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Danicopan (ALXN2040)

Cat. No. M10145
Danicopan (ALXN2040) Structure
Synonym:

ACH-4471; ACH-0144471; ALXN2040

Size Price Availability Quantity
1mg USD 95  USD95 In stock
5mg USD 220  USD220 In stock
10mg USD 380  USD380 In stock
25mg USD 600  USD600 In stock
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Quality Control & Documentation
Biological Activity

Danicopan (ALXN2040, ACH-4471, ACH-0144471) is a first-in-class, potent, selective, orally active inhibitor of complement factor D  with a Kd value of 0.54 nM for human Factor D. Danicopan can Selectively inhibits key complement factor D in the alternative pathway, blocking C3 convertase production and inhibiting alternative pathway activity. It also prevents the deposition of C3b fragments on blood erythrocytes and inhibits erythrocyte catabolism and extravascular hemolysis.

Chemical Information
Molecular Weight 580.41
Formula C26H23BrFN7O3
CAS Number 1903768-17-1
Solubility (25°C) DMSO 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Antonio M Risitano, et al. Haematologica. Danicopan: an oral complement factor D inhibitor for paroxysmal nocturnal hemoglobinuria

[2] Jason A Wiles, et al. Curr Med Chem. Discovery and Development of the Oral Complement Factor D Inhibitor Danicopan (ACH-4471)

[3] Xuan Yuan, et al. Haematologica. Small-molecule factor D inhibitors selectively block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria and atypical hemolytic uremic syndrome

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Keywords: Danicopan (ALXN2040), ACH-4471; ACH-0144471; ALXN2040 supplier, Complement System, inhibitors, activators


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