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Submit ReviewVU 0255035
说明： Highly selective M1 antagonist
化学名： N-[3-Oxo-3-[4-(4-pyridinyl)-1-piperazinyl]propyl]-2,1,3-benzothiadiazole-4-sulfonamide
纯度： ≥99% (HPLC)
生物活性 for VU 0255035
VU 0255035 is a highly selective muscarinic M1 antagonist (Ki = 14.87 nM). Targets the M1 orthosteric site with greater than 75-fold selectivity over the other receptor subtypes. Reduces pilocarpine-induced seizures in mice. Brain penetrant.
技术数据 for VU 0255035
| 分子量 | 432.52 |
| 公式 | C18H20N6O3S2 |
| 储存 | Store at -20°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 1135243-19-4 |
| PubChem ID | 24768606 |
| InChI Key | WXDHQWPQLKGANZ-UHFFFAOYSA-N |
| Smiles | O=C(CCNS(C4=CC=CC3=NSN=C34)(=O)=O)N(CC2)CCN2C1=CC=NC=C1 |
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 VU 0255035
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 8.65 | 20 |
制备储备液 for VU 0255035
以下数据基于产品分子量 432.52。 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 |
|---|---|---|---|
| 0.2 mM | 11.56 mL | 57.8 mL | 115.6 mL |
| 1 mM | 2.31 mL | 11.56 mL | 23.12 mL |
| 2 mM | 1.16 mL | 5.78 mL | 11.56 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.31 mL |
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产品说明书 for VU 0255035
参考文献 for VU 0255035
参考文献是支持产品生物活性的出版物。
Sheffler et al (2009) A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning. Mol.Pharmacol. 76 356 PMID: 19407080
If you know of a relevant reference for VU 0255035, please let us know.
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关键词: VU 0255035, VU 0255035 supplier, selective, muscarinic, receptors, M1, antagonists, mAChR, acetylcholine, ACh, VU0255035, Receptors, 3727, Tocris Bioscience
6 篇 VU 0255035 的引用文献
引用文献是使用了 Tocris 产品的出版物。 VU 0255035 的部分引用包括：
James M et al (2022) Cholinergic control of striatal GABAergic microcircuits. Cell Rep 41 111531 PMID: 36288709
Urrunaga et al (2015) M1 muscarinic receptors modify oxidative stress response to acetaminophen-induced acute liver injury. Proc Natl Acad Sci U S A 78 66 PMID: 25452146
Shin et al (2015) Muscarinic regulation of DA and glutamate transmission in the nucleus accumbens. Front Cell Neurosci 112 8124 PMID: 26080439
Martin et al (2015) Endocannabinoids Mediate Muscarinic Acetylcholine Receptor-Dependent Long-Term Depression in the Adult Medial Prefrontal Cortex. Mar Drugs 9 457 PMID: 26648844
Zhu et al (2017) Impairments of spatial memory in an Alzheimer's disease model via degeneration of hippocampal cholinergic synapses. Nat Commun 8 1676 PMID: 29162816
Rachakonda et al (2015) M1 Muscarinic Receptor Deficiency Attenuates Azoxymethane-Induced Chronic Liver Injury in Mice. Sci Rep 5 14110 PMID: 26374068
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