CERC-501(LY-2456302,Aticaprant)
Cat. No.: DC9765
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Chemical Structure
1174130-61-0
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Field of application
CERC-501(LY-2456302) is a potent, selective antagonist of the kappa opioid receptor (KOR) (Ki = 0.81 nM vs. 24.0 nM and 155 nM for the μ-opioid receptor (MOR) and δ-opioid receptor (DOR), respectively.
| Cas No.: |
1174130-61-0 |
| Chemical Name: |
(S)-4-(4-((2-(3,5-dimethylphenyl)pyrrolidin-1-yl)methyl)phenoxy)-3-fluorobenzamide |
| Synonyms: |
(S)-4-(4-((2-(3,5-dimethylphenyl)pyrrolidin-1-yl)methyl)phenoxy)-3-fluorobenzamide;4-[4-[[(2S)-2-(3,5-dimethylphenyl)pyrrolidin-1-yl]methyl]phenoxy]-3-fluorobenzamide;CERC 501;LY 2456302;Aticaprant |
| SMILES: |
O=C(N)C1=CC=C(OC2=CC=C(CN3[C@H](C4=CC(C)=CC(C)=C4)CCC3)C=C2)C(F)=C1 |
| Formula: |
C26H27N2O2F |
| M.Wt: |
418.50318 |
| Sotrage: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
LY-2456302 is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM. |
| In Vivo: |
LY2456302 has a rapid absorption (tmax=1-2 h) and good oral bioavailability (F=25%). Oral LY2456302 administration selectively and potently occupies central kappa opioid receptors (ED50=0.33 mg/kg), without evidence of mu or delta receptor occupancy. LY2456302 potently blocks kappa-agonist-mediated analgesia and disruption of prepulse inhibition, without affecting mu-agonist-mediated effects at doses >30-fold higher. LY2456302 produces antidepressant-like effects in the mouse forced swim test and enhances the effects of imipramine and citalopram. LY2456302 reduces ethanol self-administration in alcohol-preferring rats[1]. LY2456302 alleviates the nicotine withdrawal syndrome, as evidenced by decreased expression of nicotine withdrawal induced anxiety-related behavior, somatic signs, and CPA, and increased hotplate latency in nicotine withdrawn mice following pre-treatment[2]. |
| In Vitro: |
LY2456302 binds with high affinity to the human kappa opioid receptor with a 30-fold higher affinity over the human mu opioid receptor and 190-fold higher affinity over the human delta opioid receptor. LY2456302 shows no appreciable affinity for several non-opioid cell surface G-protein-coupled receptor targets, including monoaminergic, muscarinic, cholinergic, and adrenergic receptors or ion channel/transporter binding targets or the central benzodiazepine binding site[1]. |
MSDS
COA
| LOT NO. |
DOWNLOAD |
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| 2018-0101 |
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| 2018-0101 |
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