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Netazepide
CAS No. 155488-25-8
Netazepide( YF476 | YF-476 | Sograzepide )
Catalog No. M12210 CAS No. 155488-25-8
Netazepide (YF476, Sograzepide)?is a potent, selective and orally active gastrin/CCK-2 antagonist with IC50 of 0.1 nM.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 50MG | 1044 | In Stock |
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| 100MG | 1566 | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameNetazepide
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NoteResearch use only, not for human use.
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Brief DescriptionNetazepide (YF476, Sograzepide)?is a potent, selective and orally active gastrin/CCK-2 antagonist with IC50 of 0.1 nM.
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DescriptionNetazepide (YF476, Sograzepide)?is a potent, selective and orally active gastrin/CCK-2 antagonist with IC50 of 0.1 nM; displays >5,000-fold selectivity over CCK-1 receptors; inhibits pentagastrin-induced gastric acid secretion in anesthetized rats (ED50=87 nM/kg), and shows potential for the treatment of gastroesophageal reflux disease (GERD); also inhibits gastric neuroendocrine enterochromaffin-like (ECL) cell hyperplasia and gastric carcinoid tumor development.Gastric Cancer Phase 2 Clinical.
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In Vitro——
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In VivoSograzepide?(Netazepide; YF 476; YM-220) (0.1 μmol/kg; intravenous injection) has an inhibition effect on pentagastrin-induced gastric acid secretion in anethsetized rats with an ED50 of 87?nmol/kg.Sograzepide?(Netazepide; YF 476; YM-220) (intravenous injection; 10 μM/kg) inhibits pentagastrin-induced acid secretion with an ED50 value of 0.0086 μM/kg, but does not affect histamine- and bethanechol-induced acid secretion.Sograzepide (Netazepide; YF 476; YM-220) (intravenous injection; oral administration) in Heidenhain pouch dogs, inhibits pentagastrin-stimulated gastric acid secretion in a dose-dependent manner with ED50 values of 0.018 and 0.020 μM/kg, respectively .
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SynonymsYF476 | YF-476 | Sograzepide
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PathwayGPCR/G Protein
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TargetCholecystokinin Receptor
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RecptorCholecystokinin Receptor
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Research AreaCancer
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IndicationGastric Cancer
Chemical Information
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CAS Number155488-25-8
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Formula Weight498.587
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Molecular FormulaC28H30N6O3
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 100 mg/mL 200.57 mM
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SMILESO=C(NC1=CC=CC(NC)=C1)N[C@H]2C(N(CC(C(C)(C)C)=O)C3=CC=CC=C3C(C4=NC=CC=C4)=N2)=O
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Chemical Name(R)-1-(1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-(pyridin-2-yl)-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-3-(3-(methylamino)phenyl)urea
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Semple G, et al. J Med Chem. 1997 Jan 31;40(3):331-41.
2. Takinami Y, et al. Aliment Pharmacol Ther. 1997 Feb;11(1):113-20.
3. Takemoto Y, et al. Arzneimittelforschung. 1998 Apr;48(4):403-7.
4. Kidd M, et al. Regul Pept. 2010 Jun 8;162(1-3):52-60.
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