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Submit ReviewTP 003
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)
Biological Activity for TP 003
TP 003 is a 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 for TP 003
TP 003 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for TP 003
| 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 for TP 003
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.74 | 100 | |
| ethanol | 20.37 | 50 |
Preparing Stock Solutions for TP 003
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.
| 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 for TP 003
References for TP 003
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
If you know of a relevant reference for TP 003, please let us know.
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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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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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