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(S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide

Basic information Safety Supplier Related

(S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide Basic information

Product Name:
(S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide
Synonyms:
  • (S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide
  • LY2444296
  • FP3FBZ
  • Benzamide, 3-fluoro-4-[4-[[(2S)-2-(3-fluorophenyl)-1-pyrrolidinyl]methyl]phenoxy]-
  • 3-fluoro-4-(4-{[(2S)-2-(3-fluorophenyl)pyrrolidin-1-yl]methyl}phenoxy)benzamide
  • LY2444296, 10 mM in DMSO
  • Ly2444296 (fp3fbz)
CAS:
1346133-11-6
MF:
C24H22F2N2O2
MW:
408.44
Mol File:
1346133-11-6.mol
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(S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide Chemical Properties

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)
pka
15.61±0.50(Predicted)
form 
Solid
color 
Light yellow to yellow
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(S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide Usage And Synthesis

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-penetrant, orally active, short-acting, high-affinity, potent 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/K, 21.3 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

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

(S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamideSupplier

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(S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide(1346133-11-6)Related Product Information