Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C26H27FN2O2 |
Molecular Weight | 418.5032 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=CC(=CC(C)=C1)[C@@H]2CCCN2CC3=CC=C(OC4=C(F)C=C(C=C4)C(N)=O)C=C3
InChI
InChIKey=ZHPMYDSXGRRERG-DEOSSOPVSA-N
InChI=1S/C26H27FN2O2/c1-17-12-18(2)14-21(13-17)24-4-3-11-29(24)16-19-5-8-22(9-6-19)31-25-10-7-20(26(28)30)15-23(25)27/h5-10,12-15,24H,3-4,11,16H2,1-2H3,(H2,28,30)/t24-/m0/s1
LY-2456302 or CERC-501 (now JNJ-67953964) is a non-peptide, centrally-penetrant, potent, short-acting kappa opioid receptor (KOR)-selective antagonist with pharmacokinetic properties favorable for clinical development and activity in animal models predictive of efficacy in mood and addictive disorders. It is under development for depression and substance abuse disorders.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P41145 Gene ID: 4986.0 Gene Symbol: OPRK1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/24854795 |
0.18 nM [Ki] |
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02218736
Phase 2 study: Oral dosing of 10 mg CERC-501 daily for 8 weeks
Route of Administration:
Oral
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LY-2456302
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10582
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100000183561
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44129648
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1174130-61-0
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DB12341
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C170144
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DE4G8X55F5
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DTXSID90151777
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HI-125
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ACTIVE MOIETY