A κ-opioid receptor agonist
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ICI 204448 (hydrochloride)

Item No. 45206

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[3-[1-[[2-(3,4-dichlorophenyl)acetyl]methylamino]-2-(1-pyrrolidinyl)ethyl]phenoxy]-acetic acid, monohydrochloride
CAS Number
121264-04-8
Molecular Formula
C23H26Cl2N2O4 • HCl
Formula Weight
501.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
CN(C(C1=CC(OCC(O)=O)=CC=C1)CN2CCCC2)C(CC3=CC=C(Cl)C(Cl)=C3)=O.Cl
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
InChi Key
FNDGLVOYAQNQPE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $27

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    5 mg

    $108

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    10 mg

    $189

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    25 mg

    $439

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    Product Description

    ICI 204448 is a κ-opioid receptor agonist.1 It binds to the κ-opioid receptor (Ki = 2.69 nM) and is 162- and 69-fold selective for the κ-opioid receptor over the μ- and δ-opioid receptors in membranes prepared from cells expressing the human κ-, μ- and δ-opioid receptors, repectively. ICI 204448 reduces acetic acid-induced writhing and chloroquine-induced scratching in mice.1,2 It also reduces infarct size in rat hearts when administered ten minutes prior to the onset of ischemia.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kumar, V., Guo, D., Cassel, J.A., et al. Synthesis and evaluation of novel peripherally restricted κ-opioid receptor agonists. Bioorg. Med. Chem. Lett. 15(4), 1091-1095 (2005).

    2. Inan, S., and Cowan, A. Kappa opioid agonists suppress chloroquine-induced scratching in mice. Eur. J. Pharmacol. 502(3), 233-237 (2004).

    3. Peart, J.N., Gross, E.R., and Gross, G.J. Effect of exogenous kappa-opioid receptor activation in rat model of myocardial infarction. J. Cardiovasc. Pharmacol. 43(3), 410-415 (2004).