CP 481715 a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases. P-481,715 binds to human CCR1 with a Kd of 9.2 nm. and displaces 125I-labeled CCL3 from CCR1-transfected cells with an IC50 of 74 nm. CP-481,715 fully blocks the ability of CCL3 and CCL5 to stimulate receptor signaling (guanosine 5'-O-(thiotriphosphate) incorporation; IC50 = 210 nm), calcium mobilization (IC50 = 71 nm), monocyte chemotaxis (IC50 = 55 nm), and matrix metalloproteinase 9 release (IC50 = 54 nm). CP-481,715 retains activity in human whole blood, inhibiting CCL3-induced CD11b up-regulation and actin polymerization (IC50 = 165 and 57 nm, respectively) on monocytes. CP-481,715 inhibits cell infiltration and inflammatory responses in human CCR1 transgenic mice.
MedKoo Cat#: 524803
Name: CP-481715
CAS#: 212790-31-3
Chemical Formula: C26H31FN4O4
Exact Mass: 482.2329
Molecular Weight: 482.55
Elemental Analysis: C, 64.71; H, 6.48; F, 3.94; N, 11.61; O, 13.26
The following data is based on the product molecular weight 482.55 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 |
