Ibutamoren Mesylate (MK-677) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist. Ibutamoren Mesylate is an orally active growth hormone (GH) secretagogue.
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Ibutamoren Mesylate Estructura química
No. CAS : 159752-10-0
Tamaño Precio Stock Cantidad Muestra gratis (0.1 - 0.2 mg) Solicite ahora Solid + Solvent (Highly Recommended) 10 mM * 1 mL in DMSO
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Based on 5 publication(s) in Google Scholar
Other Forms of Ibutamoren Mesylate:
Ibutamoren In-stock
•Drug Test Anal. 2021 May;13(5):916-928. [Abstract] •Anal Bioanal Chem. 2020 Jun;412(15):3765-3777. [Abstract] •Drug Test Anal. 2018 Nov;10(11-12):1755-1760. [Abstract] •Amino Acids. 2015 Oct;47(10):2237-43. [Abstract] •German Sport University Cologne. 2022.
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Descripciòn
Ibutamoren Mesylate (MK-677) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist. Ibutamoren Mesylate is an orally active growth hormone (GH) secretagogue. In Vivo
Ibutamoren mesylate (5 mg/kg/day) results in a statistically significant increases body weight gain and increases serum IGF-1 and GH levels in dogs. Ibutamoren mesylate results in no significant increase in CSF IGF-1 or GH levels on days 7 or 15 of the study[1]. Pretreating mice with GH blocks activation of these neurons by Ibutamoren mesylate (50 μg, i.p.). In the knockout mice, both GH and octreotide fail to inhibit Ibutamoren mesylate activation of arcuate neurons[2]. Chronic oral administration of Ibutamoren mesylate is associated with significant increases in GH and IGF-I levels that are maintained for the duration of the treatment. The GH profile following Ibutamoren mesylate administration consists of episodic increases above control[3]. Ibutamoren mesylate significantly increases peak GH concentrations after oral administration. Ibutamoren mesylate is a potent GH secretagogue that induces an immediate, large, long lasting increase in GH levels when administered orally or i.v[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Peso molecular
624.77 Fòrmula
C28H40N4O8S2 No. CAS
159752-10-0 Appearance
Solid Color
White to light yellow SMILES
CC(N)(C(N[C@@H](C(N1CCC2(CN(C3=C2C=CC=C3)S(=O)(C)=O)CC1)=O)COCC4=CC=CC=C4)=O)C.CS(=O)(O)=O Envío
Room temperature in continental US; may vary elsewhere. Almacenamiento
4°C, sealed storage, away from moisture Solvente y solubilidad
In Vitro:
DMSO : 50 mg/mL (80.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL (80.03 mM)
*"≥" means soluble, but saturation unknown.
Preparing Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6006 mL 8.0029 mL 16.0059 mL 5 mM 0.3201 mL 1.6006 mL 3.2012 mL
View the 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Calculadora de molaridad
Calculadora de dilución
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Mass
= Concentration
× Volume
× Molecular Weight *
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 Concentration (start)
C1
× Volume (start)
V1
= Concentration (final)
C2
× Volume (final)
V2
In Vivo:
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.
Protocol 1
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.00 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.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.00 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.
For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time. 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.
Protocol 1
Add each solvent one by one: PBS
Solubility: 100 mg/mL (160.06 mM); Clear solution; Need ultrasonic
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE). Pureza y Documentación
Purity: 99.86%
Select Batch:
SDS (558 KB)
COA (252 KB) HNMR (305 KB) LCMS (86 KB)
Instrucciones de manejo (2659 KB) Referencias
[1]. Prahalada S, et al. Insulin-like growth factor-1 and growth hormone (GH) levels in canine cerebrospinal fluid are unaffected by GH or GH secretagogue (MK-0677) administration. Horm Metab Res. 1999 Feb-Mar;31(2-3):133-7. [Content Brief]
[2]. Zheng H, et al. Somatostatin receptor subtype 2 knockout mice are refractory to growth hormone-negative feedback on arcuate neurons. Mol Endocrinol. 1997 Oct;11(11):1709-17. [Content Brief]
[3]. Hickey GJ, et al. Repeat administration of the GH secretagogue MK-0677 increases and maintains elevated IGF-I levels in beagles. J Endocrinol. 1997 Feb;152(2):183-92. [Content Brief]
[4]. Jacks T, et al. MK-0677, a potent, novel, orally active growth hormone (GH) secretagogue: GH, insulin-like growth factor I, and other hormonal responses in beagles. Endocrinology. 1996 Dec;137(12):5284-9. [Content Brief]
Administraciòn de animales [2]
Compounds used are: Ibutamoren mesylate (50 μg), octreotide (100 μg), and mGH (30 μg). Mice are give an initial ip injection (0.1 mL) of either saline, octreotide or mGH, followed 10 min later by an ip injection (0.1 mL) of either saline or Ibutamoren mesylate. Thus, the first study comprised of the following groups: saline/saline, saline/Ibutamoren mesylate, mGH/saline, mGH/Ibutamoren mesylate saline/saline, saline/Ibutamoren mesylate, mGH/saline, mGH/Ibutamoren mesylate, and the second study of: saline/saline, saline/Ibutamoren mesylate, octreotide/saline, octreotide/Ibutamoren mesylate. Additionally, a number of mice are injected ip with hypertonic saline (0.2 mL, 1.5 M) to serve as positive controls for the immunocytochemistry. Ninety minutes after injection animals are terminally anesthetized with sodium pentobarbitone (60 mg/kg, ip) and perfused transcardially with heparinized saline followed by 4% paraformaldehyde in 0.1mol/Lphosphate buffer (PB, pH 7.4). Brains are then removed and placed in the same solution for 24 h before being stored at− 80°C until processing. Coronal sections of forebrain (40 μM) are cut on a freezing microtome and placed in 0.1mol/LPB containing Triton X-100 (PB-T, pH 7.4). Sections are incubated for 24 h at 4°C in Ab-2 Fos antibody (rabbit polyclonal; 1:1000 in 1% normal sheep serum). The antibody-antigen complex is localized with a 1-h incubation in biotinylated anti-rabbit Ig, followed by a 1-h incubation in avidin, biotinylated horseradish peroxidase. The reaction product is visualized using a glucose oxidase-diaminobenzidine-nickel method, and Fos-like immunoreactivity is visualized as a dense purple-black precipitate restricted to the nucleus. The number of c-fos positive nuclei in the arcuate and periventricular nuclei (six to eight sections per mouse) are counted double-blind and a group mean calculated (mean±sem). Statistical analysis is performed by a two-way ANOVA followed by an all pairwise multiple comparison of data with significance taken as P < 0.05.
MCE no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia. Referencias
[1]. Prahalada S, et al. Insulin-like growth factor-1 and growth hormone (GH) levels in canine cerebrospinal fluid are unaffected by GH or GH secretagogue (MK-0677) administration. Horm Metab Res. 1999 Feb-Mar;31(2-3):133-7. [Content Brief]
[2]. Zheng H, et al. Somatostatin receptor subtype 2 knockout mice are refractory to growth hormone-negative feedback on arcuate neurons. Mol Endocrinol. 1997 Oct;11(11):1709-17. [Content Brief]
[3]. Hickey GJ, et al. Repeat administration of the GH secretagogue MK-0677 increases and maintains elevated IGF-I levels in beagles. J Endocrinol. 1997 Feb;152(2):183-92. [Content Brief]
[4]. Jacks T, et al. MK-0677, a potent, novel, orally active growth hormone (GH) secretagogue: GH, insulin-like growth factor I, and other hormonal responses in beagles. Endocrinology. 1996 Dec;137(12):5284-9. [Content Brief]
[1]. Prahalada S, et al. Insulin-like growth factor-1 and growth hormone (GH) levels in canine cerebrospinal fluid are unaffected by GH or GH secretagogue (MK-0677) administration. Horm Metab Res. 1999 Feb-Mar;31(2-3):133-7.
[2]. Zheng H, et al. Somatostatin receptor subtype 2 knockout mice are refractory to growth hormone-negative feedback on arcuate neurons. Mol Endocrinol. 1997 Oct;11(11):1709-17.
[3]. Hickey GJ, et al. Repeat administration of the GH secretagogue MK-0677 increases and maintains elevated IGF-I levels in beagles. J Endocrinol. 1997 Feb;152(2):183-92.
[4]. Jacks T, et al. MK-0677, a potent, novel, orally active growth hormone (GH) secretagogue: GH, insulin-like growth factor I, and other hormonal responses in beagles. Endocrinology. 1996 Dec;137(12):5284-9.
* 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 (sealed storage, away from moisture). 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 / H2O 1 mM 1.6006 mL 8.0029 mL 16.0059 mL 40.0147 mL 5 mM 0.3201 mL 1.6006 mL 3.2012 mL 8.0029 mL 10 mM 0.1601 mL 0.8003 mL 1.6006 mL 4.0015 mL 15 mM 0.1067 mL 0.5335 mL 1.0671 mL 2.6676 mL 20 mM 0.0800 mL 0.4001 mL 0.8003 mL 2.0007 mL 25 mM 0.0640 mL 0.3201 mL 0.6402 mL 1.6006 mL 30 mM 0.0534 mL 0.2668 mL 0.5335 mL 1.3338 mL 40 mM 0.0400 mL 0.2001 mL 0.4001 mL 1.0004 mL 50 mM 0.0320 mL 0.1601 mL 0.3201 mL 0.8003 mL 60 mM 0.0267 mL 0.1334 mL 0.2668 mL 0.6669 mL 80 mM 0.0200 mL 0.1000 mL 0.2001 mL 0.5002 mL
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Disease Areas Metabolic or Endocrine Disease
Endocrinology
GPCR/G Protein GHSR
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Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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