MedKoo Cat#: 534907 | Name: ICI-204448 HCl
Featured New

Description:

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

ICI-204448 is a potent and peripherally selective κ-opioid agonist, with possible uses in the treatment of heart attack as well as anti-itching effects. It is used in research to distinguish centrally from peripherally mediated kappa opioid receptor effects.

Chemical Structure

ICI-204448 HCl
ICI-204448 HCl
CAS#121264-04-8 (HCl)

Theoretical Analysis

MedKoo Cat#: 534907

Name: ICI-204448 HCl

CAS#: 121264-04-8 (HCl)

Chemical Formula: C23H27Cl3N2O4

Exact Mass: 0.0000

Molecular Weight: 501.83

Elemental Analysis: C, 55.05; H, 5.42; Cl, 21.19; N, 5.58; O, 12.75

Price and Availability

Size Price Availability Quantity
50mg USD 450.00 2 Weeks
100mg USD 750.00 2 Weeks
200mg USD 1,250.00 2 Weeks
500mg USD 2,850.00 2 Weeks
1g USD 4,250.00 2 Weeks
2g USD 6,450.00 2 Weeks
Show More
Bulk Inquiry
Buy Now
Add to Cart
Synonym
ICI-204448 HCl; ICI-204448 hydrochloride; ICI-204448; ICI 204448; ICI 204448;
IUPAC/Chemical Name
Acetic acid, (3-(1-(((3,4-dichlorophenyl)acetyl)methylamino)-2-(1-pyrrolidinyl)ethyl)phenoxy)-, monohydrochloride, (+-)-
InChi Key
FNDGLVOYAQNQPE-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H26Cl2N2O4.ClH/c1-26(22(28)12-16-7-8-19(24)20(25)11-16)21(14-27-9-2-3-10-27)17-5-4-6-18(13-17)31-15-23(29)30;/h4-8,11,13,21H,2-3,9-10,12,14-15H2,1H3,(H,29,30);1H
SMILES Code
O=C(O)COC1=CC=CC(C(N(C(CC2=CC=C(Cl)C(Cl)=C2)=O)C)CN3CCCC3)=C1.[H]Cl
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
>3 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 501.83 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: Ma D, Huang Q, Gao X, Ford NC, Guo R, Zhang C, Liu S, He SQ, Raja SN, Guan Y. The Utility of Peripherally Restricted Kappa-Opioid Receptor Agonists for Inhibiting Below-Level Pain After Spinal Cord Injury in Mice. Neuroscience. 2023 Sep 1;527:92-102. doi: 10.1016/j.neuroscience.2023.07.017. Epub 2023 Jul 27. PMID: 37516437; PMCID: PMC10530135. 2: Nakasone T, Wakuda H, Sugimoto Y, Kamei C. Effects of ICI204,448, naloxone methiodide and levocetirizine on the scratching behavior induced by a κ-opioid antagonist, nor-BNI, in ICR mice. Immunopharmacol Immunotoxicol. 2017 Oct;39(5):292-295. doi: 10.1080/08923973.2017.1354879. Epub 2017 Jul 26. PMID: 28745076. 3: Sudakov SK, Bogdanova NG. Activation of Peripheral κ-Opioid Receptors Normalizes Caffeine Effects Modified in Nicotine-Dependent Rats during Nicotine Withdrawal. Bull Exp Biol Med. 2016 Oct;161(6):743-745. doi: 10.1007/s10517-016-3499-7. Epub 2016 Oct 26. PMID: 27785643. 4: Trigub MM, Bogdanova NG, Kolpakov AA, Bashkatova VG, Sudakov SK. Effect of peripheral opioid receptor agonists on depressive activity of ethanol. Bull Exp Biol Med. 2014 Apr;156(6):778-80. doi: 10.1007/s10517-014-2448-6. Epub 2014 May 3. PMID: 24824695. 5: Sudakov SK, Nazarova GA, Alekseeva EV. Changes in feeding behavior, locomotor activity, and metabolism in rats upon modulation of opioid receptors in the gastrointestinal tract. Bull Exp Biol Med. 2014 Feb;156(4):423-5. doi: 10.1007/s10517-014-2365-8. Epub 2014 Mar 5. PMID: 24771418. 6: Sudakov SK, Nazarova GA, Alekseeva EV, Kolpakov AA. Effect of activated peripheral κ-opioid receptors on the action of nicotine and its withdrawal in nicotine-dependent rats. Bull Exp Biol Med. 2014 Mar;156(5):609-11. doi: 10.1007/s10517-014-2406-3. Epub 2014 Mar 25. PMID: 24770739. 7: Alexeeva EV, Nazarova GA, Sudakov SK. Effects of peripheral μ, δ, and Κ-opioid receptor agonists on the levels of anxiety and motor activity of rats. Bull Exp Biol Med. 2012 Sep;153(5):720-1. doi: 10.1007/s10517-012-1809-2. PMID: 23113268. 8: Negus SS, O'Connell R, Morrissey E, Cheng K, Rice KC. Effects of peripherally restricted κ opioid receptor agonists on pain-related stimulation and depression of behavior in rats. J Pharmacol Exp Ther. 2012 Mar;340(3):501-9. doi: 10.1124/jpet.111.186783. Epub 2011 Nov 29. PMID: 22128346; PMCID: PMC3286312. 9: Funez MI, Ferrari LF, Duarte DB, Sachs D, Cunha FQ, Lorenzetti BB, Parada CA, Ferreira SH. Teleantagonism: A pharmacodynamic property of the primary nociceptive neuron. Proc Natl Acad Sci U S A. 2008 Dec 9;105(49):19038-43. doi: 10.1073/pnas.0807922105. Epub 2008 Sep 17. PMID: 18799742; PMCID: PMC2614711. 10: Caram-Salas NL, Reyes-García G, Bartoszyk GD, Araiza-Saldaña CI, Ambriz- Tututi M, Rocha-González HI, Arreola-Espino R, Cruz SL, Granados-Soto V. Subcutaneous, intrathecal and periaqueductal grey administration of asimadoline and ICI-204448 reduces tactile allodynia in the rat. Eur J Pharmacol. 2007 Nov 14;573(1-3):75-83. doi: 10.1016/j.ejphar.2007.06.034. Epub 2007 Jun 29. PMID: 17643411. 11: Werkheiser JL, Rawls SM, Cowan A. Mu and kappa opioid receptor agonists antagonize icilin-induced wet-dog shaking in rats. Eur J Pharmacol. 2006 Oct 10;547(1-3):101-5. doi: 10.1016/j.ejphar.2006.07.026. Epub 2006 Jul 25. PMID: 16945367. 12: Rawls SM, Ding Z, Gray AM, Cowan A. Peripheral kappa-opioid agonist, ICI 204448, evokes hypothermia in cold-exposed rats. Pharmacology. 2005 May;74(2):79-83. doi: 10.1159/000083704. Epub 2005 Jan 12. PMID: 15687734. 13: Kumar V, Guo D, Cassel JA, Daubert JD, Dehaven RN, Dehaven-Hudkins DL, Gauntner EK, Gottshall SL, Greiner SL, Koblish M, Little PJ, Mansson E, Maycock AL. Synthesis and evaluation of novel peripherally restricted kappa-opioid receptor agonists. Bioorg Med Chem Lett. 2005 Feb 15;15(4):1091-5. doi: 10.1016/j.bmcl.2004.12.018. PMID: 15686919. 14: Peart JN, Gross ER, Gross GJ. Effect of exogenous kappa-opioid receptor activation in rat model of myocardial infarction. J Cardiovasc Pharmacol. 2004 Mar;43(3):410-5. doi: 10.1097/00005344-200403000-00012. PMID: 15076225. 15: Russell KR, Moore TT, Potter DE. Elevation of atrial natriuretic peptide levels in aqueous humor of the rabbit by kappa opioid receptor agonists. Neuropeptides. 2001 Oct-Dec;35(5-6):232-7. doi: 10.1054/npep.2001.0883. PMID: 12030807. 16: Moore TT, Potter DE. Kappa opioid agonist-induced changes in IOP: correlation with 3H-NE release and cAMP accumulation. Exp Eye Res. 2001 Aug;73(2):167-78. doi: 10.1006/exer.2001.1022. PMID: 11446767. 17: Carey GJ, Bergman J. Enadoline discrimination in squirrel monkeys: effects of opioid agonists and antagonists. J Pharmacol Exp Ther. 2001 Apr;297(1):215-23. PMID: 11259547. 18: Butelman ER, Harris TJ, Kreek MJ. Effects of E-2078, a stable dynorphin A(1-8) analog, on sedation and serum prolactin levels in rhesus monkeys. Psychopharmacology (Berl). 1999 Nov;147(1):73-80. doi: 10.1007/s002130051144. PMID: 10591871. 19: Hirst RA, Hirota K, Grandy DK, Lambert DG. Coupling of the cloned rat kappa- opioid receptor to adenylyl cyclase is dependent on receptor expression. Neurosci Lett. 1997 Aug 29;232(2):119-22. doi: 10.1016/s0304-3940(97)00594-6. PMID: 9302101. 20: Cosentino M, Marino F, Bombelli R, Ferrari M, Rasini E, Giaroni C, Lecchini S, Frigo G. Modulation of neurotransmitter release by opioid mu- and kappa- receptors from adrenergic terminals in the myenteric plexus of the guinea-pig colon: effect of alpha 2-autoreceptor blockade. Neurosci Lett. 1997 Jan 31;222(2):75-8. doi: 10.1016/s0304-3940(97)13344-4. PMID: 9111732.