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LB244

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Catalog No. T79730Cas No. 3074622-05-9
Alias LB-244, LB 244

LB244 is a homologue of BB-Cl-amidine and functions as an orally effective STING inhibitor with an EC50 value of 0.8 μM, capable of suppressing STING-dependent inflammatory signaling, although pharmacokinetic studies indicate limited oral activity in mice, making it a useful tool for mechanistic investigations of innate immunity and inflammatory disease models.

LB244

LB244

😃Good
Catalog No. T79730Alias LB-244, LB 244Cas No. 3074622-05-9
LB244 is a homologue of BB-Cl-amidine and functions as an orally effective STING inhibitor with an EC50 value of 0.8 μM, capable of suppressing STING-dependent inflammatory signaling, although pharmacokinetic studies indicate limited oral activity in mice, making it a useful tool for mechanistic investigations of innate immunity and inflammatory disease models.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$28735 days35 days
5 mg$1,29035 days35 days
10 mg$2,29035 days35 days
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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
LB244 is a homologue of BB-Cl-amidine and functions as an orally effective STING inhibitor with an EC50 value of 0.8 μM, capable of suppressing STING-dependent inflammatory signaling, although pharmacokinetic studies indicate limited oral activity in mice, making it a useful tool for mechanistic investigations of innate immunity and inflammatory disease models.
Targets&IC50
STING:0.8 - 4.5 μM
In vitro
In cellular assays using human THP-1 monocytes and murine macrophages, the cells were stimulated with the cyclic dinucleotide agonist 2'3'-cGAMP to activate the pathway. LB244 was applied at concentrations corresponding to an IC50 range of 0.8 to 4.5 μM [1].
In vivo
Pharmacokinetic profiling was conducted in mice to evaluate the systemic properties of the compound. LB244 was administered via oral gavage (10 mg/kg) or intraperitoneal injection (5 mg/kg). Blood samples were analyzed to determine metabolic parameters, revealing a systemic clearance of 2854.3 mL/min/kg and a half-life (T1/2) of 2.8 hours. Following oral administration, the plasma analysis detected a maximal concentration (Cmax) of 0.04 uM [1].
SynonymsLB-244, LB 244
Chemical Properties
Molecular Weight537.57
FormulaC30H27N5O5
Cas No.3074622-05-9
SmilesO=C(C1=CC=C(C2=CC=CC=C2)C=C1)N[C@H](C3=NC4=CC=CC=C4N3)CCCCNC(C5=CC=C([N+]([O-])=O)O5)=O
Storage & Solubility Information
Storagestore at low temperature | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 80 mg/mL (148.82 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8602 mL9.3011 mL18.6022 mL93.0111 mL
5 mM0.3720 mL1.8602 mL3.7204 mL18.6022 mL
10 mM0.1860 mL0.9301 mL1.8602 mL9.3011 mL
20 mM0.0930 mL0.4651 mL0.9301 mL4.6506 mL
50 mM0.0372 mL0.1860 mL0.3720 mL1.8602 mL
100 mM0.0186 mL0.0930 mL0.1860 mL0.9301 mL

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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:
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2 Enter the in vivo formulation:
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