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SML0220

Sigma-Aldrich

YM 022

≥98% (HPLC)

Synonyme(s) :

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

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About This Item

Formule empirique (notation de Hill):
C32H28N4O3
Numéro CAS:
145084-28-2
Poids moléculaire :
516.59
Numéro MDL:
MFCD00917023
Code UNSPSC :
12352200
ID de substance PubChem :
329825239
Nomenclature NACRES :
NA.77

Pureté

≥98% (HPLC)

Forme

powder

Activité optique

[α]/D -128 to -140 (c = 1, DCM)

Couleur

white to beige

Solubilité

DMSO: 5 mg/mL (clear solution)

Température de stockage

room temp

Chaîne SMILES 

Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c4ccccc4N(CC(=O)c5ccccc5C)C2=O)c1

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

Clé InChI

YCXFHPUBGMMWJQ-PMERELPUSA-N

Actions biochimiques/physiologiques

YM022 is a very potent, selective antagonist of the gastrin/cholecystokinin (CCK)-B receptor. The Ki value for CCKB is 68 pM vs 63 nM for CCKA. In rats, YM022 inhibits pentagastrin-induced gastric emptying with an ED50 or 7.8 nM/kg.

Caractéristiques et avantages

This compound is featured on the Cholecystokinin and Gastrin Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Pictogrammes

Skull and crossbones
GHS06

Mention d'avertissement

Danger

Mentions de danger

H301

Classification des risques

Acute Tox. 3 Oral

Code de la classe de stockage

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

Certificats d'analyse (COA)

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Consulter la Bibliothèque de documents

M Björkqvist et al.
Pharmacology & toxicology, 89(4), 208-213 (2002-03-08)
Gastrin has a growth-promoting effect on the oxyntic mucosa of the stomach but has been claimed also to affect other parts of the gastrointestinal tract and pancreas. This report describes the effects of the cholecystokinin, (CCK2) receptor antagonists YM022 and
P Norlén et al.
Pharmacology & toxicology, 84(4), 159-164 (1999-05-05)
Gastrin acts via cholecystokinin-B/gastrin receptors to control histamine- and chromogranin A-producing ECL cells, which constitute the quantitatively predominant endocrine cell population in the acid-producing part of the rat stomach. Cholecystokinin-B receptor blockade is known to suppress the activity of ECL
Joseph C Harris et al.
Cancer research, 64(6), 1915-1919 (2004-03-18)
Mechanisms by which premalignant Barrett's metaplasia (BM) progresses to esophageal adenocarcinoma are currently being sought. This study investigated the role played by the polypeptide hormone gastrin, specifically its antiapoptotic effects through activation of protein kinase B/Akt (PKB/Akt). In esophageal cell
Celia Chao et al.
The Journal of biological chemistry, 280(39), 33368-33373 (2005-08-05)
The third intracellular loop domain of G protein-coupled receptors regulates their desensitization, internalization, and resensitization. Colorectal and pancreatic cancers, but not the nonmalignant tissue, express a splice variant of the cholecystokinin 2 receptor (CCK2R) called CCK(2i4sv)R that, because of intron
M Kitano et al.
Regulatory peptides, 86(1-3), 113-123 (2000-02-15)
Rat stomach ECL cells are rich in histamine and chromogranin A-derived peptides, such as pancreastatin. Gastrin causes the parietal cells to secrete acid by flooding them with histamine from the ECL cells. In the past, gastric histamine release has been
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