847998-92-9
847998-92-9 structure
- Name: BMS-681
- Chemical Name: BMS-681
- CAS Number: 847998-92-9
- Molecular Formula: C26H36F3N5O
- Molecular Weight: 491.603
- Create Date: 2020-01-20 19:00:57
- Modify Date: 2023-01-11 18:40:10
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A potent and orally bioavailable dual antagonist of CCR2 and CCR5 with binding IC50 of 0.7 nM and 2.4 nM, respectively; exhibits high selectivity against other chemokine receptors and GPCRs; shows CCR2 functional assays of monocyte chemotaxis (IC50=0.24 nM) and CD11b upregulation (whole blood IC50=4.7 nM), CCR5 functional assays of human T-cells (IC50=2.3 nM) and whole blood CCR5-mediated CD11b upregulation (IC50=4.3 nM); suitable for use in both murine and monkey models of inflammation.
| Name | BMS-681 |
|---|
| Description | A potent and orally bioavailable dual antagonist of CCR2 and CCR5 with binding IC50 of 0.7 nM and 2.4 nM, respectively; exhibits high selectivity against other chemokine receptors and GPCRs; shows CCR2 functional assays of monocyte chemotaxis (IC50=0.24 nM) and CD11b upregulation (whole blood IC50=4.7 nM), CCR5 functional assays of human T-cells (IC50=2.3 nM) and whole blood CCR5-mediated CD11b upregulation (IC50=4.3 nM); suitable for use in both murine and monkey models of inflammation. |
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| References | References 1. Zheng Y, et al. Nature. 2016 Dec 15;540(7633):458-461. 2. Carter PH, et al. ACS Med Chem Lett. 2015 Mar 4;6(4):439-44. View Related Products by Target Chemokine Receptor (CCR and CXCR) |
| Molecular Formula | C26H36F3N5O |
|---|---|
| Molecular Weight | 491.603 |