WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H319840
CAS#: 155488-25-8
Description: Netazepide, also known as YF476 and Sograzepide, is a gastrin/CCK2 receptor antagonist,. Netazepide (YF476) prevents oxyntic mucosal inflammation induced by Helicobacter pylori infection in Mongolian gerbils.
Hodoodo Cat#: H319840
Name: Netazepide
CAS#: 155488-25-8
Chemical Formula: C28H30N6O3
Exact Mass: 498.24
Molecular Weight: 498.587
Elemental Analysis: C, 67.45; H, 6.07; N, 16.86; O, 9.63
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Synonym: YF476; YF-476; YF 476; Netazepide; Sograzepide
IUPAC/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
InChi Key: YDZYKNJZCVIKPP-VWLOTQADSA-N
InChi Code: InChI=1S/C28H30N6O3/c1-28(2,3)23(35)17-34-22-14-6-5-12-20(22)24(21-13-7-8-15-30-21)32-25(26(34)36)33-27(37)31-19-11-9-10-18(16-19)29-4/h5-16,25,29H,17H2,1-4H3,(H2,31,33,37)/t25-/m0/s1
SMILES Code: O=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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 498.59 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Boyce M, Dowen S, Turnbull G, van den Berg F, Zhao CM, Chen D, Black J. 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. doi: 10.1111/bcp.12534. PubMed PMID: 25335860; PubMed Central PMCID: PMC4415711.
2: Moore AR, Boyce M, Steele IA, Campbell F, Varro A, Pritchard DM. Netazepide, a gastrin receptor antagonist, normalises tumour biomarkers and causes regression of type 1 gastric neuroendocrine tumours in a nonrandomised trial of patients with chronic atrophic gastritis. PLoS One. 2013 Oct 1;8(10):e76462. doi: 10.1371/journal.pone.0076462. eCollection 2013. PubMed PMID: 24098507; PubMed Central PMCID: PMC3788129.
3: Sørdal Ø, Waldum H, Nordrum IS, Boyce M, Bergh K, Munkvold B, Qvigstad G. The gastrin receptor antagonist netazepide (YF476) prevents oxyntic mucosal inflammation induced by Helicobacter pylori infection in Mongolian gerbils. Helicobacter. 2013 Dec;18(6):397-405. doi: 10.1111/hel.12066. Epub 2013 Jul 19. PubMed PMID: 23865485.
4: Boyce M, Warrington S, Black J. Netazepide, a gastrin/CCK2 receptor antagonist, causes dose-dependent, persistent inhibition of the responses to pentagastrin in healthy subjects. Br J Clin Pharmacol. 2013 Nov;76(5):689-98. doi: 10.1111/bcp.12099. PubMed PMID: 23432534; PubMed Central PMCID: PMC3853528.
5: Boyce M, Warrington S. Effect of repeated doses of netazepide, a gastrin receptor antagonist, omeprazole and placebo on 24 h gastric acidity and gastrin in healthy subjects. Br J Clin Pharmacol. 2013 Nov;76(5):680-8. doi: 10.1111/bcp.12095. PubMed PMID: 23432415; PubMed Central PMCID: PMC3853527.
6: Fossmark R, Sørdal Ø, Jianu CS, Qvigstad G, Nordrum IS, Boyce M, Waldum HL. Treatment of gastric carcinoids type 1 with the gastrin receptor antagonist netazepide (YF476) results in regression of tumours and normalisation of serum chromogranin A. Aliment Pharmacol Ther. 2012 Dec;36(11-12):1067-75. doi: 10.1111/apt.12090. Epub 2012 Oct 16. PubMed PMID: 23072686.
7: Metz DC. Commentary: netazepide for gastric acid suppression--another kid on the block? Aliment Pharmacol Ther. 2012 Aug;36(3):294-5. doi: 10.1111/j.1365-2036.2012.05183.x. PubMed PMID: 22747455.
8: Boyce M, David O, Darwin K, Mitchell T, Johnston A, Warrington S. 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. Aliment Pharmacol Ther. 2012 Jul;36(2):181-9. doi: 10.1111/j.1365-2036.2012.05143.x. Epub 2012 May 20. PubMed PMID: 22607579.
