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Submit ReviewVU 0357017 hydrochloride is a positive allosteric modulator of muscarinic M1 receptors (EC50 = 198 nM). Displays no activity at M2-M5 at concentrations up to 30 μM. Potentiates NMDA receptor currents in hippocampal neurons; activity reverses cognitive decifits in a rodent model of hippocampal-dependent memory. CNS penetrant.
分子量 | 369.89 |
公式 | C18H27N3O3.HCl |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1135242-13-5 |
PubChem ID | 25010775 |
InChI Key | XKJQVUIXSBOCPP-UHFFFAOYSA-N |
Smiles | CC1=CC=CC=C1C(NCCNC2CCN(C(OCC)=O)CC2)=O.Cl |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 9.25 | 25 | |
DMSO | 1.85 | 5 |
以下数据基于产品分子量 369.89。 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 |
---|---|---|---|
0.25 mM | 10.81 mL | 54.07 mL | 108.14 mL |
1.25 mM | 2.16 mL | 10.81 mL | 21.63 mL |
2.5 mM | 1.08 mL | 5.41 mL | 10.81 mL |
12.5 mM | 0.22 mL | 1.08 mL | 2.16 mL |
参考文献是支持产品生物活性的出版物。
Bridges et al (2010) Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) Lead. Part II. Development of potent and highly selective M1 PAM. Bioorg.Med.Chem.Lett. 20 1972 PMID: 20156687
Lebois et al (2010) Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M1 receptor function in the central nervous system. ACS Chem.Neurosci. 1 104
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关键词: VU 0357017 hydrochloride, VU 0357017 hydrochloride supplier, VU0357017, hydrochloride, muscarinics, acetylcholine, machrs, positive, allosteric, modulators, pams, m1, selective, M1, Receptors, 4295, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 VU 0357017 hydrochloride 的部分引用包括:
Pasko et al (2020) Muscarinic M1 Receptors Modulate Working Memory Performance and Activity via KCNQ Potassium Channels in the Primate Prefrontal Cortex. Neuron 106 649-661.e4 PMID: 32197063
Stefan et al (2018) Muscarinic M1 Receptor Overstimulation Disrupts Working Memory Activity for Rules in Primate Prefrontal Cortex. Neuron 98 1256-1268.e4 PMID: 29887340
Jadeja et al (2016) Data regarding M1 muscarinic receptor-mediated modulation of hepatic catalase activity in response to oxidative stress. J Am Soc Nephrol 6 405 PMID: 26862589
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