Danicopan
Based on 5 publication(s) in Google Scholar
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).
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- Purity: 99.91%
- CAS No.: 1903768-17-1
- 화학식: C26H23BrFN7O3
- 분자량:580.41
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Danicopan
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Cell Proliferation/Viability Assay
Biological Activity
Kd: 0.54 nM (Factor D)[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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1903768-17-1
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Appearance Solid
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분자량 580.41
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화학식 C26H23BrFN7O3
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Color White to off-white
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SMILES
O=C([C@H]1N(C(CN2N=C(C(C)=O)C3=C2C=CC(C4=CN=C(C)N=C4)=C3)=O)C[C@H](F)C1)NC5=NC(Br)=CC=C5
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Synonyms
ACH-4471
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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Bone Res
Targeting adipocyte ESRRA alleviates osteoarthritis via interrupting inter-organelle crosstalk of complement C3-CFD-MAC cascade. [Abstract]2026 Apr 29;14(1):49. PMID: 42056078 -
Front Immunol
Factor D Inhibition Blocks Complement Activation Induced by Mutant Factor B Associated With Atypical Hemolytic Uremic Syndrome and Membranoproliferative Glomerulonephritis. [Abstract]2021 Jun 10:12:690821. PMID: 34177949 -
Cancers (Basel)
Complement Factor D Is a Novel Biomarker and Putative Therapeutic Target in Cutaneous Squamous Cell Carcinoma. [Abstract]2022 Jan 8;14(2):305. PMID: 35053469
Danicopan purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2022 Jan 8;14(2):305. [Abstract]
cSCC cell cultures (UT-SCC-12A) were treated with a small-molecule factor D inhibitor (danicopan; ACH-4471) or DMSO as vehicle control for 24 h. The levels of complement factor B (FB) and its 60 kDa cleavage derivative in conditioned media of cSCC cells were determined by Western blot analysis.
Danicopan purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2022 Jan 8;14(2):305. [Abstract]
cSCC cells (UT-SCC-12A) with high basal FD expression levels were treated with small molecule FD inhibitors (danicopan; ACH-4471) or DMSO. Targeted inhibition of FD significantly suppressed cell proliferation.
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Dis Colon Rectum
Combinatorial Inhibition of Complement Factor D and BCL2 for Early-Onset Colorectal Cancer. [Abstract]2024 Jul 1;67(7):940-950. PMID: 38479005 -
bioRxiv
2025 Mar 28:2025.03.27.645793. PMID: 40196588
용액&용해도
DMSO : 125 mg/mL (215.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7229 mL | 8.6146 mL | 17.2292 mL | 43.0730 mL |
| 5 mM | 0.3446 mL | 1.7229 mL | 3.4458 mL | 8.6146 mL | |
| 10 mM | 0.1723 mL | 0.8615 mL | 1.7229 mL | 4.3073 mL | |
| 15 mM | 0.1149 mL | 0.5743 mL | 1.1486 mL | 2.8715 mL | |
| 20 mM | 0.0861 mL | 0.4307 mL | 0.8615 mL | 2.1537 mL | |
| 25 mM | 0.0689 mL | 0.3446 mL | 0.6892 mL | 1.7229 mL | |
| 30 mM | 0.0574 mL | 0.2872 mL | 0.5743 mL | 1.4358 mL | |
| 40 mM | 0.0431 mL | 0.2154 mL | 0.4307 mL | 1.0768 mL | |
| 50 mM | 0.0345 mL | 0.1723 mL | 0.3446 mL | 0.8615 mL | |
| 60 mM | 0.0287 mL | 0.1436 mL | 0.2872 mL | 0.7179 mL | |
| 80 mM | 0.0215 mL | 0.1077 mL | 0.2154 mL | 0.5384 mL | |
| 100 mM | 0.0172 mL | 0.0861 mL | 0.1723 mL | 0.4307 mL |
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