859218-37-4
859218-37-4 structure
- Name: ER-464195-01
- Chemical Name: ER-464195-01
- CAS Number: 859218-37-4
- Molecular Formula: C23H39ClN2
- Molecular Weight: 379.029
- Create Date: 2020-01-12 00:00:50
- Modify Date: 2024-01-27 15:05:35
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ER-464195-01 is a specific, orally active inhibitor that inhibits Calreticulin (CRT) binding to integrin α subunits (ITGAs) with IC50 of 0.17, 0.36, and 0.23 uM in the interaction between CRT and ITGA α4, αL, and αM/α2/α5; dose-dependently and specificly inhibits GST-fused CRT proteins binding to ITGA4 in vitro pull-down assay; inhibits the PMA-induced T cells and the fMLP-stimulated neutrophils bound to VCAM1 (IC50=0.15 μM) and ICAM-1 (IC50=0.19 μM), respectively; suppresses the cell adhesion and the migration of leukocytes, prevents colitis and downregulates the expression of inflammation-related genes in DSS-treated mice, ameliorates the severity of disease in IBD mouse models.
| Name | ER-464195-01 |
|---|
| Description | ER-464195-01 is a specific, orally active inhibitor that inhibits Calreticulin (CRT) binding to integrin α subunits (ITGAs) with IC50 of 0.17, 0.36, and 0.23 uM in the interaction between CRT and ITGA α4, αL, and αM/α2/α5; dose-dependently and specificly inhibits GST-fused CRT proteins binding to ITGA4 in vitro pull-down assay; inhibits the PMA-induced T cells and the fMLP-stimulated neutrophils bound to VCAM1 (IC50=0.15 μM) and ICAM-1 (IC50=0.19 μM), respectively; suppresses the cell adhesion and the migration of leukocytes, prevents colitis and downregulates the expression of inflammation-related genes in DSS-treated mice, ameliorates the severity of disease in IBD mouse models. |
|---|---|
| References | References 1. Ohkuro M, et al. Nat Commun. 2018 May 17;9(1):1982. View Related Products by Target Integrin |
| Molecular Formula | C23H39ClN2 |
|---|---|
| Molecular Weight | 379.029 |