L-365260
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 559120

CAS#: 118101-09-0

Description: L-365260 is a selective cholecystokinin receptor 2 (CCK2) antagonist (IC50 values are 2 and 280 nM at CCK2 and CCK1 receptors respectively).

Chemical Structure

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L-365260
CAS# 118101-09-0
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 559120
Name: L-365260
CAS#: 118101-09-0
Chemical Formula: C24H22N4O2
Exact Mass: 398.17
Molecular Weight: 398.466
Elemental Analysis: C, 72.34; H, 5.57; N, 14.06; O, 8.03

Price and Availability

Size Price Availability Quantity
10mg USD 450 2 Weeks
25mg USD 850 2 Weeks
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Synonym: L-365260; L 365260; L365260.

IUPAC/Chemical Name: N-[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)urea

InChi Key: KDFQABSFVYLGPM-QFIPXVFZSA-N

InChi Code: InChI=1S/C24H22N4O2/c1-16-9-8-12-18(15-16)25-24(30)27-22-23(29)28(2)20-14-7-6-13-19(20)21(26-22)17-10-4-3-5-11-17/h3-15,22H,1-2H3,(H2,25,27,30)/t22-/m0/s1

SMILES Code: O=C(NC1=CC=CC(C)=C1)N[C@H]2C(N(C)C3=CC=CC=C3C(C4=CC=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

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:

Product Data:
Product Data
Instruction:
View handling instruction
Biological target: L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively.
In vitro activity: The excitatory actions of CCK8S were mimicked by the selective CCK(B) receptor agonist CCK4, and attenuated by the selective CCK(B) receptor antagonist L365260, indicating a role for CCK(B) receptors. Reference: Brain Res. 2009 Jul 28;1282:10-9. https://pubmed.ncbi.nlm.nih.gov/19497313/
In vivo activity: Rats injected twice daily for 6 days with incremental doses of morphine became tolerant to the analgesic effects of the drug. Twice daily injections of either 8 mg/kg L-365,031 or 0.2 mg/kg L-365,260 prevented the development of tolerance to morphine analgesia. Reference: Eur J Pharmacol. 1990 Jan 25;176(1):35-44. https://pubmed.ncbi.nlm.nih.gov/2311658/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.9 100.00
Ethanol 39.9 100.00

Preparing Stock Solutions

The following data is based on the product molecular weight 398.47 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.

Recalculate based on batch purity %
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: 1. Chung L, Moore SD, Cox CL. Cholecystokinin action on layer 6b neurons in somatosensory cortex. Brain Res. 2009 Jul 28;1282:10-9. doi: 10.1016/j.brainres.2009.05.061. Epub 2009 Jun 2. PMID: 19497313; PMCID: PMC2738607. 2. Dourish CT, O'Neill MF, Coughlan J, Kitchener SJ, Hawley D, Iversen SD. The selective CCK-B receptor antagonist L-365,260 enhances morphine analgesia and prevents morphine tolerance in the rat. Eur J Pharmacol. 1990 Jan 25;176(1):35-44. doi: 10.1016/0014-2999(90)90129-t. PMID: 2311658. 3. Lotti VJ, Chang RS. A new potent and selective non-peptide gastrin antagonist and brain cholecystokinin receptor (CCK-B) ligand: L-365,260. Eur J Pharmacol. 1989 Mar 21;162(2):273-80. doi: 10.1016/0014-2999(89)90290-2. PMID: 2721567.
In vitro protocol: 1. Chung L, Moore SD, Cox CL. Cholecystokinin action on layer 6b neurons in somatosensory cortex. Brain Res. 2009 Jul 28;1282:10-9. doi: 10.1016/j.brainres.2009.05.061. Epub 2009 Jun 2. PMID: 19497313; PMCID: PMC2738607.
In vivo protocol: 1. Dourish CT, O'Neill MF, Coughlan J, Kitchener SJ, Hawley D, Iversen SD. The selective CCK-B receptor antagonist L-365,260 enhances morphine analgesia and prevents morphine tolerance in the rat. Eur J Pharmacol. 1990 Jan 25;176(1):35-44. doi: 10.1016/0014-2999(90)90129-t. PMID: 2311658. 2. Lotti VJ, Chang RS. A new potent and selective non-peptide gastrin antagonist and brain cholecystokinin receptor (CCK-B) ligand: L-365,260. Eur J Pharmacol. 1989 Mar 21;162(2):273-80. doi: 10.1016/0014-2999(89)90290-2. PMID: 2721567.

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1: Matto V, Harro J, Allikmets L. The effects of cholecystokinin A and B receptor antagonists, devazepide and L 365260, on citalopram-induced decrease of exploratory behaviour in rat. J Physiol Pharmacol. 1996 Dec;47(4):661-9. PubMed PMID: 9116333.