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Complement factor D-IN-1

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Catalog No. T16898Cas No. 1386455-76-0

Complement factor D-IN-1 is a potent and selective small-molecule reversible Factor D inhibitor, with IC50 values of 0.006 μM in the FD Thioesterolytic Fluorescent Assay and 0.05 μM in the MAC Deposition Assay.

Complement factor D-IN-1

Complement factor D-IN-1

Copy Product Info
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Catalog No. T16898Cas No. 1386455-76-0
Complement factor D-IN-1 is a potent and selective small-molecule reversible Factor D inhibitor, with IC50 values of 0.006 μM in the FD Thioesterolytic Fluorescent Assay and 0.05 μM in the MAC Deposition Assay.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$1,1007-10 days7-10 days
10 mg$1,4987-10 days7-10 days
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Product Introduction

Bioactivity
Description
Complement factor D-IN-1 is a potent and selective small-molecule reversible Factor D inhibitor, with IC50 values of 0.006 μM in the FD Thioesterolytic Fluorescent Assay and 0.05 μM in the MAC Deposition Assay.
Targets&IC50
MAC:0.05 μM, FD:0.006 μM
In vitro
Complement factor D-IN-1 displays similar potency against human and monkey FD (IC50s: 0.005 μM in FD thioesterolytic assays and 0.011 μM in 50% serum MAC deposition assays for both human and monkey) [1].
In vivo
Complement factor D-IN-1 shows an excellent oral PK profile in Sprague–Dawley rats and, following an oral dose (10 mg/kg) in Brown Norway rats, demonstrates a good distribution and sustained exposure in ocular tissues including the neural retina. Mean exposure levels in plasma, the PEC, and the retina at 6 h after dosing are 0.36, 0.43, and 0.09 μM, respectively [1].
Chemical Properties
Molecular Weight483.32
FormulaC21H19BrN6O3
Cas No.1386455-76-0
SmilesNC(=O)c1nn(CC(=O)N2[C@@H]3C[C@@H]3C[C@H]2C(=O)Nc2cccc(Br)n2)c2ccccc12
Relative Density.1.82 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 250 mg/mL (517.26 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (6.83 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0690 mL10.3451 mL20.6902 mL103.4511 mL
5 mM0.4138 mL2.0690 mL4.1380 mL20.6902 mL
10 mM0.2069 mL1.0345 mL2.0690 mL10.3451 mL
20 mM0.1035 mL0.5173 mL1.0345 mL5.1726 mL
50 mM0.0414 mL0.2069 mL0.4138 mL2.0690 mL
100 mM0.0207 mL0.1035 mL0.2069 mL1.0345 mL

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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:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 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 DMSOTargetMol | reagent 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | reagent 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.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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

Keywords

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