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ER-464195-01 is an orally active inhibitor that targets the interaction between CRT and ITGAs. By disrupting the binding of CRT and ITGAs, ER-464195-01 reduces leukocyte infiltration and subsequent inflammatory cascade reactions. It downregulates the expression of pro-inflammatory genes induced by DSS, such as [TNF-α], [IL-1β], [IL-6], [IL-17f], and inhibits the phosphorylation of STAT3 and the production of serum amyloid A (SAA). This compound is applicable for research in inflammatory bowel disease (IBD).
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | ER-464195-01 is an orally active inhibitor that targets the interaction between CRT and ITGAs. By disrupting the binding of CRT and ITGAs, ER-464195-01 reduces leukocyte infiltration and subsequent inflammatory cascade reactions. It downregulates the expression of pro-inflammatory genes induced by DSS, such as [TNF-α], [IL-1β], [IL-6], [IL-17f], and inhibits the phosphorylation of STAT3 and the production of serum amyloid A (SAA). This compound is applicable for research in inflammatory bowel disease (IBD). |
| In vitro | ER-464195-01 (5 μM) effectively inhibits the interaction between CRT and ITGA4 within Jurkat cells and significantly reduces the level of CRT on the cell surface. Additionally, ER-464195-01 (0.01-10 μM, 60 minutes) suppresses the adhesion capability of VCAM-1 cells stimulated by PMA and ICAM-1 cells stimulated by fMLP, with IC50 values of 0.15 μM and 0.19 μM, respectively, while showing no inhibitory effect under MnCl2 stimulation. |
| In vivo | ER-464195-01, administered orally at 5-10 mg/kg once daily for 6-32 consecutive days, effectively reduces disease severity in mouse models of inflammatory bowel disease (IBD) when used for both prevention and treatment. |
| Molecular Weight | 379.03 |
| Formula | C23H39ClN2 |
| Cas No. | 859218-37-4 |
| Smiles | Cl.C=1C=CC(=C(C1)N2CCN(CC2)CCC)C3CC(C)(C)CC(C)(C)C3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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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