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BI-1230

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Catalog No. T14555Cas No. 849022-32-8

BI-1230 is a potent inhibitor of HCV NS3 protease, exhibiting efficacy in the low nanomolar range, and notably suppresses viral replication. This compound demonstrates high selectivity, distinguishing effectively between other serine/cysteine proteases. Additionally, BI-1230 exhibits favorable pharmacokinetic (PK) properties[1].

BI-1230

BI-1230

😃Good
Catalog No. T14555Cas No. 849022-32-8
BI-1230 is a potent inhibitor of HCV NS3 protease, exhibiting efficacy in the low nanomolar range, and notably suppresses viral replication. This compound demonstrates high selectivity, distinguishing effectively between other serine/cysteine proteases. Additionally, BI-1230 exhibits favorable pharmacokinetic (PK) properties[1].
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25 mg$1,520InquiryInquiry
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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
BI-1230 is a potent inhibitor of HCV NS3 protease, exhibiting efficacy in the low nanomolar range, and notably suppresses viral replication. This compound demonstrates high selectivity, distinguishing effectively between other serine/cysteine proteases. Additionally, BI-1230 exhibits favorable pharmacokinetic (PK) properties[1].
Targets&IC50
HCV NS3 protease:6.7 nM
In vitro
BI-1230 demonstrates potent activity in biochemical and cellular assays. With a 60-minute incubation, it exhibits an IC50 value of 6.7 nM in an enzymatic assay[1]. Over 72 hours, BI-1230 shows EC50 values of 4.6 nM and <1.8 nM in a cell-based HCVPV RNA replication luciferase reporter assay with genotype backgrounds 1a and 1b, respectively, in Huh7 cells.
In vivo
BI-1230 (intravenous?injection; 2 mg/kg) shows good PK activity in rat: CL: 15 ml/min/kg, Mean residence time after iv dose: 2.3 hours, Vss: 2.05 L/kg[1]. BI-1230 (oral administation; 5 mg/kg) shows good PK activity in rat: T1/2: 2.1 hours; Tmax: 1.8 nM; Cmax: 405 nM; AUC0-inf: 2550 nM*h; F: 42%.
Chemical Properties
Molecular Weight816.96
FormulaC42H52N6O9S
Cas No.849022-32-8
SmilesC(O)(=O)[C@]12[C@@](C1)(/C=C\CCCCC[C@H](NC(OC3CCCC3)=O)C(=O)N4[C@](C(=O)N2)(C[C@@H](OC=5C6=C(N=C(C5)C=7N=C(NC(C(C)C)=O)SC7)C(C)=C(OC)C=C6)C4)[H])[H]
Relative Density.1.38 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.

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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

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