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Danicopan Complement System inhibitor

Name: Danicopan
Brand: Selleck Chemicals
SKU: S0803
Rating: 5 (1 reviews)

Cat.No.S0803

Danicopan is a potent, selective and orally active inhibitor of factor D with Kd of 0.54 nM for human Factor D. This compound inhibits alternative pathway of complement (APC) activity, and has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS).

Chemical Structure

Molecular Weight: 580.41

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Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	PD-1/PD-L1 CXCR STING AhR Immunology & Inflammation related CD markers Interleukins Anti-infection Antioxidant COX
Other Complement System Inhibitors	Compstatin SB290157 trifluoroacetate Phaseoloidin TLQP-21 TFA JR14a Pegcetacoplan acetate

Chemical Information, Storage & Stability

Molecular Weight	580.41	Formula	C₂₆H₂₃BrFN₇O₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1903768-17-1	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ACH-4471, ACH-0144471, ACH-CFDIS, ALXN 2040			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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (172.29 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (8.61mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (8.61mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	alternative pathway of complement (APC) human Factor D (Cell-free assay) 0.54 nM(Kd)
References	[1] https://pubmed.ncbi.nlm.nih.gov/27810992/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05019521	Active not recruiting	Geographic Atrophy	Alexion Pharmaceuticals Inc.	August 23 2021	Phase 2
NCT04469465	Completed	Paroxysmal Nocturnal Hemoglobinuria	Alexion Pharmaceuticals Inc.	December 16 2020	Phase 3
NCT04451434	Completed	Healthy	Alexion Pharmaceuticals Inc.	August 17 2020	Phase 1
NCT04551599	Completed	Healthy	Alexion Pharmaceuticals Inc.	February 21 2020	Phase 1

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Handling Instructions

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