CAS NO: | 887401-92-5 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | INCB 3284 is a potent, selective and orally bioavailable humanCCR2antagonist, inhibiting monocyte chemoattractant protein-1 binding tohCCR2, with anIC50of 3.7 nM. INCB 3284 can be used in the research of acute liver failure. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | INCB 3284 is a pentent, selective and orally bioavailable human CCR2 antagonist, inhibiting monocyte chemoattractant protein-1 binding to hCCR2, with an IC50of 3.7 nM. INCB 3284 also causes an IC50of 4.7 nM in antagonism of chemotaxis activity, an IC50of 84 μM in inhibition of the hERG potassium current. However, INCB 3284 has no effec on CCR1, CCR3, CCR5, CXCR3, and CXCR5, or additional GPCRs at a concentration of 1 μM. Moreover, INCB 3284 potently inhibits CCR2-mediated signaling events such as intracellular calcium mobilization and ERK phosphorylation with IC50values of 6 and 2.6 nM, respectively[1]. | ||||||||||||||||
体内研究 (In Vivo) | INCB 3284 (1 mg/kg/day, ip) reduces liver damage, and decreases microglia activation in AOM-treated mice via inhibition on CCR2. INCB 3284 also significantly reduces the pERK1/2 to tERK1/2 ratio, as well as G-protein signaling pathway activity and proinflammatory cytokine production in cortex lysates from mice administed with azoxymethane[2]. | ||||||||||||||||
分子量 | 520.54 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C26H31F3N4O4 | ||||||||||||||||
CAS 号 | 887401-92-5 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : ≥ 83.3 mg/mL(160.03 mM) H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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