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Description: Positive allosteric modulator of GABAA receptors; displays subunit selectivity
Chemical Name: 4-Chloro-N-[2-(2-thienyl)imidazo[1,2-a]pyridin-3-yl]benzamide
Purity: ≥97% (HPLC)
Biological Activity for DS2
DS2 is a positive allosteric modulator of GABAA receptors. Potentiates GABA-evoked currents mediated by α4β3δ receptors (EC50 = 142 nM, in vitro). Displays complex selectivity profile, with selectivity for δ-containing receptors (α4/6βxδ > α1βxδ >> γ2 > α4β3 GABAA receptors). Enhances tonic currents of thalamocortical neurons in wild-type mice.
Compound Libraries for DS2
DS2 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for DS2
| M. Wt | 353.83 |
| Formula | C18H12ClN3OS |
| Storage | Desiccate at +4°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 374084-31-8 |
| PubChem ID | 979718 |
| InChI Key | AZKMWHRDICVYEI-UHFFFAOYSA-N |
| Smiles | O=C(C4=CC=C(Cl)C=C4)NC2=C(C3=CC=CS3)N=C1C=CC=CN12 |
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 DS2
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 17.69 | 50 |
Preparing Stock Solutions for DS2
The following data is based on the product molecular weight 353.83. 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 |
|---|---|---|---|
| 0.5 mM | 5.65 mL | 28.26 mL | 56.52 mL |
| 2.5 mM | 1.13 mL | 5.65 mL | 11.3 mL |
| 5 mM | 0.57 mL | 2.83 mL | 5.65 mL |
| 25 mM | 0.11 mL | 0.57 mL | 1.13 mL |
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Product Datasheets for DS2
References for DS2
References are publications that support the biological activity of the product.
Wafford et al (2009) Novel compounds selectively enhance δ subunit containing GABAA receptors and increase tonic currents in thalamus. Neuropharmacology 56 182 PMID: 18762200
Jensen et al (2013) A study of subunit selectivity, mechanism and site of action of the delta selective compound 2 (DS2) at human recombinant and rodent native GABAA receptors. Br.J.Pharmacol. 168 1118 PMID: 23061935
Ahring et al (2016) A pharmacological assessment of agonists and modulators at α4β2γ2 and α4β2δ GABAA receptors: The challenge in comparing apples with oranges. Pharmacol.Res. 111 563 PMID: 27178730
If you know of a relevant reference for DS2, please let us know.
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Keywords: DS2, DS2 supplier, Positive, allosteric, modulators, delta, GABAA, receptors, PAM, Receptors, 3679, Tocris Bioscience
8 Citations for DS2
Citations are publications that use Tocris products. Selected citations for DS2 include:
Kerti-Szigeti et al (2014) Synaptic GABAA receptor clustering without the γ2 subunit. Nat Methods 34 10219 PMID: 25080584
Mirheydari et al (2014) Unexpected Properties of δ-Containing GABAA Receptors in Response to Ligands Interacting with the α+ β- Site. Neurochem Res 39 1057 PMID: 24072672
Tong et al (2015) Ectopic Expression of α6 and δ GABAA Receptor Subunits in Hilar Somatostatin Neurons Increases Tonic Inhibition and Alters Network Activity in the Dentate Gyrus. J Neurosci 35 16142 PMID: 26658866
Hammer et al (2015) Functional characterization of the 1,5-benzodiazepine clo. and its major active metabolite N-desmethylclobazam at human GABA(A) receptors expressed in Xenopus laevis oocytes. PLoS One 10 e0120239 PMID: 25798598
Shu et al (2012) Characteristics of concatemeric GABA(A) receptors containing α4/δ subunits expressed in Xenopus oocytes. Br J Pharmacol 165 2228 PMID: 21950777
Olander et al (2018) Delineation of the functional properties and the mechanism of action of AA29504, an allosteric agonist and positive allosteric modulator of GABAA receptors. Biochem Pharmacol 150 305 PMID: 29454619
Mennerick et al (2014) Phosphatidylinositol 4,5-bisphosphate depletion fails to affect neurosteroid modulation of GABAA receptor function. Psychopharmacology (Berl) 231 3493 PMID: 24553581
Patel et al (2016) Context-Dependent Modulation of GABAAR-Mediated Tonic Currents. J Neurosci 36 607 PMID: 26758848
Do you know of a great paper that uses DS2 from Tocris? Please let us know.
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