4729 mL | 0.9458 mL | 2.3645 mL | |
| 25 mM | 0.0757 mL | 0.3783 mL | 0.7566 mL | 1.8916 mL | |
| 30 mM | 0.0631 mL | 0.3153 mL | 0.6305 mL | 1.5763 mL | |
| 40 mM | 0.0473 mL | 0.2364 mL | 0.4729 mL | 1.1822 mL | |
| 50 mM | 0.0378 mL | 0.1892 mL | 0.3783 mL | 0.9458 mL | |
| 60 mM | 0.0315 mL | 0.1576 mL | 0.3153 mL | 0.7882 mL | |
| 80 mM | 0.0236 mL | 0.1182 mL | 0.2364 mL | 0.5911 mL | |
| 100 mM | 0.0189 mL | 0.0946 mL | 0.1892 mL | 0.4729 mL |
Ibutamoren Related Classifications
Referencia número: HY-10199A
Powered by Bioz
- Ibutamoren
- 159634-47-6
- MK-677
- MK-0677
- MK677
- MK 677
- MK0677
- MK 0677
- GHSR
- Insulin Receptor
- fibromyalgia
- growth hormone secretagogue receptor
- insulin-like growth factor I
- postmenopausal osteoporotic women
- Alzheimer's disease
- young healthy men
- pituitary gland
- growth hormone
- insulin-like growth factor binding protein 3
- idiopathic growth hormone deficiency
- Inhibitor
- inhibitor
- inhibit