CCR2 antagonist 4 (hydrochloride)
CAS No. : 1313730-14-1
(Synonyms: Teijin compound 1 (hydrochloride))
| Size | Price | Stock |
|---|---|---|
| 5mg | $110 | In-stock |
| 10mg | $180 | In-stock |
| 25mg | $380 | In-stock |
| 50mg | $650 | In-stock |
| 100mg | $1000 | In-stock |
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| Cat. No. : | HY-103362 |
| M.Wt: | 476.32 |
| Formula: | C21H22Cl2F3N3O2 |
| Purity: | >98 % |
| Solubility: | DMSO : 250 mg/mL (524.86 mM; Need ultrasonic) |
CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM[1]. In Vitro: Ile263 and Thr292 in CCR2 contribute significantly to binding of CCR2 antagonist 4 in CCR2. Residue Glu291 in TM7, a highly conserved residue in many CC chemokine receptors, contributes substantially to binding of the protonated CCR2 antagonist 4 hydrochloride, and CCL2. His121 on TM3 and Ile263 on TM6 also strongly interact with CCR2 antagonist 4 hydrochloride[2]. In Vivo: In ApoE-deficient mice, Vp-TSL targets specifically aortic plaque endothelial VCAM-1 and CCR2 antagonist 4 hydrochloride reduces the mouse monocyte/macrophage cell line (RAW 264.7) adhesion/ infiltration into the aorta[3].
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