CP-481715 

CP-481715 is a potent, reversible and selective CCR1 antagonist with a K_d of 9.2 nM for human CCR1. CP-481715 is >100-fold selective for CCR1 as compared with a panel of G-protein-coupled receptors including related chemokine receptors. CP-481715 has the potential for rheumatoid arthritis and other inflammatory diseases research^[1].

CP-481715 displaces ¹²⁵I-labeled CCL3 from CCR1-transfected cells with an IC₅₀ of 74 nM^[1].
CP-481715 lacks intrinsic agonist activity but 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 MMP9 release (IC₅₀ = 54 nM)^[1].
CP-481715 retains activity in human whole blood, inhibiting CCL3-induced CD11b up-regulation and actin polymerization (IC₅₀ = 165 and 57 nM, respectively) on monocytes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

482.55

C₂₆H₃₁FN₄O₄

212790-31-3

O=C(C1=NC2=CC=CC=C2N=C1)N[C@@H](CC3=CC=CC(F)=C3)[C@@H](O)C[C@H](C(N)=O)CCC(C)(O)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Gladue RP, Tylaska LA, Brissette WH, Lira PD, Kath JC, Poss CS, Brown MF, Paradis TJ, Conklyn MJ, Ogborne KT, McGlynn MA, Lillie BM, DiRico AP, Mairs EN, McElroy EB, Martin WH, Stock IA, Shepard RM, Showell HJ, Neote K.CP-481,715, a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases.J Biol Chem. 2003 Oct 17;278(42):40473-80. Epub 2003 Aug 7.  [Content Brief]

  [2]. Borregaard J, Skov L, Wang L, Ting N, Wang C, Beck LA, Sonne J, Clucas A.Evaluation of the effect of the specific CCR1 antagonist CP-481715 on the clinical and cellular responses observed following epicutaneous nickel challenge in human subjects.Contact Dermatitis. 2008 Oct;59(4):212-9.  [Content Brief]

  [3]. Gladue RP, Cole SH, Roach ML, Tylaska LA, Nelson RT, Shepard RM, McNeish JD, Ogborne KT, Neote KS.The human specific CCR1 antagonist CP-481,715 inhibits cell infiltration and inflammatory responses in human CCR1 transgenic mice.J Immunol. 2006 Mar 1;176(5):3141-8.  [Content Brief]

  [4]. Ronald P Gladue, et al. CP-481,715, a potent and selective CCR1 antagonist with potential therapeutic implications for inflammatory diseases. J Biol Chem. 2003 Oct 17;278(42):40473-80.  [Content Brief]