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Sograzepide

Catalog No. T16906   CAS 155488-25-8
Synonyms: YM-220, Netazepide, YF 476

Sograzepide is an effective and highly selective Gastrin/CCK-B antagonist (IC50: 0.1 nM), has an inhibitory effect on Gastrin/CCK-A activity (IC50: 502 nM). Sograzepide replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine, and cloned human Gastrin/CCK-B receptors (Ki: 0.068, 0.62 and 0.19 nM, respectively).

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Sograzepide Chemical Structure
Sograzepide, CAS 155488-25-8
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 893.00
50 mg 6-8 weeks $ 1,160.00
100 mg 6-8 weeks $ 1,740.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Sograzepide is an effective and highly selective Gastrin/CCK-B antagonist (IC50: 0.1 nM), has an inhibitory effect on Gastrin/CCK-A activity (IC50: 502 nM). Sograzepide replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine, and cloned human Gastrin/CCK-B receptors (Ki: 0.068, 0.62 and 0.19 nM, respectively).
Targets&IC50 Gastrin/CCK-A:501 nM, Gastrin/CCK-B:0.1 nM
In vivo Sograzepide (0.1 μmol/kg; intravenous injection) has an inhibition effect on pentagastrin-induced gastric acid secretion in anesthetized rats (ED50: 87?nmol/kg). Sograzepide (intravenous injection; 10 μM/kg) inhibits pentagastrin-induced acid secretion (ED50: 0.0086 μM/kg). Sograzepide (intravenous injection; p.o.) in Heidenhain pouch dogs, inhibits pentagastrin-stimulated gastric acid secretion in a dose-dependent manner (ED50: 0.018 and 0.020 μM/kg, respectively) [1][2].
Synonyms YM-220, Netazepide, YF 476
Molecular Weight 498.58
Formula C28H30N6O3
CAS No. 155488-25-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (200.57 mM)

TargetMolReferences and Literature

1. 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. 2. 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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Keywords

Sograzepide 155488-25-8 Others YM 220 YM-220 Netazepide YF 476 YF476 YM220 YF-476 inhibitor inhibit

 

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