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 取代了 CCR1 转染细胞中的 ¹²⁵I 标记的 CCL3，IC₅₀ 为 74 nM^[1]。
CP-481715 缺乏内在激动剂活性，但完全阻断了 CCL3 和 CCL5 刺激受体信号传导（Guanosine 5'-O-(thiotriphosphate) ）掺入；IC₅₀ = 210 nM）、钙动员（IC₅₀ = 71 nM）、单核细胞趋化性（IC₅₀ = 55 nM）和 MMP9 释放（IC₅₀ = 54 nM）的能力^[1]。
CP-481715 在人类全血中保持活性，抑制 CCL3 诱导的单核细胞 CD11b 上调和肌动蛋白聚合（IC₅₀ 分别为 165 和 57 nM）^[1]。

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

482.55

C₂₆H₃₁FN₄O₄

212790-31-3

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]