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说明： Selective positive allosteric modulator of M4 receptors; active in vivo; antipsychotic
化学名： 3-Amino-5-chloro-N-cyclopropyl-6-methoxy-4-methylthieno[2,3-b]pyridine-2-carboxamide
纯度： ≥98% (HPLC)
生物活性 for LY 2033298
LY 2033298 is a selective positive allosteric modulator of M4 receptor (KB = 200 nM, α = 35); increases the potency of acetylcholine by 40-fold. Exhibits no effect at hM1/3/5 receptors and a small effect at hM2 (KB = 1 μM α = 3.7). Potentiates other full and partial orthosteric agonists, including Carbachol, Oxotremorine-M, and McN-A343. Does not affect binding of antagonist NMS. Active in vivo. Antipsychotic.
α indicates the degree of allosteric enhancement when both orthosteric and allosteric sites are occupied (derived from the allosteric ternary complex model).
化合物库 for LY 2033298
LY 2033298 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 LY 2033298
| 分子量 | 311.79 |
| 公式 | C13H14ClN3O2S |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 886047-13-8 |
| PubChem ID | 11536903 |
| InChI Key | CTEGQKDJTBWFHW-UHFFFAOYSA-N |
| Smiles | NC1=C(C(NC2CC2)=O)SC3=NC(OC)=C(Cl)C(C)=C31 |
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 LY 2033298
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 31.18 | 100 | |
| ethanol | 6.24 | 20 |
制备储备液 for LY 2033298
以下数据基于产品分子量 311.79。 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 | 3.21 mL | 16.04 mL | 32.07 mL |
| 5 mM | 0.64 mL | 3.21 mL | 6.41 mL |
| 10 mM | 0.32 mL | 1.6 mL | 3.21 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.64 mL |
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产品说明书 for LY 2033298
参考文献 for LY 2033298
参考文献是支持产品生物活性的出版物。
Leach et al (2010) Molecular mechanisms of action and in vivo validation of an M4 muscarinic acetylcholine receptor allosteric modulator with potential antipsychotic properties. Neuropsychopharmacology 35 855 PMID: 19940843
Huynh et al (2015) Synthesis and pharmacological evaluation of M4 muscarinic receptor positive allosteric modulators derived from VU10004. ACS Chem. Neurosci. 6 838 PMID: 25857219
Chan et al (2008) Allosteric modulation of the muscarinic M4 receptor as an approach to treating schizophrenia Proc.Natl.Acad.Sci.U.S.A. 105 10978 PMID: 18678919
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关键词: LY 2033298, LY 2033298 supplier, LY2033298, Selective, positive, allosteric, modulators, M4, receptors, PAMs, active, in, vivo, antipsychotic, acetylcholine, modulates, Receptors, 7027, Tocris Bioscience
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