CAS NO: | 608141-41-9 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotidephosphodiesterase(PDE-4) with anIC50of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50of 104 nM[1]. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | Apremilast (CC-10004) inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50of 104 nM (pIC50=6.98±0.2), which almost exactly replicates previous reported TNF-α inhibition by Apremilast on peripheral blood mononuclear cells (PBMCs) (IC50=110 nM) and which is similar to the potency of Apremilast for PDE4 enzymatic inhibition (IC50=74 nM). These results are clearly consistent with the hypothesis that Apremilast inhibits TNF-α by increasing intracellular cAMP levels. PKA, Epac1 and Epac2 knockdowns prevented TNF-α inhibition and IL-10 stimulation by Apremilast[1]. | ||||||||||||||||
体内研究 (In Vivo) | Apremilast (CC-10004), orally administered (5 mg/kg), significantly inhibits TNF-α production in the air pouch by 39 % (61±6 % of vehicle, P<0.001) and diminishes (by 28 %) the number of leukocytes present (72±12 % of vehicle, P<0.05). In agreement, immunohistologic analysis shows that neutrophil accumulation in the air pouch membrane is dramatically reduced by Apremilast. In the murine air pouch model, both Apremilast and methotrexate (MTX) significantly inhibit leukocyte infiltration, while Apremilast, but not MTX, significantly inhibits TNF-α release. The addition of MTX (1 mg/kg) to Apremilast (5 mg/kg) yields no more inhibition of leukocyte infiltration or TNF-α release than with Apremilast alone[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 460.50 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C22H24N2O7S | ||||||||||||||||
CAS 号 | 608141-41-9 | ||||||||||||||||
中文名称 | 阿普司特 | ||||||||||||||||
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 : 44 mg/mL(95.55 mM;Need ultrasonic) 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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