1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIbutamoren MesylateCat. No.: HY-50844CAS No.: 159752-10-0Synonyms: MK-677; MK-0677分式: CHNOS分量: 624.77作靶點(diǎn): GHSR作通路: GPCR/G Protein儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) H2O : 50 mg/mL (80.

2、03 mM)DMSO : 50 mg/mL (80.03 mM; Need ultrasonic)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.6006 mL 8.0029 mL 16.0059 mL5 mM 0.3201 mL 1.6006 mL 3.2012 mL10 mM 0.1601 mL 0.8003 mL 1.6006 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式

3、選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.00 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/3 Master of Small Molecules 您邊的抑制劑師w

4、ww.MedChemESolubility: 2.5 mg/mL (4.00 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.00 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Ibutamoren Mesylate種有效的，肽段類長(zhǎng)激素促分泌素受體 (GHSR) 激動(dòng)劑。體內(nèi)研究 Ibutamoren mesylate (5 mg/kg/day) results in a statistically significant increases b

5、ody weight gain andincreases serum IGF-1 and GH levels in dogs. Ibutamoren mesylate results in no significant increase in CSFIGF-1 or GH levels on days 7 or 15 of the study 1. Pretreating mice with GH blocks activation of theseneurons by Ibutamoren mesylate (50 g, i.p.). In the knockout mice, both G

6、H and octreotide fail to inhibitIbutamoren mesylate activation of arcuate neurons 2. Chronic oral administration of MK-0677 is associatedwith significant increases in GH and IGF-I levels that are maintained for the duration of the treatment. TheGH profile following MK-0677 administration consists of

7、 episodic increases above control 3. MK-0677significantly increases peak GH concentrations after oral administration. MK-0677 is a potent GHsecretagogue that induces an immediate, large, long lasting increase in GH levels when administered orallyor i.v 4.PROTOCOLAnimal Compounds used are: Ibutamoren

8、 mesylate (50 g), octreotide (100 g), and mGH (30 g). Mice are give anAdministration 2 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:

9、 saline/saline,saline/Ibutamoren mesylate, mGH/saline, mGH/Ibutamoren mesylate saline/saline, saline/Ibutamorenmesylate, mGH/saline, mGH/Ibutamoren mesylate, and the second study of: saline/saline, saline/Ibutamorenmesylate, octreotide/saline, octreotide/Ibutamoren mesylate. Additionally, a number o

10、f mice are injected ipwith hypertonic saline (0.2 mL, 1.5 M) to serve as positive controls for the immunocytochemistry. Ninetyminutes after injection animals are terminally anesthetized with sodium pentobarbitone (60 mg/kg, ip) andperfused transcardially with heparinized saline followed by 4% parafo

11、rmaldehyde in 0.1mol/Lphosphatebuffer (PB, pH 7.4). Brains are then removed and placed in the same solution for 24 h before being storedat 80C until processing. Coronal sections of forebrain (40 M) are cut on a freezing microtome and placedin 0.1mol/LPB containing Triton X-100 (PB-T, pH 7.4). Sectio

12、ns are incubated for 24 h at 4C in Ab-2 Fosantibody (rabbit polyclonal; 1:1000 in 1% normal sheep serum). The antibody-antigen complex is localizedwith a 1-h incubation in biotinylated anti-rabbit Ig, followed by a 1-h incubation in avidin, biotinylatedhorseradish peroxidase. The reaction product is

13、 visualized using a glucose oxidase-diaminobenzidine-nickelmethod, and Fos-like immunoreactivity is visualized as a dense purple-black precipitate restricted to thenucleus. The number of c-fos positive nuclei in the arcuate and periventricular nuclei (six to eight sections permouse) are counted doub

14、le-blind and a group mean calculated (meansem). Statistical analysis is performedby a two-way ANOVA followed by an all pairwise multiple comparison of data with significance taken as P 0.05.MCE has not independently confirmed the accuracy of these methods. They are for reference only.2/3 Master of S

15、mall Molecules 您邊的抑制劑師www.MedChemE戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Drug Test Anal. 2018 Nov;10(11-12):1755-1760. Amino Acids. 2015 Oct;47(10):2237-43.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Prahalada S, et al. Insulin-like growth factor-1 and growth hormone (GH) levels in canine cerebrospin

16、al fluid are unaffected by GH or GHsecretagogue (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. Hicke

17、y GJ, et al. Repeat administration of the GH secretagogue MK-0677 increases and maintains elevated IGF-I levels in beagles. JEndocrinol. 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 otherhormonal respo