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Chemical Structure : BMS-687681
Catalog No.: PC-60322Not For Human Use, Lab Use Only.
BMS-687681 (BMS-681) is a potent and orally bioavailable dual antagonist of CCR2 and CCR5 with binding IC50 of 0.7 nM and 2.4 nM, respectively.
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BMS-687681 (BMS-681) is a potent and orally bioavailable dual antagonist of CCR2 and CCR5 with binding IC50 of 0.7 nM and 2.4 nM, respectively.
BMS-681 exhibits high selectivity against other chemokine receptors and GPCRs.
BMS-681 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),
BMS-681 is suitable for use in both murine and monkey models of inflammation.
| M.Wt | 491.603 | |
| Formula | C26H36F3N5O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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.
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