BMS-681 is an orthosteric antagonist of chemokine receptor 2 (CCR2) that forms a ternary complex with CCR2 and its allosteric antagonist, CCR2-RA-[R]. Together, the complex inhibits chemokine binding with BVMS-681 in the orthosteric pocket and CCR2-RA-[R] in the intracellular allosteric G-protein binding site. When chemokine binding is inhibited, modulation responses implicated in several inflammatory and neurodegenerative diseases, including atherosclerosis, multiple sclerosis, asthma, neuropathic pain, diabetic nephropathy, and cancer can be controlled. This action occurs as the migration of monocytes, immature dendritic cells, and T-cell subpopulations towards endogenous CC chemokine ligands is mediated.
MedKoo Cat#: 571514
Name: BMS-681
CAS#: 2760844-13-9
Chemical Formula: C26H36F3N5O
Exact Mass: 491.2872
Molecular Weight: 491.60
Elemental Analysis: C, 63.52; H, 7.38; F, 11.59; N, 14.25; O, 3.25
The following data is based on the product molecular weight 491.60 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
