DS2

Name: DS2
Brand: Tocris Bioscience
SKU: 3679

Tocris Bioscience a Bio-Techne Brand

Catalog # 3679

Citations (8)

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Key Product Details

Description:	Positive allosteric modulator of GABA_A receptors; displays subunit selectivity
Chemical Name:	4-Chloro-N-[2-(2-thienyl)imidazo[1,2-a]pyridin-3-yl]benzamide
Purity:	≥97% (HPLC)
Molecular Weight:	353.83

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Biological Activity for DS2

DS2 is a positive allosteric modulator of GABA_A 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 GABA_A 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 for DS2

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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	11.30 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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References for DS2

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

Ahring A pharmacological assessment of agonists and modulators at α4β2γ2 and α4β2δ GABA_A receptors: The challenge in comparing apples with oranges. Pharmacol.Res. 2016 PMID: 27178730
Jensen A study of subunit selectivity, mechanism and site of action of the delta selective compound 2 (DS2) at human recombinant and rodent native GABA_A receptors. Br.J.Pharmacol. 2013 PMID: 23061935
Wafford Novel compounds selectively enhance δ subunit containing GABA_A receptors and increase tonic currents in thalamus. Neuropharmacology 2009 PMID: 18762200

Citations for DS2 (8)

Showing 1 - 8 of 8 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for DS2 include:

Olander et al. (2018) Delineation of the functional properties and the mechanism of action of AA29504, an allosteric agonist and positive allosteric modulator of GABA_A receptors. Biochem Pharmacol. 150:305
PMID: 29454619
Patel et al. (2016) Context-Dependent Modulation of GABAAR-Mediated Tonic Currents. J Neurosci. 36:607
PMID: 26758848
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
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
Kerti-Szigeti et al. (2014) Synaptic GABAA receptor clustering without the γ2 subunit. Nat Methods. 34:10219
PMID: 25080584
Mennerick et al. (2014) Phosphatidylinositol 4,5-bisphosphate depletion fails to affect neurosteroid modulation of GABAA receptor function. Psychopharmacology (Berl). 231:3493
PMID: 24553581
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

There are no citations that match your criteria.