(S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide
- Product Name
- (S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide
- CAS No.
- 1346133-11-6
- Chemical Name
- (S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide
- Synonyms
- FP3FBZ;LY2444296;Ly2444296 (fp3fbz);LY2444296, 10 mM in DMSO;(S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide;3-fluoro-4-(4-{[(2S)-2-(3-fluorophenyl)pyrrolidin-1-yl]methyl}phenoxy)benzamide;Benzamide, 3-fluoro-4-[4-[[(2S)-2-(3-fluorophenyl)-1-pyrrolidinyl]methyl]phenoxy]-
- CBNumber
- CB24858724
- Molecular Formula
- C24H22F2N2O2
- Formula Weight
- 408.44
- MOL File
- 1346133-11-6.mol
(S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide Property
- 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
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P280Wear protective gloves/protective clothing/eye protection/face protection.
P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P302+P352IF ON SKIN: wash with plenty of soap and water.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- SML2452
- Product name
- LY2444296
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $84.83
- Updated
- 2025/07/31
- Product number
- SML2452
- Product name
- LY2444296
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $360
- Updated
- 2025/07/31
- Product number
- CS-0110108
- Product name
- LY2444296
- Purity
- 99.78%
- Packaging
- 50mg
- Price
- $600
- Updated
- 2021/12/16
- Product number
- CS-0110108
- Product name
- LY2444296
- Purity
- 99.78%
- Packaging
- 5mg
- Price
- $80
- Updated
- 2021/12/16
- Product number
- CS-0110108
- Product name
- LY2444296
- Purity
- 99.78%
- Packaging
- 10mg
- Price
- $150
- Updated
- 2021/12/16
(S)-3-fluoro-4-(4-((2-(3-fluorophenyl)pyrrolidin-1-yl)methyl)phenoxy)benzamide Chemical Properties,Usage,Production
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)benzamide Preparation Products And Raw materials
Raw materials
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