A-65186

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

MedKoo CAT#: 571164

CAS#: 119295-94-2

Description: A 65186 is a Type A Cholecystokinin (CCK) receptor antagonist. Cholecystokinin (CCK) is a peptide hormone which is found both in the gastrointestinal tract throughout the human small intestine and in the enteric and central nervous system. It has a potential therapeutic role as an appetite suppressor.


Chemical Structure

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A-65186
CAS# 119295-94-2

Theoretical Analysis

MedKoo Cat#: 571164
Name: A-65186
CAS#: 119295-94-2
Chemical Formula: C25H35N3O4
Exact Mass: 441.2628
Molecular Weight: 441.57
Elemental Analysis: C, 68.00; H, 7.99; N, 9.52; O, 14.49

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: A 65186; A-65186; A65186

IUPAC/Chemical Name: Pentanoic acid, 5-(dipentylamino)-5-oxo-4-((3-quinolinylcarbonyl)amino)-, (R)-

InChi Key: LVIZXRRZYVZZEN-JOCHJYFZSA-N

InChi Code: InChI=1S/C25H35N3O4/c1-3-5-9-15-28(16-10-6-4-2)25(32)22(13-14-23(29)30)27-24(31)20-17-19-11-7-8-12-21(19)26-18-20/h7-8,11-12,17-18,22H,3-6,9-10,13-16H2,1-2H3,(H,27,31)(H,29,30)/t22-/m1/s1

SMILES Code: O=C(O)CC[C@@H](NC(C1=CC2=CC=CC=C2N=C1)=O)C(N(CCCCC)CCCCC)=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

Preparing Stock Solutions

The following data is based on the product molecular weight 441.57 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

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1: Woltman TA, Hulce M, Reidelberger RD. Relative blood-brain barrier permeabilities of the cholecystokinin receptor antagonists devazepide and A-65186 in rats. J Pharm Pharmacol. 1999 Aug;51(8):917-20. PubMed PMID: 10504030.

2: Asin KE, Bednarz L, Nikkel AL, Gore PA Jr, Nadzan AM. A-71623, a selective CCK-A receptor agonist, suppresses food intake in the mouse, dog, and monkey. Pharmacol Biochem Behav. 1992 Aug;42(4):699-704. PubMed PMID: 1513850.

3: Britton DR, Yahiro L, Cullen MJ, Kerwin JF Jr, Kopecka H, Nadzan AM. Centrally administered CCK-8 suppresses activity in mice by a "peripheral-type" CCK receptor. Pharmacol Biochem Behav. 1989 Dec;34(4):779-83. PubMed PMID: 2623030.

4: Peter SA, D'Amato M, Beglinger C. CCK1 antagonists: are they ready for clinical use? Dig Dis. 2006;24(1-2):70-82. Review. PubMed PMID: 16699265.

5: Shigeri Y, Shinohara S, Murata S, Fujimoto M, Kawasaki K. Expression of two different cholecystokinin receptors in Xenopus oocytes injected with mRNA from rabbit pancreas and rat hippocampus. Jpn J Pharmacol. 1996 Sep;72(1):9-15. PubMed PMID: 8902594.

6: Parrott RF. Central effects of CCK ligands in pigs making operant responses for food. Pharmacol Biochem Behav. 1994 Nov;49(3):463-9. PubMed PMID: 7862695.

7: Reidelberger RD, Hernandez J, Fritzsch B, Hulce M. Abdominal vagal mediation of the satiety effects of CCK in rats. Am J Physiol Regul Integr Comp Physiol. 2004 Jun;286(6):R1005-12. Epub 2003 Dec 30. PubMed PMID: 14701717.

8: Reidelberger RD, Castellanos DA, Hulce M. Effects of peripheral CCK receptor blockade on food intake in rats. Am J Physiol Regul Integr Comp Physiol. 2003 Aug;285(2):R429-37. Epub 2003 May 8. PubMed PMID: 12738611.

9: Reidelberger RD, Kelsey L, Heimann D, Hulce M. Effects of peripheral CCK receptor blockade on gastric emptying in rats. Am J Physiol Regul Integr Comp Physiol. 2003 Jan;284(1):R66-75. Epub 2002 Oct 3. PubMed PMID: 12388446.

10: van Westerloo DJ, Helmerhorst HJ. A little fat every day keeps the doctor away*. Crit Care Med. 2013 Nov;41(11):2662-3. doi: 10.1097/CCM.0b013e3182963e7c. PubMed PMID: 24162686.

11: Lubbers T, de Haan JJ, Luyer MD, Verbaeys I, Hadfoune M, Dejong CH, Buurman WA, Greve JW. Cholecystokinin/Cholecystokinin-1 receptor-mediated peripheral activation of the afferent vagus by enteral nutrients attenuates inflammation in rats. Ann Surg. 2010 Aug;252(2):376-82. doi: 10.1097/SLA.0b013e3181dae411. PubMed PMID: 20585240.

12: de Haan JJ, Windsant IV, Lubbers T, Hanssen SJ, Hadfoune M, Prinzen FW, Greve JW, Buurman WA. Prevention of hemolysis-induced organ damage by nutritional activation of the vagal anti-inflammatory reflex*. Crit Care Med. 2013 Nov;41(11):e361-7. doi: 10.1097/CCM.0b013e31828e9262. PubMed PMID: 24105450.

13: Kerwin JF Jr, Wagenaar F, Kopecka H, Lin CW, Miller T, Witte D, Stashko M, Nadzan AM. Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors. J Med Chem. 1991 Dec;34(12):3350-9. PubMed PMID: 1766000.

14: Ebenezer IS. The effects of a peripherally acting cholecystokinin1 receptor antagonist on food intake in rats: implications for the cholecystokinin-satiety hypothesis. Eur J Pharmacol. 2003 Feb 14;461(2-3):113-8. PubMed PMID: 12586206.

15: Ebenezer IS, Parrott RF. A70104 and food intake in pigs: implication for the CCK 'satiety' hypothesis. Neuroreport. 1993 May;4(5):495-8. PubMed PMID: 8513125.

16: Reidelberger RD, Heimann D, Kelsey L, Hulce M. Effects of peripheral CCK receptor blockade on feeding responses to duodenal nutrient infusions in rats. Am J Physiol Regul Integr Comp Physiol. 2003 Feb;284(2):R389-98. Epub 2002 Oct 31. PubMed PMID: 12414437.