Devazepide - CAS 103420-77-5
Catalog number:
103420-77-5
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C25H20N4O2
Molecular Weight:
408.45
COA:
Inquire
Targets:
Cholecystokinin A(CCKA)
Description:
Devazepide is a potent and orally active cholecystokinin A(CCK-A) receptor antagonist with IC50 value of 0.26 nM. It is a derivative of benzodiazepine that displays appetite-stimulant effects. It blocks the anorectic response to CCK-8 and increases food intake in rats. It increases appetite and accelerates gastric emptying. It is used as a potential treatment for a variety of gastrointestinal problems including gastroparesis, dyspepsia and gastric reflux. It was developed by Merck Sharp & Dohme and was terminated in clinic phase 2 trials.
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Purity:
>99 %
Appearance:
Solid powder
Synonyms:
(3S)-1-Methyl-3-[(1H-indol-2-yl)carbonylamino]-5-phenyl-1H-1,4-benzodiazepin-2(3H)-one;L-364718;MK-329;(S)-N-(2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl)indole-2-carboxamide;MK-329;MK329;N-[(3S)-1-methyl-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]-1H-indole-2-carboxamide
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol
Storage:
2-8°C
MSDS:
Inquire
Application:
Devazepide is used as a potential treatment for a variety of gastrointestinal problems including gastroparesis, dyspepsia and gastric reflux.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams to Kilograms
Boiling Point:
758.6±60.0 °C | Condition: Press: 760 Torr
Density:
1.31±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
NFHRQQKPEBFUJK-HSZRJFAPSA-N
InChI:
InChI=1S/C25H20N4O2/c1-29-21-14-8-6-12-18(21)22(16-9-3-2-4-10-16)27-23(25(29)31)28-24(30)20-15-17-11-5-7-13-19(17)26-20/h2-15,23,26H,1H3,(H,28,30)/t23-/m1/s1
Canonical SMILES:
CN1C2=CC=CC=C2C(=NC(C1=O)NC(=O)C3=CC4=CC=CC=C4N3)C5=CC=CC=C5
Current Developer:
Devazepide was developed by Merck Sharp & Dohme and was terminated in clinic phase 2 trials.
1.The cholecystokinin-1 receptor antagonist devazepide increases cholesterol cholelithogenesis in mice.
Wang HH1,2, Portincasa P3, Wang DQ1,2. Eur J Clin Invest. 2016 Feb;46(2):158-69. doi: 10.1111/eci.12580. Epub 2016 Jan 12.
BACKGROUND: A defect in gallbladder contraction function plays a key role in the pathogenesis of gallstones. The cholecystokinin-1 receptor (CCK-1R) antagonists have been extensively investigated for their therapeutic effects on gastrointestinal and metabolic diseases in animal studies and clinical trials. However, it is still unknown whether they have a potential effect on gallstone formation.
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