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CAS No.: 159752-10-0

伊布莫仑甲磺酸盐 Catalog No. CSN17135

Synonyms: MK-677;MK-0677;Crescendo

Ibutamoren mesylate is an agonist of nonpeptide growth hormone secretagogue receptor.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述MK-677 is a potent, orally active growth hormone (GH) secretagogue with EC50 value of 1.3nM for releasing GH from rat pituitary cells in culture. Addition of 10nM MK-677 elicited transient elevations of cytosolic free calcium through the activation of L-type Ca²⁺ channels in rat somatotrophs. MK-677 at concentration of 0.1μM greatly potentiated the effect of GHRH (10nM) on GH release and the accumulation of intracellular cAMP in the pituitary cell assay. Elevation of GH could be observed in dogs after oral doses of MK-677 as low as 0.125mg/kg, without significant effect on plasma levels of aldosterone, luteinizing hormone, thyroxine, and prolactin after oral administration of 1 mg/kg.
动物研究
剂量
Dog: 0.25 mg/kg - 1 mg/kg^[2] (p.o.); Mice: 0.1 mg/kg - 5 mg/kg^[3] (i.p.)

给药途径
p.o., i.p.
临床研究

动物研究
剂量	Dog: 0.25 mg/kg - 1 mg/kg^[2] (p.o.); Mice: 0.1 mg/kg - 5 mg/kg^[3] (i.p.)
给药途径	p.o., i.p.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00074529	Alzheimer's Disease	Phase 2	Completed	-	-
NCT00128115	Hip Fracture	Phase 2	Terminated	-	Germany ... more >> Msd Sharp & Dohme Gmbh Haar, Germany, 85540 Norway MSD (Norge) AS Drammen, Norway, 3011 Spain Merck Sharp & Dohme De Espana, S.A.E. Madrid, Spain, 28027 Sweden Merck Sharp & Dohme (Sweden) AB Sollentuna, Sweden, 192 07 United Kingdom Merch Sharp & Dohme Ltd. Hoddesdon, Hertfordshire, United Kingdom, EN11 9BU Collapse <<
NCT00395291	Chronic Kidney Disease ... more >> End Stage Renal Disease Collapse <<	Not Applicable	Completed	-	United States, Virginia ... more >> University of Virginia Charlottesville, Virginia, United States, 22908 Collapse <<

更多
参考文献

[1] Patchett AA, Nargund RP, et al. Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue. Proc Natl Acad Sci U S A. 1995 Jul 18;92(15):7001-5.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.6006 mL
- 8.0030 mL
- 16.0059 mL
- 5 mM
- 0.3201 mL
- 1.6006 mL
- 3.2012 mL
- 10 mM
- 0.1601 mL
- 0.8003 mL
- 1.6006 mL

技术信息

CAS号

159752-10-0

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H40N4O8S2

运输

蓝冰

分子量

624.77

别名

MK-677;MK-0677;Crescendo;Ibutamoren (mesylate);L-163,191;Ibutamoren;L-163191;伊布莫仑甲磺酸盐

溶解度

DMSO	98.0 mg/mL (156.9 mM)
Ethanol	100.0 mg/mL (160.1 mM)

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT00074529	Alzheimer's Disease	Phase 2	Completed	-	-
NCT00128115	Hip Fracture	Phase 2	Terminated	-	Germany ... more >> Msd Sharp & Dohme Gmbh Haar, Germany, 85540 Norway MSD (Norge) AS Drammen, Norway, 3011 Spain Merck Sharp & Dohme De Espana, S.A.E. Madrid, Spain, 28027 Sweden Merck Sharp & Dohme (Sweden) AB Sollentuna, Sweden, 192 07 United Kingdom Merch Sharp & Dohme Ltd. Hoddesdon, Hertfordshire, United Kingdom, EN11 9BU Collapse <<
NCT00395291	Chronic Kidney Disease ... more >> End Stage Renal Disease Collapse <<	Not Applicable	Completed	-	United States, Virginia ... more >> University of Virginia Charlottesville, Virginia, United States, 22908 Collapse <<
NCT00474279	Aging	Phase 1 Phase 2	Completed	-	United States, Virginia ... more >> University of Virginia Charlottesville, Virginia, United States, 22908 Collapse <<
NCT00395291	-	-	Completed	-	-
NCT00116129	Fibromyalgia	Phase 2	Completed	-	United States, Oregon ... more >> Oregon Health & Science University Portland, Oregon, United States, 97239 Collapse <<
NCT01343641	Chronic Kidney Disease ... more >> Kidney Disease Collapse <<	Phase 2	Withdrawn(Could not obtain dru... more >>g supply from manufacturer) Collapse <<	-	United States, Virginia ... more >> University of Virginia Charlottesville, Virginia, United States, 22908 Collapse <<

伊布莫仑甲磺酸盐 Catalog No. CSN17135

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