For research use only. Not for therapeutic Use.
Danicopan (ACH-4471), a selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with Kd value of 0.54 nM. Danicopan (ACH-4471) inhibits alternative pathway of complement (APC) activity, has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS)[1].
Danicopan (ACH-4471) inhibits the proteolytic activity of purified Factor D against its natural substrate Factor B in complex with C3b, blocking production of Bb fragment in a dose-dependent manner with an IC50 value of 0.015 μM[1].?
Danicopan (ACH-4471) potently inhibits hemolysis with IC50 values ranging from 0.0040 μM to 0.027 μM (IC90 values from 0.015 μM to 0.11 μM)[1].
| Catalog Number | I017972 |
| CAS Number | 1903768-17-1 |
| Synonyms | (2S,4R)-1-[2-[3-acetyl-5-(2-methylpyrimidin-5-yl)indazol-1-yl]acetyl]-N-(6-bromopyridin-2-yl)-4-fluoropyrrolidine-2-carboxamide |
| Molecular Formula | C26H23BrFN7O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C26H23BrFN7O3/c1-14(36)25-19-8-16(17-10-29-15(2)30-11-17)6-7-20(19)35(33-25)13-24(37)34-12-18(28)9-21(34)26(38)32-23-5-3-4-22(27)31-23/h3-8,10-11,18,21H,9,12-13H2,1-2H3,(H,31,32,38)/t18-,21+/m1/s1 |
| InChIKey | PIBARDGJJAGJAJ-NQIIRXRSSA-N |
| SMILES | CC1=NC=C(C=N1)C2=CC3=C(C=C2)N(N=C3C(=O)C)CC(=O)N4CC(CC4C(=O)NC5=NC(=CC=C5)Br)F |
| Reference | [1]. Yuan X, 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 Mar;102(3):466-475. [2]. Boyer DD, Ko YP, Podos SD, et al. Danicopan, an Oral Complement Factor D Inhibitor, Exhibits High and Sustained Exposure in Ocular Tissues in Preclinical Studies. Transl Vis Sci Technol. 2022;11(10):37. |
