Home >> Research Area >>GPCR/G protein>>GHSR>> Ibutamoren Mesylate

Ibutamoren Mesylate

Growth hormone (GH) secretagogue CAS# 159752-10-0

Ibutamoren Mesylate

Catalog No. BCC1638----Order now to get a substantial discount!

Product Name & Size Price Stock
Ibutamoren Mesylate: 5mg $115 In Stock
Ibutamoren Mesylate: 10mg Please Inquire In Stock
Ibutamoren Mesylate: 20mg Please Inquire Please Inquire
Ibutamoren Mesylate: 50mg Please Inquire Please Inquire
Ibutamoren Mesylate: 100mg Please Inquire Please Inquire
Ibutamoren Mesylate: 200mg Please Inquire Please Inquire
Ibutamoren Mesylate: 500mg Please Inquire Please Inquire
Ibutamoren Mesylate: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of Ibutamoren Mesylate

Number of papers citing our products

Chemical structure

Ibutamoren Mesylate

3D structure

Chemical Properties of Ibutamoren Mesylate

Cas No. 159752-10-0 SDF Download SDF
PubChem ID 6450830 Appearance Powder
Formula C28H40N4O8S2 M.Wt 624.77
Type of Compound N/A Storage Desiccate at -20°C
Synonyms MK-677;Crescendo;MK 0677;MK-0677;MK0677
Solubility DMSO : 50 mg/mL (80.03 mM; Need ultrasonic)
H2O : ≥ 50 mg/mL (80.03 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 2-amino-2-methyl-N-[(2R)-1-(1-methylsulfonylspiro[2H-indole-3,4'-piperidine]-1'-yl)-1-oxo-3-phenylmethoxypropan-2-yl]propanamide;methanesulfonic acid
SMILES CC(C)(C(=O)NC(COCC1=CC=CC=C1)C(=O)N2CCC3(CC2)CN(C4=CC=CC=C34)S(=O)(=O)C)N.CS(=O)(=O)O
Standard InChIKey DUGMCDWNXXFHDE-VZYDHVRKSA-N
Standard InChI InChI=1S/C27H36N4O5S.CH4O3S/c1-26(2,28)25(33)29-22(18-36-17-20-9-5-4-6-10-20)24(32)30-15-13-27(14-16-30)19-31(37(3,34)35)23-12-8-7-11-21(23)27;1-5(2,3)4/h4-12,22H,13-19,28H2,1-3H3,(H,29,33);1H3,(H,2,3,4)/t22-;/m1./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Ibutamoren Mesylate

DescriptionHigh affinity ghrelin receptor agonist (pKi = 8.14). Growth hormone (GH) secretagog; stimulates GH release from rat pituitary cells in vitro (EC50 = 1.3 nM) and enhances GH plasma levels in vivo. Also attenuates isoproterenol -induced lipolysis in rat adipocytes in vitro. Orally bioavailable.

Ibutamoren Mesylate Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

Ibutamoren Mesylate Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of Ibutamoren Mesylate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.6006 mL 8.0029 mL 16.0059 mL 32.0118 mL 40.0147 mL
5 mM 0.3201 mL 1.6006 mL 3.2012 mL 6.4024 mL 8.0029 mL
10 mM 0.1601 mL 0.8003 mL 1.6006 mL 3.2012 mL 4.0015 mL
50 mM 0.032 mL 0.1601 mL 0.3201 mL 0.6402 mL 0.8003 mL
100 mM 0.016 mL 0.08 mL 0.1601 mL 0.3201 mL 0.4001 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University

Background on Ibutamoren Mesylate

Ibutamoren mesylate (MK-0677) is an orally active nonpeptide growth hormone (GH) secretagogue. Ibutamoren mesylate (MK-0677) stimulates GH release through a pituitary and hypothalamic receptor that is different from the GH-releasing hormone receptor. MK-677is a drug which acts as a potent, orally active growth hormone secretagogue, mimicking the GH stimulating action of the endogenous hormone ghrelin. It has been demonstrated to increase the release of, and produces sustained increases in plasma levels of several hormones including growth hormone and IGF-1, but without affecting cortisol levels. It is currently under development as a potential treatment for reduced levels of these hormones, such as in growth hormone deficient children or elderly adults, and human studies have shown it to increase both muscle mass and bone mineral density, making it a promising therapy for the treatment of frailty in the elderly. Ibutamoren mesylate (MK-0677) also alters metabolism of body fat and so may have application in the treatment of obesity.

Featured Products
New Products
 

References on Ibutamoren Mesylate

MK-0677 (ibutamoren mesylate) for the treatment of patients recovering from hip fracture: a multicenter, randomized, placebo-controlled phase IIb study.[Pubmed:21067829]

Arch Gerontol Geriatr. 2011 Sep-Oct;53(2):183-9.

Most elderly patients admitted for hip fracture suffer functional decline. Previous studies with MK-0677 in hip fracture patients suggested possible benefits to functional recovery. This is a randomized, double-blind study of 123 elderly hip fracture patients assigned to receive 25mg/day of MK-0677 (n = 62) or placebo (n = 61). Primary outcomes were a rank analysis of change during the study in objective functional performance measurements and insulin-like growth factor-1 (IGF-1) levels in blood. At 24-weeks, the mean stair climbing power increased by 12.5 W in the MK-0677 group (95% confidence interval (CI) = -10.95-35.88; p = 0.292) compared with placebo. Gait speed increased by a 0.7-score difference in the means (95% CI = 0.17-1.28; p = 0.011). There was no improvement in MK-0677 treated patients in several other functional performance measures. The MK-0677 group experienced fewer falls during the study compared to placebo and smaller number of patients who had any falls (p = 0.096). Levels of IGF-1 in treated patients increased by 51.4 ng/ml (95% CI = 34.42-68.44; p < 0.001) compared to placebo. Trial was terminated early due to a safety signal of congestive heart failure in a limited number of patients. In hip fracture patients treated with 25mg/day MK-0677, the increase in plasma IGF-1 levels was not paralleled by improvement in most functional performance measures. MK-0677 has an unfavorable safety profile in this patient population.

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.[Pubmed:11452249]

Clin Pharmacol Ther. 2001 Jul;70(1):91-8.

Ibutamoren Mesylate (MK-0677), an orally active nonpeptide growth hormone (GH) secretagogue, stimulates GH release through a pituitary and hypothalamic receptor that is different from the GH-releasing hormone receptor. We evaluated the safety and tolerability and the GH-insulin-like growth factor (IGF) responses to two dosages of oral Ibutamoren Mesylate given to children with GH deficiency for 7 to 8 days. The patients, 18 prepubertal children (15 male, 3 female) with idiopathic GH deficiency, had a chronologic age of 10.6 +/- 0.8 years (mean +/- SD), bone age of 7.4 +/- 0.7 years, growth velocity < 10th percentile for age, height < 10th percentile for age, and a maximum GH response of < or = 10 microg/L to two different GH stimulation tests. The children were assigned as follows to one of three treatment groups with Ibutamoren Mesylate: 0.2 mg/kg per day for 7 days (days 1-7 or 8-14) and matching placebo for the alternate 7 days (groups I and II, respectively) or 0.8 mg/kg per day for 7 days (days 8-14, group III). On day 15 all patients received an 0.8-mg/kg dose of Ibutamoren Mesylate. Patients in groups I and II were studied first to assess safety at the low dose before advancement to the high dose. Hormonal profiles were evaluated on day -1 (baseline) and day 15, and the results were expressed as the change from baseline within each group. After administration of Ibutamoren Mesylate 0.8 mg/kg for 8 days (group III), the median increases (on day 15) from baseline were as follows: 3.8 microg/L (range, 0 to 34.3) for serum GH peak concentration (P = .001), 4.3 microg x h/L (range, 1.3 to 35.6) for the GH area under the concentration-time curve from time zero to 8 hours (AUC(0-8)) (P < .001), 12 microg/L (range, -4 to 116) for serum IGF-I (P = .01), and 0.4 microg/L (range, -0.9 to 1.5) for serum IGF-binding protein 3 (IGFBP-3) (P = .01). There was no change in serum prolactin, glucose, triiodothyronine, thyroxine, thyrotropin, peak serum cortisol, and insulin concentrations or 24-hour urinary free cortisol after administration of 0.8 mg/kg per day of Ibutamoren Mesylate for 8 days. We conclude that short-term administration of Ibutamoren Mesylate can increase GH, IGF-I, and IGFBP-3 levels in some children with GH deficiency. Thus this compound is applicable for testing its effect on growth velocity.

Growth hormone secretagogues and growth hormone releasing peptides act as orthosteric super-agonists but not allosteric regulators for activation of the G protein Galpha(o1) by the Ghrelin receptor.[Pubmed:19625579]

Mol Pharmacol. 2009 Oct;76(4):802-11.

Some growth hormone secretagogues act as agonists at the ghrelin receptor and have been described as "ago-allosteric" ligands because of an ability to also modulate the maximum efficacy and potency of ghrelin (Holst et al., 2005). In membranes prepared from cells coexpressing the human ghrelin receptor and the G protein Galpha(o1), N-[1(R)-1, 2-dihydro-1-ethanesulfonylspiro-3H-indole-3,4'-piperidin)-1'-yl]carbonyl-2-(pheny lmethoxy)-ethyl-2-amino-2-methylpropanamide (MK-677), growth hormone-releasing peptide 6 (GHRP-6), and the 2(R)-hydroxypropyl derivative of 3-amino-3-methyl-N-(2,3,4,5-tetrahydro-2-oxo-1-([2'-(1H-tetrazol-5-yl) (1,1'-biphenyl)-4-yl]methyl)-1H-1-benzazepin-3(R)-yl)-butanamide (L-692,585) each functioned as direct agonists, and each displayed higher efficacy than ghrelin. The effect of multiple, fixed concentrations of each of these ligands on the function and concentration-dependence of ghrelin and the effect of multiple, fixed concentrations of ghrelin on the action of MK-677, GHRP-6, and L-692,585 was analyzed globally according to a modified version of an operational model of allosterism that accounts for allosteric modulation of affinity, efficacy, and allosteric agonism. Each of the data sets was best fit by a model of simple competition between a partial and a full agonist. Both positive and negative allosteric modulators are anticipated to alter the kinetics of binding of an orthosteric agonist. However, none of the proposed ago-allosteric regulators tested had any effect on the dissociation kinetics of (125)I-[His]-ghrelin, and GHRP-6 and MK-677 were able to fully displace (125)I-[His]-ghrelin from the receptor. At least in the system tested, each of the ligands acted in a simple competitive fashion with ghrelin as demonstrated by analysis according to a model whereby ghrelin is a partial agonist with respect to each of the synthetic agonists tested.

Ghrelin and des-acyl ghrelin both inhibit isoproterenol-induced lipolysis in rat adipocytes via a non-type 1a growth hormone secretagogue receptor.[Pubmed:15363972]

Eur J Pharmacol. 2004 Sep 13;498(1-3):27-35.

Besides possessing a strong growth hormone (GH)-releasing activity, the gastrointestinal octanoylated peptide ghrelin has been reported to antagonize lipolysis in rat adipocytes. It is not yet clear whether this inhibitory activity on lipolysis is also shared by the major circulating isoform, des-acyl ghrelin, that does not activate the ghrelin receptor, namely the type 1a GH secretagogue-receptor (GHS-R1a) and lacks the endocrine effects of the acylated form. Here we show that des-acyl ghrelin, like ghrelin and some synthetic GHS (hexarelin and MK0677) and carboxy-terminally ghrelin fragments such as ghrelin-(1-5) and ghrelin-(1-10), all significantly reduced, over concentrations ranging from 1 to 1000 nM, the stimulation of glycerol release caused in rat epididymal adipocytes by the nonselective beta-adrenoceptor agonist isoproterenol in vitro. The order of potency on stimulated-lipolysis was: des-acyl ghrelin=ghrelin>MK0677=hexarelin>ghrelin-(1-5)=ghrelin-(1-10). This ranking was consistent with the binding experiments performed on membranes of epididymal adipose tissue or isolated adipocytes that did not express mRNA for GHS-R1a. A common high-affinity binding site was recognized in these cells by both acylated and des-acylated ghrelin and also by hexarelin, MK0677, ghrelin-(1-5) and ghrelin-(1-10). In conclusion, these findings provide the first evidence that des-acyl ghrelin, as well as ghrelin, short ghrelin fragments and synthetic GHS, may act directly as antilipolytic factors on the adipose tissue through binding to a specific receptor which is distinct from GHS-R1a.

Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue.[Pubmed:7624358]

Proc Natl Acad Sci U S A. 1995 Jul 18;92(15):7001-5.

A potent, orally active growth hormone (GH) secretagogue L-163,191 belonging to a recently synthesized structural class has been characterized. L-163,191 releases GH from rat pituitary cells in culture with EC50 = 1.3 +/- 0.09 nM and is mechanistically indistinguishable from the GH-releasing peptide GHRP-6 and the prototypical nonpeptide GH secretagogue L-692,429 but clearly distinguishable from the natural GH secretagogue, GH-releasing hormone. L-163,191 elevates GH in dogs after oral doses as low as 0.125 mg/kg and was shown to be specific in its release of GH without significant effect on plasma levels of aldosterone, luteinizing hormone, thyroxine, and prolactin after oral administration of 1 mg/kg. Only modest increases in cortisol were observed. Based on these properties, L-163,191 has been selected for clinical studies.

Description

Ibutamoren (Mesylate) is a potent, non-peptide Growth hormone secretagogue receptor (GHSR) agonist.

Keywords:

Ibutamoren Mesylate,159752-10-0,MK-677;Crescendo;MK 0677;MK-0677;MK0677,Natural Products,GHSR, buy Ibutamoren Mesylate , Ibutamoren Mesylate supplier , purchase Ibutamoren Mesylate , Ibutamoren Mesylate cost , Ibutamoren Mesylate manufacturer , order Ibutamoren Mesylate , high purity Ibutamoren Mesylate

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: