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Complement C1s-IN-1
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Catalog No. T74816Cas No. 3033831-40-9
Complement C1s-IN-1 is a potent and selective inhibitor of complement C1s with the advantage of being orally available and brain penetrable, significantly inhibiting human serum-induced formation of membrane attack complexes in a dose-dependent manner and effectively blocking the classical complement pathway
Complement C1s-IN-1
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Purity: 97.77%
Catalog No. T74816Cas No. 3033831-40-9
Complement C1s-IN-1 is a potent and selective inhibitor of complement C1s with the advantage of being orally available and brain penetrable, significantly inhibiting human serum-induced formation of membrane attack complexes in a dose-dependent manner and effectively blocking the classical complement pathway
| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $1,130 | - | In Stock | |
| 5 mg | $2,270 | - | In Stock |
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Batch Information
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Purity:97.77%
ee:97.68%
Appearance:Solid
Color:Yellow
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Complement C1s-IN-1 is a potent and selective inhibitor of complement C1s with the advantage of being orally available and brain penetrable, significantly inhibiting human serum-induced formation of membrane attack complexes in a dose-dependent manner and effectively blocking the classical complement pathway |
| Targets&IC50 | C1s (mouse):61 nM, Other serine proteases:>30,000 nM, C1s (human):36 nM |
| In vitro | Complement C1s-IN-1 (compound (R)-8) is a highly selective C1s inhibitor with an IC₅₀ of 36 nM for human C1s and 61 nM for mouse C1s. Complement C1s-IN-1 showed minimal activity against other serine proteases (IC₅₀ > 30,000 nM). Complement C1s-IN-1 also dose-dependently inhibited serum-induced classical complement pathway activation in vitro[1]. |
| In vivo | Following oral administration in mice (10–100 mg/kg), Complement C1s-IN-1 showed dose-dependent plasma exposure (Cmax up to 8895.5 ng/mL; AUC₀–₂₄h = 139,341 ng·h/mL) with a mean residence time of 7.66 h. Complement C1s-IN-1 exhibited strong brain penetration, with brain concentrations reaching 33,559.5 ng/g at 2 h and a brain/plasma ratio up to 1.7[1]. |
| Molecular Weight | 422.43 |
| Formula | C22H20F2N6O |
| Cas No. | 3033831-40-9 |
| Smiles | CC1=CC([C@@H]2N(CCN(C2)C3=CC4=C(C(F)=C3)C(N)=NN=C4)C5=CC(F)=CC=C5)=NO1 |
| Relative Density. | no data available |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
Dose Conversion
You can also refer to dose conversion for different animals. More Dose Conversion
Tech Support
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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