MedKoo Cat#: 317148 | Name: Lorediplon
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

Lorediplon
Lorediplon
CAS#917393-39-6

Theoretical Analysis

MedKoo Cat#: 317148

Name: Lorediplon

CAS#: 917393-39-6

Chemical Formula: C20H15FN4O2S

Exact Mass: 394.0900

Molecular Weight: 394.42

Elemental Analysis: C, 60.90; H, 3.83; F, 4.82; N, 14.21; O, 8.11; S, 8.13

Price and Availability

Size Price Availability Quantity
50mg USD 250.00 2 weeks
100mg USD 450.00 2 weeks
200mg USD 850.00 2 weeks
500mg USD 1,650.00 2 weeks
1g USD 2,650.00 2 weeks
2g USD 3,950.00 2 weeks
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Related CAS #
No Data
Synonym
Lorediplon
IUPAC/Chemical Name
N-[2-fluoro-5-[3-(thiophene-2-carbonyl)pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]-N-methylacetamide
InChi Key
NQPOCLFSADOXBR-UHFFFAOYSA-N
InChi Code
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
SMILES Code
CC(N(C1=CC(C2=CC=NC3=C(C(C4=CC=CS4)=O)C=NN23)=CC=C1F)C)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Biological target:
Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
In vitro activity:
TBD
In vivo activity:
TBD
Solvent mg/mL mM
Solubility
DMF 25.0 63.38
DMF:PBS (pH 7.2) (1:1) 0.5 1.27
DMSO 57.0 144.51
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 394.42 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
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.