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155488-25-8,MFCD00937935
Catalog No.:AA00ADVN

155488-25-8 | Sograzepide

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Purity
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5mg
98%
1 week  
$447.00   $313.00
- +
10mg
98%
1 week  
$765.00   $535.00
- +
50mg
98%
1 week  
$2,273.00   $1,591.00
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100mg
98%
1 week  
$3,384.00   $2,369.00
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  • Technical Information
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  • Literature
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA00ADVN
Chemical Name:
Sograzepide
CAS Number:
155488-25-8
Molecular Formula:
C28H30N6O3
Molecular Weight:
498.5762
MDL Number:
MFCD00937935
SMILES:
CNc1cccc(c1)NC(=O)N[C@@H]1N=C(c2ccccn2)c2c(N(C1=O)CC(=O)C(C)(C)C)cccc2
Properties
Computed Properties
 
Complexity:
869  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
1  
Heavy Atom Count:
37  
Hydrogen Bond Acceptor Count:
6  
Hydrogen Bond Donor Count:
3  
Rotatable Bond Count:
7  
XLogP3:
3.8  

Literature

Title: Regulated endocrine-specific protein 18 (RESP18) is localized to and regulated in A-like cells and G-cells in rat stomach.

Journal: Regulatory peptides 20120820

Title: Single oral doses of netazepide (YF476), a gastrin receptor antagonist, cause dose-dependent, sustained increases in gastric pH compared with placebo and ranitidine in healthy subjects.

Journal: Alimentary pharmacology & therapeutics 20120701

Title: JNJ-26070109 [(R)4-bromo-N-[1-(2,4-difluoro-phenyl)-ethyl]-2-(quinoxaline-5-sulfonylamino)-benzamide]: a novel, potent, and selective cholecystokinin 2 receptor antagonist with good oral bioavailability.

Journal: The Journal of pharmacology and experimental therapeutics 20110701

Title: The CCK(2) receptor antagonist, YF476, inhibits Mastomys ECL cell hyperplasia and gastric carcinoid tumor development.

Journal: Regulatory peptides 20100608

Title: Reflections on some pilot trials of gastrin receptor blockade in pancreatic cancer.

Journal: European journal of cancer (Oxford, England : 1990) 20090201

Title: Achiral, selective CCK2 receptor antagonists based on a 1,3,5-benzotriazepine-2,4-dione template.

Journal: Bioorganic & medicinal chemistry 20080315

Title: A comparison of the effects of gastrin, somatostatin and dopamine receptor ligands on rat gastric enterochromaffin-like cell secretion and proliferation.

Journal: Regulatory peptides 20071004

Title: Optimization of 1,3,4-benzotriazepine-based CCK(2) antagonists to obtain potent, orally active inhibitors of gastrin-mediated gastric acid secretion.

Journal: Journal of medicinal chemistry 20070628

Title: Gastrin regulates the TFF2 promoter through gastrin-responsive cis-acting elements and multiple signaling pathways.

Journal: American journal of physiology. Gastrointestinal and liver physiology 20070601

Title: Novel, achiral 1,3,4-benzotriazepine analogues of 1,4-benzodiazepine-based CCK(2) antagonists that display high selectivity over CCK(1) receptors.

Journal: Journal of medicinal chemistry 20060406

Title: Gastrin increases murine intestinal crypt regeneration following injury.

Journal: Gastroenterology 20060401

Title: Synergistic inhibitory effects of gastrin and histamine receptor antagonists on Helicobacter-induced gastric cancer.

Journal: Gastroenterology 20050601

Title: Secretory organelles in ECL cells: effects of pharmacological blockade of the gastrin/CCK2 receptor versus its elimination by gene targeting.

Journal: Inflammopharmacology 20050101

Title: CCK-B receptor antagonist YF476 inhibits pancreatic enzyme secretion at a duodenal level in pigs.

Journal: Scandinavian journal of gastroenterology 20040901

Title: Validation of a liquid chromatographic-tandem mass spectrometric method for the measurement of (R)-1-[2,3-dihydro-2-oxo-1-pivaloylmethyl-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl]-3-(3-methylaminophenyl)urea (YF476) in human plasma.

Journal: Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20020605

Title: Pharmacological analysis of CCK(2) receptor ligands using COS-7 and SK-N-MC cells, expressing the human CCK(2) receptor.

Journal: Regulatory peptides 20020115

Title: Gastric acid secretion in L-histidine decarboxylase-deficient mice.

Journal: Gastroenterology 20020101

Title: Effects of CCK2 receptor blockade on growth parameters in gastrointestinal tract and pancreas in rats.

Journal: Pharmacology & toxicology 20011001

Title: Mobilization of rat stomach ECL-cell histamine in response to short- or long-term treatment with omeprazole and/or YF 476 studied by gastric submucosal microdialysis in conscious rats.

Journal: British journal of pharmacology 20010501

Title: Carbon-11 labelled cholecystokininB antagonists: radiosynthesis and evaluation in rats.

Journal: Life sciences 20010202

Title: YF476 is a new potent and selective gastrin/cholecystokinin-B receptor antagonist in vitro and in vivo.

Journal: Alimentary pharmacology & therapeutics 19970201

Title: (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.

Journal: Journal of medicinal chemistry 19970131

Title: Boyce M, et al. Effect of netazepide, a gastrin/CCK2 receptor antagonist, on gastric acid secretion and rabeprazole-induced hypergastrinaemia in healthy subjects. Br J Clin Pharmacol. 2015 May;79(5):744-55.

Title: Takinami Y, et al. YF476 is a new potent and selective gastrin/cholecystokinin-B receptor antagonist in vitro and in vivo.Aliment Pharmacol Ther. 1997 Feb;11(1):113-20.

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