CAS NO: | 1802148-05-5 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | Brensocatib (AZD7986) is an oraldipeptidyl peptidase1(DPP1) inhibitor withpIC50s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, dog and rabbit, respectively[1]. | ||||||||||||||||
IC50& Target | pIC50: 6.85 (human DPP1), 7.6 (mouse DPP1), 7.7 (rat DPP1), 7.8 (dog DPP1), 7.8 (rabbit DPP1)[1] | ||||||||||||||||
体外研究 (In Vitro) | Results from cell assay show that Brensocatib (AZD7986) is a Dipeptidyl peptidase 1 (DPP1) inhibitor with pIC50s of 6.85, 7.6, 7.7, 7.8, and 7.8 in human, mouse, rat, dog and rabbit, respectively. Brensocatib is stable in the propionaldehyde reactivity assay, with a half-life over 50 h. After differentiation in the presence of Brensocatib (38 pM to 10 μM), concentration-dependent decreases in cell lysate enzyme activity are observed for DPP1, as well as for all of the three NSPs, NE, Pr3, and CatG. Brensocatib inhibits activation of all three NSPs in a concentration dependent manner, with pIC50values of around 7 for all three NSPs. The reduction of the activities is almost complete, with NE, Pr3, and CatG activities reduced to 4 to 10% of control at 10 μM Brensocatib[1]. | ||||||||||||||||
体内研究 (In Vivo) | Brensocatib (AZD7986) shows good stability in plasma, with a half life of >10 h. Brensocatib inhibits activation of NE and Pr3, but not CatG, in bone marrow cell lysates in a dose dependent mannerin vivo[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 420.46 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C23H24N4O4 | ||||||||||||||||
CAS 号 | 1802148-05-5 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
| ||||||||||||||||
溶解性数据 | In Vitro: DMSO : ≥ 100 mg/mL(237.83 mM) *"≥" 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
|