Indiplon

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Cat.No. 3597 - Indiplon | C20H16N4O2S | CAS No. 325715-02-4
Description: Subtype-selective GABAA receptor positive allosteric modulator
Alternative Names: NBI 34060
Chemical Name: N-Methyl-N-[3-[3-[2-thienylcarbonyl]pyrazolo[1,5-a]pyrimidin-7-yl]phenyl]acetamide
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

Potent GABAA receptor positive allosteric modulator that acts at the benzodiazepine site (Ki values are 1.2 and 1.7 nM in rat frontal cortex and cerebellum respectively). Displays ~ 10-fold selectivity for α1 subunit-containing receptors (EC50 values are 2.6, 24, 60 and 77 nM for α1β2γ2, α2β2γ2, α3β3γ2 and α5β2γ2 receptors respectively). Exhibits sedative, hypnotic, anxiolytic and anticonvulsant activity in vivo and is orally active.

Compound Libraries

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Technical Data

M. Wt 376.43
Formula C20H16N4O2S
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 325715-02-4
PubChem ID 6450813
InChI Key CBIAWPMZSFFRGN-UHFFFAOYSA-N
Smiles CN(C(C)=O)C1=CC=CC(C3=CC=NC2=C(C(C4=CC=CS4)=O)C=NN23)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 18.82 50
ethanol 1.88 5

Preparing Stock Solutions

The following data is based on the product molecular weight 376.43. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.66 mL 13.28 mL 26.57 mL
5 mM 0.53 mL 2.66 mL 5.31 mL
10 mM 0.27 mL 1.33 mL 2.66 mL
50 mM 0.05 mL 0.27 mL 0.53 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

Sullivan et al (2004) Characterization of the interaction of indiplon, a novel pyrazolopyrimidine sedative-hypnotic, with the GABAA receptor. J.Pharmacol.Exp.Ther. 311 537 PMID: 15256540

Foster et al (2004) In vivo pharmacological characterization of indiplon, a novel pyrazolopyrimidine sedative-hypnotic. J.Pharmacol.Exp.Ther. 311 547 PMID: 15256538

Petroski et al (2006) Indiplon is a high-affinity positive allosteric modulator with selectivity for α1 subunit-containing GABAA receptors. J.Pharmacol.Exp.Ther. 317 369 PMID: 16399882


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Keywords: Subtype-selective GABAA receptor positive allosteric modulators Receptors NBI34060 NBI 34060 GABAA Receptors

Citations for Indiplon

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Pathways for Indiplon

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