Lorediplon

Lorediplon is a nonbenzodiazepine of the pyrazolopyrimidine family that is being pursued as a treatment for insomnia but has not completed development. Lorediplon demonstrated a dose-dependent improvement in sleep, whereas zolpidem showed a more sustained WASO effect. No next-day hangover effects were observed. These sleep effects are also consistent with the pharmacokinetic profile of lorediplon. These results warrant clinical trials in patients with insomnia.

Product information

CAS Number: 917393-39-6

Molecular Weight: 394.42

Formula: C20H15FN4O2S

Synonym:

UNII-VKU6Z23NSY

VKU6Z23NSY

Lorediplon [INN]

SCHEMBL1316601

CHEMBL4303403

DTXSID00238684

BCP24663

EX-A4221

ZINC43207623

AKOS030526996

CS-5271

SB16784

Lorediplon

N-(2-Fluoro-5-(3-(thiophene-2-carbonyl)pyrazolo(1,5-a)pyrimidin-7-yl)phenyl)-N-methylacetamide

N-[2-fluoro-5-[3-(thiophene-2-carbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-N-methylacetamide

Acetamide, N-(2-fluoro-5-(3-(2-thienylcarbonyl)pyrazolo(1,5-a)pyrimidin-7-yl)phenyl)-N-methyl-

AK548104

AS-56211

HY-19371

GF-015535-00

Q6680290

N-{2-fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide

Chemical Name:  N-[2-fluoro-5-[3-(thiophene-2-carbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-N-methylacetamide

Smiles: CN(C1=CC(=CC=C1F)C1=CC=NC2=C(C=NN12)C(=O)C1=CC=CS1)C(C)=O

InChiKey: NQPOCLFSADOXBR-UHFFFAOYSA-N

InChi: InChI=1S/C20H15FN4O2S/c1-12(26)24(2)17-10-13(5-6-15(17)21)16-7-8-22-20-14(11-23-25(16)20)19(27)18-4-3-9-28-18/h3-11H,1-2H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

References:

1. Zisapel N. Current Phase II investigational therapies for insomnia. Expert Opin Investig Drugs. 2015 Mar;24(3):401-11. doi: 10.1517/13543784.2015.987340. Epub 2014 Nov 25. Review. PubMed PMID: 25423562.
2. Horoszok L, Baleeiro T, D'Aniello F, Gropper S, Santos B, Guglietta A, Roth T. A single-dose, randomized, double-blind, double dummy, placebo and positive-controlled, five-way cross-over study to assess the pharmacodynamic effects of lorediplon in a phase advance model of insomnia in healthy Caucasian adult male subjects. Hum Psychopharmacol. 2014 May;29(3):266-73. doi: 10.1002/hup.2395. PubMed PMID: 24911577.

Products are for research use only. Not for human use.