| 產品描述： | Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM. Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM) |
| 靶點： |
mGluR1a:60.1 nM (EC50);GluR |
| 體外研究： |
In the Purkinje cells of rat cerebellar slices, Ro 67-7476 increases the amplitude of mGluR1 excitatory postsynaptic potentials (EPSCs) evoked by 2,3-dihydroxy-6-nitro-7-sulfamoylbenzoquionxaline, picrotoxin, or AP5. Ro 67-7476 activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM). The EC50 value of full P-ERK1/2 activation for Ro 67-7476 are nearly identical to the EC50 for calcium mobilization potentiation. Ro 67-7476 increases basal cAMP production approximately by 8%. It potentiated threshold responses to glutamate in the cAMP accumulation assay, with an EC50 value of 17.7 μM |
| 參考文獻： |
1. F Knoflach, et al. Positive allosteric modulators of metabotropic glutamate 1 receptor: characterization, mechanism of action, and binding site. Proc Natl Acad Sci U S A. 2001 Nov 6;98(23):13402-7 2. Kamondanai Hemstapat, et al. A novel class of positive allosteric modulators of metabotropic glutamate receptor subtype 1 interact with a site distinct from that of negative allosteric modulators. Mol Pharmacol. 2006 Aug;70(2):616-26. 3. Douglas J Sheffler, et al. Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells. Neuropharmacology. 2008 Sep;55(4):419-27 |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
-20℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
3.131 ml |
15.655 ml |
31.309 ml |
| 5 mM |
0.626 ml |
3.131 ml |
6.262 ml |
| 10 mM |
0.313 ml |
1.565 ml |
3.131 ml |
| 50 mM |
0.063 ml |
0.313 ml |
0.626 ml |
|
| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京