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Submit ReviewINCB 3284 dimesylate is a potent, selective hCCR2 antagonist. Exhibits potent antagonism against monocyte chemoattractant molecule binding to hCCR2 and chemotaxis activity (IC50 values are 3.7 and 4.7 nM respectively). Also displays weak hERG activity; inhibits the hERG potassium current (IC50 = 84μ M). Orally bioavailable.
INCB 3284 dimesylate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Antiviral Library. 了解 Tocris 化合物库的更多信息。
分子量 | 712.76 |
公式 | C26H31F3N4O4.2CH4O3S |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 887401-93-6 |
PubChem ID | 11679268 |
InChI Key | PNPNUHKICDECDH-SEBNIYPMSA-N |
Smiles | O=C(NCC(N[C@@H]2CCN([C@H]3CC[C@](C4=CC=C(OC)N=C4)(O)CC3)C2)=O)C1=CC(C(F)(F)F)=CC=C1.CS(=O)(O)=O.CS(=O)(O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 71.28 | 100 | |
DMSO | 71.28 | 100 |
以下数据基于产品分子量 712.76。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.4 mL | 7.01 mL | 14.03 mL |
5 mM | 0.28 mL | 1.4 mL | 2.81 mL |
10 mM | 0.14 mL | 0.7 mL | 1.4 mL |
50 mM | 0.03 mL | 0.14 mL | 0.28 mL |
参考文献是支持产品生物活性的出版物。
Xue et al (2011) Discovery of INCB3284, a potent, selective, and orally bioavailable hCCR2 antagonist. ACS.Med.Chem.Lett. 2 450 PMID: 24900329
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关键词: INCB 3284 dimesylate, INCB 3284 dimesylate supplier, INCB3284, CCR2, antagonist, antagonists, hCCR2, human, chemokine, receptor, receptors, Chemokine, CC, Receptors, 4306, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 INCB 3284 dimesylate 的部分引用包括:
Liu et al (2016) Cancer-associated fibroblasts promote hepatocellular carcinoma metastasis through chemokine-activated hedgehog and TGF-β pathways. Cancer Lett. 379 49 PMID: 27216982
Zhou et al (2015) Klotho gene deficiency causes salt-sensitive hypertension via monocyte chemotactic protein-1/CC chemokine receptor 2-mediated inflammation. Nat Commun 26 121 PMID: 24904083
McMillin et al (2014) Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J Neuroinflammation 11 121 PMID: 25012628
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.