L-365,260A non-peptide competitive CCK-BR antagonist

L-365,260 (CAS 118101-09-0)

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Synonym: N-[(3R)-2,3-dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N′-(3-methylphenyl)-urea
Application: A non-peptide competitive CCK-BR antagonist
CAS Number: 118101-09-0
Purity: ≥99%
Molecular Weight: 398.46
Molecular Formula: C24H22N4O2
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* Refer to Certificate of Analysis for lot specific data (including water content).
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L-365,260 is a non-peptide competitive CCK-BR (CCK2; CCK-B; cholecystokinin 2) receptor antagonist reported to inhibit the cyclic AMP-dependent protein kinase pathway. CCK is a neuroendocrine peptide described to play an important role in cell growth, cell proliferation, and other biological functions. Lung cancer cell studies show that L-365,260 blocks the elevated levels of cytosolic Ca2+ induced by CCK-8, and inhibits CCK-8 binding to SCLC cells and the cell proliferation of NCI-H209 cells. Other CCKB inhibitors include CI 988 (sc-205244).


References

1. Lotti, V.J. and Chang, R.S. 1989. Eur. J. Pharmacol. 162: 273-280. PMID: 2721567
2. Oiry, C., et al. 1999. Br. J. Pharmacol. 127: 259-267. PMID: 10369481
3. Moody, T.W. and Jensen, R.T. 2001. J. Pharmacol. Exp. Ther. 299: 1154-1160. PMID: 11714907
4. McCleane, G.J. 2003. Neurosci. Lett. 338: 151-154. PMID: 12566175
5. Carrillo, J., et al. 2009. Anticancer Drugs. 20: 527-533. PMID: 19407653
6. Chung, L., et al. 2009. Brain Res. 1282 : 10-19. PMID: 19497313

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and ethanol (100 mM).
Storage :
Desiccate at -20° C
Melting Point :
266.72° C (Predicted)
Boiling Point :
~611.5° C at 760 mmHg (Predicted)
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.65 (Predicted)
Optical Activity :
α20D +78°, c = 1.1 in chloroform
IC50 :
CCK-BR: IC50 = 1.1 nM (human); CCK2 receptors: IC50 = 2 nM; CCK-AR: IC50 = 2 nM (Cavia porcellus); CCK-BR: IC50 = 2 nM (mouse); CCK1 receptors: IC50 = 280 nM
Ki Data :
CCK-BR: Ki= 1.8 nM (human)
pK Values :
pKa: 11.66 (Predicted), pKb: 3.52 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
Transport :
UN 2811, Class 6.1, Packing group III
PubChem CID :
5311201
MDL Number :
MFCD00869756
SMILES :
CC1=CC(=CC=C1)NC(=O)N[C@H]2C(=O)N(C3=CC=CC=C3C(=N2)C4=CC=CC=C4)C

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Certificate of Analysis

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