| Identification | Back Directory | [Name]
(S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide | [CAS]
1346133-11-6 | [Synonyms]
FP3FBZ
LY2444296
(S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide | [Molecular Formula]
C24H22F2N2O2 | [MDL Number]
MFCD32067413 | [MOL File]
1346133-11-6.mol | [Molecular Weight]
408.44 |
| Chemical Properties | Back Directory | [Boiling point ]
491.6±45.0 °C(Predicted) | [density ]
1.276±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Ethanol: 27.5 mg/mL (67.33 mM); Methanol: 5 mg/mL (12.24 mM) | [form ]
Solid | [pka]
15.61±0.50(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
LY2444296 is a brain-penetrantorally activeshort-actinghigh-affinitypotent and selective K (kappa) opioid receptor (KOR) antagonist (human K/μ/δ Ki = 0.565/35.8/211 nM against diprenorphine binding; GTP-γ-S binding IC50/agonist/subtype transfectant = 1.57 nM/300 nM U69593/K21.3 nM/1 μM DAMGO/μ 293 nM/30 nM DPDPE/d). LY2444296 reverses K agonist antinociceptive efficacy in vivo (ED50 = 0.24 mg/kg p.o. against 1 mg/kg U69593 sc. by r at formalin test)decreases immobility time (10 or 30 mg/kg sc.) and prevents enhanced alcohol consumption (5 mg/kg i.p.) among mice subjected to stress by forced swimming. | [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-na?ve 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-na?ve 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-na?ve rats. |
| [IC 50]
κ Opioid Receptor/KOR | [storage]
Store at -20°C | [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. DOI:10.1016/j.neulet.2016.01.017
[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. DOI:10.1007/s00213-017-4647-0 |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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