TP 003

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Cat.No. 4414 - TP 003 | C23H16F3N3O | CAS No. 628690-75-5
Description: GABAA partial agonist; acts at benzodiazepine site
Chemical Name: 2',4-Difluoro-5'-[8-fluoro-7-(1-hydroxy-1-methylethyl)imidazo[1,2-a]-pyridin-3-yl]-[1,1'-biphenyl]-2-carbonitrile
Purity: ≥98% (HPLC)
Datasheet
Citations (3)
Reviews
Literature (7)

Biological Activity

GABAA receptor partial agonist that demonstrates affinity for the benzodiazepine site. Potentiates GABAA α3 response with high efficacy. Produces anxiolytic-like effects in rodent elevated plus maze via action at GABAA α2 subtype receptors. Also evokes GABAA α1 mediated sedation and GABAA α3 mediated muscle relaxation in mice.

Compound Libraries

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Technical Data

M. Wt 407.39
Formula C23H16F3N3O
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 628690-75-5
PubChem ID 10001434
InChI Key SJMMDWXJSSJHOQ-UHFFFAOYSA-N
Smiles FC1=C(C(C)(O)C)C=CN2C1=NC=C2C3=CC=C(F)C(C4=CC=C(F)C=C4C#N)=C3

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 40.74 100
ethanol 20.37 50

Preparing Stock Solutions

The following data is based on the product molecular weight 407.39. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.45 mL 12.27 mL 24.55 mL
5 mM 0.49 mL 2.45 mL 4.91 mL
10 mM 0.25 mL 1.23 mL 2.45 mL
50 mM 0.05 mL 0.25 mL 0.49 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Dias et al (2005) Evidence for a significant role of α3-containing GABAA receptors in mediating the anxiolytic effects of benzodiazepines. J.Neurosci. 25 10682 PMID: 16291941

Fischer et al (2011) Contribution of GABA(A) receptors containing α3 subunits to the therapeutic-related and side effects of benzodiazepine-type drugs in monkeys. Psychopharmacology (Berl.) 215 311 PMID: 21190016

Neumann et al (2018) TP003 is a non-selective benzodiazepine site agonist that induces anxiolysis via α2GABAA receptors. Neuropharmacology 143 71 PMID: 30240781


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Keywords: TP 003, TP 003 supplier, TP003, GABAA, GABA, receptors, a3, alpha3, α3, agonists, anxiolytic, Receptors, 4414, Tocris Bioscience

3 Citations for TP 003

Citations are publications that use Tocris products. Selected citations for TP 003 include:

Seifi et al (2018) GABAA Receptor Subtypes Regulate Stress-Induced Colon Inflammation in Mice. Gastroenterology 155 852 PMID: 29802853

Soderhielm et al (2018) Probing the molecular basis for affinity/potency- and efficacy-based subtype-selectivity exhibited by benzodiazepine-site modulators at GABAA receptors. Biochem Pharmacol 158 339 PMID: 30121248

Seifi et al (2014) Molecular and functional diversity of GABA-A receptors in the enteric nervous system of the mouse colon. Gastroenterology 34 10361 PMID: 25080596


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