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CAS No.: 1903768-17-1

Danicopan Catalog No. CSN25566

Synonyms: ACH-4471;ACH-0144471

Danicopan is selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with Kd value of 0.54 nM. It has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS).

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技术信息

生物活性

描述The complement system provides an important defense against bacteria, fungi, and viruses. Complement factor D (CFD) is a specific serine protease that cleaves its unique substrate and is a promising therapeutic target to treat paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS). Danicopan (ACH-4471) is selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with Kd value of 0.54 nM. ACH-4471 potently inhibited hemolysis with IC50 values ranging from 0.0040 μM to 0.027 μM, and blocked the APC-mediated killing by aHUS patient sera at sub-micromolar concentrations, which indicates ACH-4471 has the potential as oral therapeutics for human diseases driven by the alternative pathway of complement, including aHUS^[1]. In a second study in PNH patients with poor response to eculizumab (defined as the need of red blood cell transfusion), ACH-4471 was given as add-on treatment on top of standard eculizumab at three different doses (100, 150, or 200 mg thrice a day)^[2].
参考文献

[1] Yuan X, Gavriilaki E, Thanassi JA, et al. Small-molecule factor D inhibitors selectively block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria and atypical hemolytic uremic syndrome. Haematologica. 2017;102(3):466-475.
[2] A Treatment Study of ACH-0144471 in Patients With Paroxysmal Nocturnal Hemoglobinuria (PNH) With Inadequate Response to Eculizumab (PNH)

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7229 mL
- 8.6146 mL
- 17.2293 mL
- 5 mM
- 0.3446 mL
- 1.7229 mL
- 3.4459 mL
- 10 mM
- 0.1723 mL
- 0.8615 mL
- 1.7229 mL

技术信息

CAS号

1903768-17-1

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C26H23BrFN7O3

运输

蓝冰

分子量

580.41

别名

ACH-4471;ACH-0144471

溶解度

DMSO	98.0 mg/mL (168.8 mM)
Water	Insoluble
Ethanol	Insoluble

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