L-365260 | CAS#118101-09-0 |CCK2 antagonist

MedKoo Cat#: 559120 | Name: L-365260

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Description:

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

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

L-365260

CAS#118101-09-0

Theoretical Analysis

MedKoo Cat#: 559120

Name: L-365260

CAS#: 118101-09-0

Chemical Formula: C24H22N4O2

Exact Mass: 398.1743

Molecular Weight: 398.47

Elemental Analysis: C, 72.34; H, 5.57; N, 14.06; O, 8.03

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 450.00	2 Weeks
25mg	USD 850.00	2 Weeks

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Related CAS #

No Data

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/

	Solvent	mg/mL	mM
Solubility
	DMSO	39.9	100.00
	Ethanol	39.9	100.00

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.

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:

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.

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.