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MedKoo Cat#: 513691 | Name: CI-988
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Description:

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

CI-988 is potent and selective CCK2 (CCK-B) receptor antagonist that displays ~ 1600-fold selectivity over CCK1 receptors (IC50 values are 1.7 and 2717 nM for CCK2 and CCK1 respectively).

Chemical Structure

CI-988
CI-988
CAS#130332-27-3

Theoretical Analysis

MedKoo Cat#: 513691

Name: CI-988

CAS#: 130332-27-3

Chemical Formula: C35H42N4O6

Exact Mass: 614.3104

Molecular Weight: 614.74

Elemental Analysis: C, 68.38; H, 6.89; N, 9.11; O, 15.62

Price and Availability

Size Price Availability Quantity
10mg USD 650.00 2 Weeks
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Related CAS #
No Data
Synonym
CI-988; CI 988; CI988; PD 134308; PD134308; PD-134308;
IUPAC/Chemical Name
4-[[(1R)-2-[[(2R)-2-(2-adamantyloxycarbonylamino)-3-(1H-indol-3-yl)-2-methylpropanoyl]amino]-1-phenylethyl]amino]-4-oxobutanoic acid
InChi Key
FVQSSYMRZKLFDR-ZABPBAJSSA-N
InChi Code
InChI=1S/C35H42N4O6/c1-35(18-26-19-36-28-10-6-5-9-27(26)28,39-34(44)45-32-24-14-21-13-22(16-24)17-25(32)15-21)33(43)37-20-29(23-7-3-2-4-8-23)38-30(40)11-12-31(41)42/h2-10,19,21-22,24-25,29,32,36H,11-18,20H2,1H3,(H,37,43)(H,38,40)(H,39,44)(H,41,42)/t21?,22?,24?,25?,29-,32?,35+/m0/s1
SMILES Code
O=C(O)CCC(N[C@H](C1=CC=CC=C1)CNC([C@](C)(NC(OC2C3CC4CC(C3)CC2C4)=O)CC5=CNC6=C5C=CC=C6)=O)=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

Preparing Stock Solutions

The following data is based on the product molecular weight 614.74 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
1: Moody TW, Nuche-Berenguer B, Moreno P, Jensen RT. CI-988 Inhibits EGFR Transactivation and Proliferation Caused by Addition of CCK/Gastrin to Lung Cancer Cells. J Mol Neurosci. 2015 Jul;56(3):663-72. doi: 10.1007/s12031-015-0533-6. PubMed PMID: 25761747; PubMed Central PMCID: PMC4479967. 2: Kim J, Kim Y, Hahm SC, Yoon YW. Effect of the Combination of CI-988 and Morphine on Neuropathic Pain after Spinal Cord Injury in Rats. Korean J Physiol Pharmacol. 2015 Mar;19(2):125-30. doi: 10.4196/kjpp.2015.19.2.125. PubMed PMID: 25729274; PubMed Central PMCID: PMC4342732. 3: Moody TW, Jensen RT. CI-988 inhibits growth of small cell lung cancer cells. J Pharmacol Exp Ther. 2001 Dec;299(3):1154-60. PubMed PMID: 11714907. 4: Coudoré-Civiale MA, Courteix C, Fialip J, Boucher M, Eschalier A. Spinal effect of the cholecystokinin-B receptor antagonist CI-988 on hyperalgesia, allodynia and morphine-induced analgesia in diabetic and mononeuropathic rats. Pain. 2000 Oct;88(1):15-22. PubMed PMID: 11098095. 5: Coudoré-Civiale MA, Courteix C, Boucher M, Méen M, Fialip J, Eschalier A, Ardid D. Potentiation of morphine and clomipramine analgesia by cholecystokinin -B antagonist CI-988 in diabetic rats. Neurosci Lett. 2000 May 26;286(1):37-40. PubMed PMID: 10822147. 6: Pande AC, Greiner M, Adams JB, Lydiard RB, Pierce MW. Placebo-controlled trial of the CCK-B antagonist, CI-988, in panic disorder. Biol Psychiatry. 1999 Sep 15;46(6):860-2. PubMed PMID: 10494457. 7: Goddard AW, Woods SW, Money R, Pande AC, Charney DS, Goodman WK, Heninger GR, Price LH. Effects of the CCK(B) antagonist CI-988 on responses to mCPP in generalized anxiety disorder. Psychiatry Res. 1999 Mar 22;85(3):225-40. PubMed PMID: 10333376. 8: Dethloff LA, Barr BM, Bestervelt LL. Inhibition of gastrin-stimulated cell proliferation by the CCK-B/gastrin receptor ligand CI-988. Food Chem Toxicol. 1999 Feb-Mar;37(2-3):105-10. PubMed PMID: 10227733. 9: Dethloff LA, Patmore SJ, Tierney BM, Bestervelt LL, Zandee JC. Gastric effects of the CCK-B/gastrin receptor ligand CI-988 in cynomolgus monkeys. Food Chem Toxicol. 1998 Jan;36(1):61-71. PubMed PMID: 9487364. 10: Dethloff LA, Robertson DG, Tierney BM, Breider MA, Bestervelt LL. Gastric gland degeneration induced in monkeys by the CCK-B/gastrin receptor antagonist CI-988. Toxicol Pathol. 1997 Sep-Oct;25(5):441-8. PubMed PMID: 9323831. 11: Xu XJ, Elfvin A, Hao JX, Fournié-Zaluski MC, Roques BP, Wiesenfeld-Hallin Z. CI 988, an antagonist of the cholecystokinin-B receptor, potentiates endogenous opioid-mediated antinociception at spinal level. Neuropeptides. 1997 Jun;31(3):287-91. PubMed PMID: 9243527. 12: Marvik R, Sandvik AK, Waldum HL. Evaluation of biologic gastrin activity of compound CI-988 in the isolated, vascularly perfused rat stomach. Scand J Gastroenterol. 1997 Jun;32(6):519-22. PubMed PMID: 9200280. 13: van Megen HJ, Westenberg HG, den Boer JA, Slaap B, van Es-Radhakishun F, Pande AC. The cholecystokinin-B receptor antagonist CI-988 failed to affect CCK-4 induced symptoms in panic disorder patients. Psychopharmacology (Berl). 1997 Feb;129(3):243-8. PubMed PMID: 9084062. 14: Augelli-Szafran CE, Horwell DC, Kneen C, Ortwine DF, Pritchard MC, Purchase TS, Roth BD, Trivedi BK, Hill D, Suman-Chauhan N, Webdale L. Cholecystokinin B antagonists. Synthesis and quantitative structure-activity relationships of a series of C-terminal analogues of CI-988. Bioorg Med Chem. 1996 Oct;4(10):1733-45. PubMed PMID: 8931944. 15: Hinks GL, Brown P, Field M, Poat JA, Hughes J. The anxiolytics CI-988 and chlordiazepoxide fail to reduce immediate early gene mRNA stimulation following exposure to the rat elevated X-maze. Eur J Pharmacol. 1996 Sep 26;312(2):153-61. PubMed PMID: 8894590. 16: Cowley DS, Adams JB, Pyke RE, Cook J, Zaccharias P, Wingerson D, Roy-Byrne PP. Effect of CI-988, a cholecystokinin-B receptor antagonist, on lactate-induced panic. Biol Psychiatry. 1996 Sep 15;40(6):550-2. PubMed PMID: 8879478. 17: Hinton JP, Pablo JC, Bjorge SM, Hoffman K, Jennings K, Wright DS. Three complementary liquid chromatographic methods for determination of the peptoid cholecystokinin-B antagonist, CI-988, in rat plasma. J Pharm Biomed Anal. 1996 May;14(7):815-24. PubMed PMID: 8809706. 18: Romani R, Howes LG, Morris DL. Dose dependent in vivo inhibition of human colorectal cancer (LoVo) by the gastrin receptor antagonist, CI-988. Clin Exp Pharmacol Physiol. 1996 May;23(5):438-40. PubMed PMID: 8713686. 19: Romani R, Howes LG, Morris DL. Gastrin receptor antagonist CI-988 inhibits growth of human colon cancer in vivo and in vitro. Aust N Z J Surg. 1996 Apr;66(4):235-7. PubMed PMID: 8611133. 20: Webb JK, Rupniak NM, Boyce S. Inhibition of pentagastrin-induced pressor response in conscious rats by the CCK-B receptor antagonist CI-988 and chlordiazepoxide. Regul Pept. 1996 Jan 16;61(1):71-6. PubMed PMID: 8701030.