| 產品描述： | RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 89 nM and > 100 μM for inhibition of human recombinant CCR2 and CCR1 receptors respectively). |
| 靶點： |
CCR2：89 nM (IC50)；Human α1a receptor：72 nM (IC50)；Human α1d receptor：460 nM (IC50)；5HT-1a receptor：1070 nM (IC50);CCR |
| 體內研究： |
RS504393 (0.3-3 μg) with CCL2 progressively blocks thermal hyperalgesia dose-dependently in mice. RS 504393 (5 mg/kg, i.v.) supresses the elevated numbers of leukocytes and increased total protein content in BALF induced by The LPS. RS504393 significantly down regulates the LPS-induced elevation of IL-1β, PAI-1 mRNA and protein expressions. RS504393 significantly suppresses induced lung edema, protein-rich fluid, polymorphonuclear accumulation and bronchial wall thickening induced by LPS. RS-504393 significantly reduces renal pathology, especially the extensive interstitial fibrosis mediated by decrease in type I collagen synthesis in a UUO mode |
| 參考文獻： |
1. Baamonde, Ana., et al. Involvement of glutamate NMDA and AMPA receptors, glial cells and IL-1β in the spinal hyperalgesia evoked by the chemokine CCL2 in mice. Neuroscience Letters (2011), 502(3), 178-181. 2. Yang, Dong., et al. Roles of CC chemokine receptors (CCRs) on lipopolysaccharide-induced acute lung injury. Respiratory Physiology & Neurobiology (2010), 170(3), 253-259. 3. Kitagawa, Kiyoki., et al. Blockade of CCR2 ameliorates progressive fibrosis in kidney. American Journal of Pathology (2004), 165(1), 237-246. 4. Tominaga T, et al. Blocking mast cell-mediated type I hypersensitivity in experimental allergic conjunctivitis by monocyte chemoattractant protein-1/CCR2. Invest Ophthalmol Vis Sci. 2009 Nov;50(11):5181-8. 5. Mirzadegan T, et al. Identification of the binding site for a novel class of CCR2b chemokine receptor antagonists: binding to a common chemokine receptor motif within the helical bundle. J Biol Chem. 2000 Aug 18;275(33):25562-71. |
| 溶解性： |
Soluble in DMSO |
| 保存條件： |
2-8℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.395 ml |
11.976 ml |
23.952 ml |
| 5 mM |
0.479 ml |
2.395 ml |
4.79 ml |
| 10 mM |
0.24 ml |
1.198 ml |
2.395 ml |
| 50 mM |
0.048 ml |
0.24 ml |
0.479 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）
營業執照(三證合一)
北京