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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 Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $287 | 35 days | 35 days | |
| 5 mg | $1,290 | 35 days | 35 days | |
| 10 mg | $2,290 | 35 days | 35 days |
| 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]. |
| Synonyms | LB-244, LB 244 |
| Molecular Weight | 537.57 |
| Formula | C30H27N5O5 |
| Cas No. | 3074622-05-9 |
| Smiles | O=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 | store 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
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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.
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.
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