| 中文名称 |
Usmarapride
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| 英文名称 |
Usmarapride
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| 英文别名 |
Usmarapride;1JPX7J35CG;2-[1-(3-methoxypropyl)piperidin-4-yl]-5-(1-propan-2-ylindazol-3-yl)-1,3,4-oxadiazole;oxalic acid;SUVN-D4010 oxalate
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| Cas No. |
1428862-33-2
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| 分子式 |
C23H31N5O6
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| 分子量 |
473.52
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| 包装储存 |
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| 详情描述 |
Usmarapride (SUVN-D4010) 是一种有效的、具有选择性、口服活性和可透过血脑屏障的 5-HT4 受体部分激动剂 (EC50=nM)。Usmarapride (SUVN-D4010) 可用于阿尔茨海默病相关认知缺陷的研究。
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| 产品详情 |
Usmarapride (SUVN-D4010) 是一种有效的、具有选择性、口服活性和可透过血脑屏障的 5-HT4 受体部分激动剂 (EC50=nM)。Usmarapride (SUVN-D4010) 可用于阿尔茨海默病相关认知缺陷的研究。
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| 生物活性 |
Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT 4 receptor partial agonist (EC 50 =44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimers disease.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
5-HT4 Receptor 44 nM (EC50)
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| 体内研究(In Vivo) |
Usmarapride (SUVN-D4010) (1-3 mg/kg; p.o.; Male Wistar rats 10-12 weeks old) attenuates the long-term memory deficits in object recognition test (ORT).
Usmarapride (1, 3, and 10 mg/kg; p.o.) significantly reverses the scopolamine-induced amnesia.
Usmarapride shows a statistically significant effect at 3.0 mg/kg on both exploration time and recognition index.
Usmarapride (SUVN-D4010) shows good oral exposures, good bioavailability, and good brain exposures in rats.
Pharmacokinetic of Usmarapride in Rats
(3.0 mg/kg for p.o. dosing; 1.0 mg/kg for i.v.)
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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| ClinicalTrial |
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| 参考文献 |
[1]. Nirogi, Ramakrishna; Mohammed, Abdul Rasheed; Yarlgadda, Suresh; Ravella, Srinivasa Rao; Shinde, Anil Karbhari; Kambhampati, Ramasastri; Roayalley, Praveen Kumar; Jayarajan, Pradeep; Bhyrapuneni, Gopinadh; Patnala, Sriramachandra Murthy; et al. Preparatio
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| 溶解度数据 |
In Vitro: DMSO : 33.33 mg/mL (70.39 mM; Need ultrasonic)配制储备液
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[1]. Nirogi, Ramakrishna; Mohammed, Abdul Rasheed; Yarlgadda, Suresh; Ravella, Srinivasa Rao; Shinde, Anil Karbhari; Kambhampati, Ramasastri; Roayalley, Praveen Kumar; Jayarajan, Pradeep; Bhyrapuneni, Gopinadh; Patnala, Sriramachandra Murthy; et al. Preparatio
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。