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Submit ReviewB 973B
说明： Positive allosteric modulator of α7 nAChRs; analgesic
别名： (-)-(S)-B 973B
化学名： 3,4-Difluoro-N-[(1S)-1-[6-[4-(2-pyridinyl)-1-piperazinyl]-2-pyrazinyl]ethyl]benzenepropanamide
纯度： ≥98% (HPLC)
生物活性 for B 973B
B 973B is a positive allosteric modulator of α7 nAChRs (EC50 ~0.3 μM); active enantiomer. Increases potency of acetylcholine (EC50 values are 0.007 mM and 0.3 mM in the presence and absence of B 937B, respectively). Potentiates peak acetylcholine-induced currents 6-fold relative to maximal acetylcholine, and slows channel desensitization, resulting in a 6900-fold increase in charge transfer. Decreases paw edema in vivo. Analgesic.
化合物库 for B 973B
B 973B 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 B 973B
| 分子量 | 452.5 |
| 公式 | C24H26F2N6O |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2244989-34-0 |
| PubChem ID | 137319851 |
| InChI Key | WQYZERNSONBUCW-KRWDZBQOSA-N |
| Smiles | C[C@@H](C1=CN=CC(N2CCN(C3=CC=CC=N3)CC2)=N1)NC(CCC4=CC(F)=C(C=C4)F)=O |
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 B 973B
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 45.25 | 100 | |
| ethanol | 22.62 | 50 |
制备储备液 for B 973B
以下数据基于产品分子量 452.5。 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 |
|---|---|---|---|
| 1 mM | 2.21 mL | 11.05 mL | 22.1 mL |
| 5 mM | 0.44 mL | 2.21 mL | 4.42 mL |
| 10 mM | 0.22 mL | 1.1 mL | 2.21 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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产品说明书 for B 973B
参考文献 for B 973B
参考文献是支持产品生物活性的出版物。
Garai et al (2018) B-973, a novel α7 nAChR Ago-PAM: racemic and asymmetric synthesis, electrophysiological studies, and in vivo evaluation. ACS Med.Chem.Lett. 9 1144 PMID: 30429960
Post-Munson et al (2017) B-973, a novel piperazine positive allosteric modulator of the α7 nicotinic acetylcholine receptor. Eur.J.Pharmacol. 15 799 PMID: 28132910
Quadri et al (2019) Macroscopic and microscopic activation of a7 nicotinic acetylcholine receptors by the structurally unrelated allosteric agonist-positive allosteric modulators (ago-PAMs) B-973B and GAT107. Mol.Pharmacol. 95 43 PMID: 30348894
If you know of a relevant reference for B 973B, please let us know.
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关键词: B 973B, B 973B supplier, B973B, B973, Positive, allosteric, modulators, of, α7, nAChRs, acetylcholine, nicotinic, receptors, PAMs, (-)-(S)-B, 973B, Nicotinic, (a7), Receptors, 6764, Tocris Bioscience
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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。
Nicotinic ACh Receptors Scientific Review
Updated in 2014, this review by Sue Wonnacott summarizes the diverse structure and function of nicotinic acetylcholine receptors and gives an in-depth review of the ligands available for nAChR research. Compounds available from Tocris are listed.
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