LY2444296

  Cat. No.:  DC28780   Featured
Chemical Structure
1346133-11-6
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More than 5000 active chemicals with high quality for research!
Field of application
LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects.
Cas No.: 1346133-11-6
Synonyms: LY2444296; FP3FBZ;LY-2444296;LY 2444296
SMILES: O=C(C1C=C(F)C(OC2C=CC(CN3CCC[C@H]3C3C=C(F)C=CC=3)=CC=2)=CC=1)N
Formula: C24H22F2N2O2
M.Wt: 408.440493106842
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [1]. Huang P, et al. Two short-acting kappa opioid receptor antagonists (zyklophin and LY2444296) exhibited different behavioral effects from the long-acting antagonist norbinaltorphimine in mouse anxiety tests. Neurosci Lett. 2016 Feb 26;615:15-20. [2]. Valenza M, et al. "Effects of the novel relatively short-acting kappa opioid receptor antagonist LY2444296 in behaviors observed after chronic extended-access cocaine self-administration in rats". Psychopharmacology (Berl). 2017 Aug;234(15):2219-2231.
Description: LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects[1][2].
Target: Ki: ~1 nM (KOPR)[1]
In Vivo: LY2444296 displays anti-anxiety like effects in the EPM test[1]. LY2444296 (3 mg/kg; i.p.; 30 min before U69,593 administration) prevents behavioral and neuroendocrine effects caused by the reference kappa agonist U69,593 in cocaine-naïve rats[2]. LY2444296 reduces anxiety-like and depressive-like behaviors, as well as CORT release, in rats tested after chronic extended access cocaine self-administration, but not in cocaine-naïve rats[2]. Animal Model: Adult male Sprague Dawley rats (240–250 g)[2] Dosage: 3 mg/kg Administration: Injected intraperitoneally; 30 min before U69,593 administration Result: Prevented behavioral and neuroendocrine effects caused by U69,593 in cocaine-naïve rats.
References: [1]. Huang P, et al. Two short-acting kappa opioid receptor antagonists (zyklophin and LY2444296) exhibited different behavioral effects from the long-acting antagonist norbinaltorphimine in mouse anxiety tests. Neurosci Lett. 2016 Feb 26;615:15-20. [2]. Valenza M, et al. "Effects of the novel relatively short-acting kappa opioid receptor antagonist LY2444296 in behaviors observed after chronic extended-access cocaine
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
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DC28780 LY2444296 LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a Ki value of ∼1 nM. LY2444296 exhibits anti-anxiety like effects.
DC10290 PZM21 PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.
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