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Merck

SML0220

YM 022

≥98% (HPLC)

Sinónimos:

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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Fórmula empírica (notación de Hill):
C32H28N4O3
Número CAS:
145084-28-2
Peso molecular:
516.59
NACRES:
NA.77
PubChem Substance ID:
329825239
UNSPSC Code:
12352200
MDL number:
MFCD00917023

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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 string

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

InChI key

YCXFHPUBGMMWJQ-PMERELPUSA-N

assay

≥98% (HPLC)

form

powder

optical activity

[α]/D +128 to +140 (c = 1, DCM)

color

white to beige

solubility

DMSO: 5 mg/mL (clear solution)

storage temp.

room temp

Quality Level

100

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Este artículo
SML0140SML0844SML2666
YM 022 ≥98% (HPLC)

Sigma-Aldrich

SML0220

YM 022

BV02 ≥98% (HPLC)

Sigma-Aldrich

SML0140

BV02

GNF 5837 ≥98% (HPLC)

Sigma-Aldrich

SML0844

GNF 5837

Diflapolin ≥98% (HPLC)

Sigma-Aldrich

SML2666

Diflapolin

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥98% (HPLC)

form

powder

form

powder

form

powder

form

powder

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

-

storage temp.

room temp

storage temp.

room temp

storage temp.

2-8°C

storage temp.

2-8°C

solubility

DMSO: 5 mg/mL (clear solution)

solubility

DMSO: >5 mg/mL

solubility

DMSO: 5 mg/mL, clear (warmed)

solubility

DMSO: 2 mg/mL, clear

color

white to beige

color

white to off-white

color

yellow to orange

color

white to beige

Biochem/physiol Actions

YM022 is a very potent, selective antagonist of the gastrin/cholecystokinin (CCK)-B receptor.
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.

Features and Benefits

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.

pictograms

Skull and crossbones
GHS06

signalword

Danger

hcodes

H301

Hazard Classifications

Acute Tox. 3 Oral

Clase de almacenamiento

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

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Certificados de análisis (COA)

Lot/Batch Number
0000438064
0000438064
0000426479
0000426479
0000156429

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Kazuhiro Imatake et al.
Journal of gastroenterology, 44(5), 396-404 (2009-03-20)
Capsaicin has beneficial pharmacological properties, such as the ability to improve appetite and digestion. However, capsaicin has been reported to suppress gastric acid output, but to increase secretion; no consensus as to its effects on gastric acid output has been
R Håkanson et al.
Regulatory peptides, 80(1-2), 1-12 (1999-05-11)
Gastrin-recognizing CCK2 receptors are expressed in parietal cells and in so-called ECL cells in the acid-producing part of the stomach. ECL cells are endocrine/paracrine cells that produce and store histamine and chromogranin A (CGA)-derived peptides, such as pancreastatin. The ECL
Salem I Abdalla et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 10(14), 4784-4792 (2004-07-23)
Cyclooxygenase (COX)-2 has been causally implicated in carcinogenesis. The evidence for increased COX-2 in the malignant progression of Barrett's esophagus is contradictory. We hypothesize that COX-2 expression may be causally affected by the gastrin status via the cholecystokinin 2 (CCK(2))
M Beinborn et al.
The Yale journal of biology and medicine, 71(3-4), 337-346 (1999-08-26)
The gastric cholecystokinin-B/gastrin receptor (CCK-BR) is a key regulator of enterochromaffin-like cell function and proliferation. Over the last decade, a number of small non-peptide CCK-BR "antagonists" have been discovered. Here, we demonstrate that some of these non-peptide ligands in fact
S Attoub et al.
Endocrinology, 140(10), 4406-4410 (1999-09-28)
In the present study, we investigated whether cholecystokinin (CCK) or its structurally related peptide gastrin participates in long term regulation of adipocyte leptin secretion. The levels of circulating leptin observed after 2 and 6 h of refeeding in 18-h fast
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