NPS 2390

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Chemical Structure| 226878-01-9 同义名 : -
CAS号 : 226878-01-9
货号 : A839361
分子式 : C19H21N3O
纯度 : 99%+
分子量 : 307.39
MDL号 : MFCD05865239
存储条件:

Pure form Sealed in dry, room temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 NPS 2390 is a group I mGlu antagonist; displays noncompetitive antagonist activity at both mGlu1 and mGlu5 receptors. Thought to act on a site separate from the glutamate binding pocket. GdCl(3), an activator of CaR, and NPS-2390, a specific inhibitor, were administered. The PC and PC (post-conditioning) with NPS-2390 groups improved the recovery of cardiac function during reperfusion compared to the IR and PC groups with GdCl(3), respectively[1]. The intracellular calcium concentration ([Ca(2+)](i)) was increased by an increment of [Ca(2+)](o). This [Ca(2+)](i) increment was inhibited by the pretreatment with NPS 2390, an antagonist of CaSR (calcium sensing receptor)[2]. Calcium oxalate increased OS, crystal adhesion, PS ectropion, and the expression of CaSR and ERK, OPN, and KIM-1 in vivo. In addition, lower levels of urine citrate as well as increased serum creatinine and urea levels were observed after treatment with calcium oxalate (p < .05). Compared with calcium oxalate treatment alone, the above deleterious changes were further significantly confirmed by GdCl3 but were reversed by NPS-2390. However, urine calcium excretion was decreased after ethylene glycol treatment but was significantly reduced by NPS 2390 and increased by GdCl3 (p < .05)[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.25mL

0.65mL

0.33mL

16.27mL

3.25mL

1.63mL

32.53mL

6.51mL

3.25mL

参考文献

[1]Gan R, Hu G, Zhao Y, Li H, Jin Z, Ren H, Dong S, Zhong X, Li H, Yang B, Xu C, Lu F, Zhang W. Post-conditioning protecting rat cardiomyocytes from apoptosis via attenuating calcium-sensing receptor-induced endo(sarco)plasmic reticulum stress. Mol Cell Biochem. 2012 Feb;361(1-2):123-34

[2]Jung SY, Kwak JO, Kim HW, Kim DS, Ryu SD, Ko CB, Cha SH. Calcium sensing receptor forms complex with and is up-regulated by caveolin-1 in cultured human osteosarcoma (Saos-2) cells. Exp Mol Med. 2005 Apr 30;37(2):91-100

[3]Li X, Chen S, Feng D, Fu Y, Wu H, Lu J, Bao J. Calcium-sensing receptor promotes calcium oxalate crystal adhesion and renal injury in Wistar rats by promoting ROS production and subsequent regulation of PS ectropion, OPN, KIM-1, and ERK expression. Ren Fail. 2021 Dec;43(1):465-476