貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S86563-5mg	99.8%	￥160.00 S86563-5mg ￥160.00 現(xiàn)貨	6 6	-	-	-
S86563-10mg	99.8%	￥260.00 S86563-10mg ￥260.00 現(xiàn)貨	9 9	-	-	-
S86563-25mg	99.8%	￥490.00 S86563-25mg ￥490.00 現(xiàn)貨	6 6	-	-	-

產(chǎn)品介紹

Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM

產(chǎn)品描述：

Basimglurant (RG7090) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM

靶點(diǎn)：

mGlu5 Receptor:1.1 nM (Kd);GluR

體外研究：

[3H]-basimglurant saturation analysis on recombinant human mGlu5 reveals monophasic saturation isotherms with Kd?of 1.1 nM. In competition binding experiments on human recombinant mGlu5, Basimglurant (RG7090) fully displaces [3H]-MPEP with a Ki?of 35.6 nM and [3H]-ABP688 with a Ki?of 1.4 nM. In HEK293 cells stably expressing human mGlu5, Basimglurant (RG7090) inhibits quisqualate induced Ca2+?mobilization with an IC50?of 7.0 nM and [3H]-inositolphosphate accumulation with an IC50?of 5.9 nM. Basimglurant (RG7090) shows similar potencies in radioligand binding and functional assay on human and rodent mGlu5 receptor orthologues

體內(nèi)研究：

Basimglurant (RG7090) is a potent, selective, and safe mGlu5 inhibitor with good oral bioavailability and long half-life supportive of once-daily administration, good brain penetration, and high in vivo potency. It has antidepressant properties which are corroborated by its functional magnetic imaging (fMRI) profile, as well as anxiolytic-like and antinociceptive features. It is currently in phase II clinical studies for the treatment of depression and fragile X syndrome. In the Vogel conflict drinking test, Basimglurant dose dependently increases the drinking time. The total plasma exposure of efficacious doses of Basimglurant (RG7090) ranges from 5 ng/mL (0.03 mg/kg) to 37 ng/mL (0.3 mg/kg)

參考文獻(xiàn)：

1. Lindemann L, et al. Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression. J Pharmacol Exp Ther. 2015 Apr;353(1):213-33. 2. Jaeschke G, et al. Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases. J Med Chem. 2015 Feb 12;58(3):1358-71.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	3.07 ml	15.348 ml	30.697 ml
5 mM	0.614 ml	3.07 ml	6.139 ml
10 mM	0.307 ml	1.535 ml	3.07 ml
50 mM	0.061 ml	0.307 ml	0.614 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

質(zhì)檢證書(COA)

輸入產(chǎn)品批號(hào)：

如何獲取質(zhì)檢證書(COA)?

請(qǐng)輸入貨號(hào)和一個(gè)與之匹配的批號(hào)。
例如:
批號(hào)：JS298415 貨號(hào)：S20001-25g
在貨品標(biāo)簽上如何找到貨號(hào)和批號(hào)?

摩爾濃度計(jì)算器

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

質(zhì)量

濃度

體積

分子摩爾量

計(jì)算重置

玖玖资源网站,爆乳久久久,日韩精品乱码久久久蜜桃,精品呦国产一区二区三区,国产伦高清一区二区三区,sese一区二区,午夜精品福利一区二区三区,三级黄色网站久久免费