YM-022 | CAS#145084-28-2 | CCK-BR Antagonist

MedKoo Cat#: 532982 | Name: YM-022

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

YM-022 is a potent and selective antagonist of the cholecystokinin type B (CCK-B) receptor, which plays a role in gastric acid secretion and neurological functions. It exhibits high bioactivity in vitro and in vivo, effectively inhibiting CCK-B receptor-mediated signaling with potential applications in gastrointestinal disorders and psychiatric conditions. By blocking CCK-B receptors, YM-022 may modulate gastric acid secretion, anxiety-related behaviors, and pain perception, making it a candidate for therapeutic development in these areas.

Chemical Structure

YM-022

CAS#145084-28-2

Theoretical Analysis

MedKoo Cat#: 532982

Name: YM-022

CAS#: 145084-28-2

Chemical Formula: C32H28N4O3

Exact Mass: 516.2161

Molecular Weight: 516.60

Elemental Analysis: C, 74.40; H, 5.46; N, 10.85; O, 9.29

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 350.00
10mg	USD 560.00

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Synonym

YM-022; YM 022; YM022.

IUPAC/Chemical Name

3-(3-methylphenyl)-1-[(3R)-1-[2-(2-methylphenyl)-2-oxoethyl]-2-oxo-5-phenyl-3H-1,4-benzodiazepin-3-yl]urea

InChi Key

YCXFHPUBGMMWJQ-PMERELPUSA-N

InChi Code

InChI=1S/C32H28N4O3/c1-21-11-10-15-24(19-21)33-32(39)35-30-31(38)36(20-28(37)25-16-7-6-12-22(25)2)27-18-9-8-17-26(27)29(34-30)23-13-4-3-5-14-23/h3-19,30H,20H2,1-2H3,(H2,33,35,39)/t30-/m0/s1

SMILES Code

O=C(NC1=CC=CC(C)=C1)N[C@H]2C(N(CC(C3=CC=CC=C3C)=O)C4=CC=CC=C4C(C5=CC=CC=C5)=N2)=O

Appearance

White to light brown 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

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 516.60 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

1: Keringer P, Furedi N, Gaszner B, Miko A, Pakai E, Fekete K, Olah E, Kelava L, Romanovsky AA, Rumbus Z, Garami A. The hyperthermic effect of central cholecystokinin is mediated by the cyclooxygenase-2 pathway. Am J Physiol Endocrinol Metab. 2022 Jan 1;322(1):E10-E23. doi: 10.1152/ajpendo.00223.2021. Epub 2021 Nov 15. PMID: 34779255. 2: Duan LL, Qiu XY, Wei SQ, Su HY, Bai FR, Traub RJ, Zhou Q, Cao DY. Spinal CCK contributes to somatic hyperalgesia induced by orofacial inflammation combined with stress in adult female rats. Eur J Pharmacol. 2021 Dec 15;913:174619. doi: 10.1016/j.ejphar.2021.174619. Epub 2021 Nov 5. PMID: 34748768; PMCID: PMC9016487. 3: Yano K, Kimura M, Watanabe Y, Ogihara T. Rapid Increase of Gastrointestinal P-Glycoprotein Functional Activity in Response to Etoposide Stimulation. Biol Pharm Bull. 2021;44(5):701-706. doi: 10.1248/bpb.b21-00007. PMID: 33952826. 4: Tang WZ, Cui ZJ. Permanent Photodynamic Activation of the Cholecystokinin 2 Receptor. Biomolecules. 2020 Feb 4;10(2):236. doi: 10.3390/biom10020236. PMID: 32033232; PMCID: PMC7072308. 5: Lloyd KA, Parsons BN, Burkitt MD, Moore AR, Papoutsopoulou S, Boyce M, Duckworth CA, Exarchou K, Howes N, Rainbow L, Fang Y, Oxvig C, Dodd S, Varro A, Hall N, Pritchard DM. Netazepide Inhibits Expression of Pappalysin 2 in Type 1 Gastric Neuroendocrine Tumors. Cell Mol Gastroenterol Hepatol. 2020;10(1):113-132. doi: 10.1016/j.jcmgh.2020.01.010. Epub 2020 Jan 28. PMID: 32004755; PMCID: PMC7215182. 6: Sundaresan S, Kang AJ, Hayes MM, Choi EK, Merchant JL. Deletion of Men1 and somatostatin induces hypergastrinemia and gastric carcinoids. Gut. 2017 Jun;66(6):1012-1021. doi: 10.1136/gutjnl-2015-310928. Epub 2016 Feb 9. Erratum in: Gut. 2017 Nov;66(11):2012. doi: 10.1136/gutjnl-2015-310928corr1. PMID: 26860771; PMCID: PMC4980289. 7: Goswami C, Shimada Y, Yoshimura M, Mondal A, Oda S, Tanaka T, Sakai T, Sakata I. Motilin Stimulates Gastric Acid Secretion in Coordination with Ghrelin in Suncus murinus. PLoS One. 2015 Jun 26;10(6):e0131554. doi: 10.1371/journal.pone.0131554. PMID: 26115342; PMCID: PMC4482737. 8: Huang Y, Yoon K, Ko H, Jiao S, Ito W, Wu JY, Yung WH, Lu B, Morozov A. 5-HT3a Receptors Modulate Hippocampal Gamma Oscillations by Regulating Synchrony of Parvalbumin-Positive Interneurons. Cereb Cortex. 2016 Feb;26(2):576-85. doi: 10.1093/cercor/bhu209. Epub 2014 Sep 21. PMID: 25246509; PMCID: PMC4712794. 9: Wang R, King T, De Felice M, Guo W, Ossipov MH, Porreca F. Descending facilitation maintains long-term spontaneous neuropathic pain. J Pain. 2013 Aug;14(8):845-53. doi: 10.1016/j.jpain.2013.02.011. Epub 2013 Apr 19. PMID: 23602267; PMCID: PMC4028636. 10: Wagner KM, Roeder Z, Desrochers K, Buhler AV, Heinricher MM, Cleary DR. The dorsomedial hypothalamus mediates stress-induced hyperalgesia and is the source of the pronociceptive peptide cholecystokinin in the rostral ventromedial medulla. Neuroscience. 2013 May 15;238:29-38. doi: 10.1016/j.neuroscience.2013.02.009. Epub 2013 Feb 13. PMID: 23415792; PMCID: PMC3638803. 11: Lee SY, Földy C, Szabadics J, Soltesz I. Cell-type-specific CCK2 receptor signaling underlies the cholecystokinin-mediated selective excitation of hippocampal parvalbumin-positive fast-spiking basket cells. J Neurosci. 2011 Jul 27;31(30):10993-1002. doi: 10.1523/JNEUROSCI.1970-11.2011. PMID: 21795548; PMCID: PMC3158608. 12: Chen P, Lingen M, Sonis ST, Walsh-Reitz MM, Toback FG. Role of AMP-18 in oral mucositis. Oral Oncol. 2011 Sep;47(9):831-9. doi: 10.1016/j.oraloncology.2011.06.012. Epub 2011 Jul 6. PMID: 21737340; PMCID: PMC3164219. 13: Lee CW, Rickman B, Rogers AB, Muthupalani S, Takaishi S, Yang P, Wang TC, Fox JG. Combination of sulindac and antimicrobial eradication of Helicobacter pylori prevents progression of gastric cancer in hypergastrinemic INS-GAS mice. Cancer Res. 2009 Oct 15;69(20):8166-74. doi: 10.1158/0008-5472.CAN-08-3856. Epub 2009 Oct 13. PMID: 19826057; PMCID: PMC2766772. 14: Paillasse MR, de Medina P, Amouroux G, Mhamdi L, Poirot M, Silvente-Poirot S. Signaling through cholesterol esterification: a new pathway for the cholecystokinin 2 receptor involved in cell growth and invasion. J Lipid Res. 2009 Nov;50(11):2203-11. doi: 10.1194/jlr.M800668-JLR200. Epub 2009 Jun 5. PMID: 19502590; PMCID: PMC2759826. 15: Tsutsumi E, Kanai S, Ohta M, Suwa Y, Miyasaka K. Stimulatory effect of N-methyltyramine, a congener of beer, on pancreatic secretion in conscious rats. Alcohol Clin Exp Res. 2010 Feb;34 Suppl 1:S14-7. doi: 10.1111/j.1530-0277.2009.00893.x. Epub 2009 Mar 6. PMID: 19298333. 16: Imatake K, Matsui T, Moriyama M. The effect and mechanism of action of capsaicin on gastric acid output. J Gastroenterol. 2009;44(5):396-404. doi: 10.1007/s00535-009-0018-x. Epub 2009 Mar 19. PMID: 19296048. 17: Przemeck SM, Varro A, Berry D, Steele I, Wang TC, Dockray GJ, Pritchard DM. Hypergastrinemia increases gastric epithelial susceptibility to apoptosis. Regul Pept. 2008 Feb 7;146(1-3):147-56. doi: 10.1016/j.regpep.2007.09.002. Epub 2007 Sep 7. PMID: 17900712. 18: Földy C, Lee SY, Szabadics J, Neu A, Soltesz I. Cell type-specific gating of perisomatic inhibition by cholecystokinin. Nat Neurosci. 2007 Sep;10(9):1128-30. doi: 10.1038/nn1952. Epub 2007 Aug 5. PMID: 17676058. 19: Zhao CM, Håkanson R, Chen D. Secretory organelles in ECL cells: effects of pharmacological blockade of the gastrin/CCK2 receptor versus its elimination by gene targeting. Inflammopharmacology. 2005;13(1-3):75-82. doi: 10.1163/156856005774423818. PMID: 16259729. 20: Chao C, Ives KL, Goluszko E, Kolokoltsov AA, Davey RA, Townsend CM Jr, Hellmich MR. SRC regulates constitutive internalization and rapid resensitization of a cholecystokinin 2 receptor splice variant. J Biol Chem. 2005 Sep 30;280(39):33368-73. doi: 10.1074/jbc.M506337200. Epub 2005 Aug 3. PMID: 16079138.

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