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说明： Positive allosteric modulator of GABAA receptors; displays subunit selectivity
化学名： 4-Chloro-N-[2-(2-thienyl)imidazo[1,2-a]pyridin-3-yl]benzamide
纯度： ≥97% (HPLC)
生物活性 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.
化合物库 for DS2
DS2 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for DS2
| 分子量 | 353.83 |
| 公式 | C18H12ClN3OS |
| 储存 | Desiccate at +4°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for DS2
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 17.69 | 50 |
制备储备液 for DS2
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for DS2
参考文献 for DS2
参考文献是支持产品生物活性的出版物。
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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关键词: DS2, DS2 supplier, Positive, allosteric, modulators, delta, GABAA, receptors, PAM, Receptors, 3679, Tocris Bioscience
8 篇 DS2 的引用文献
引用文献是使用了 Tocris 产品的出版物。 DS2 的部分引用包括：
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
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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