CCR2-RA-[R]
CAS No. : 512177-83-2
| Size | Price | Stock |
|---|---|---|
| 5mg | $80 | In-stock |
| 10mg | $120 | In-stock |
| 25mg | $240 | In-stock |
| 50mg | $390 | In-stock |
| 100mg | $540 | In-stock |
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| Cat. No. : | HY-50081 |
| M.Wt: | 351.80 |
| Formula: | C18H19ClFNO3 |
| Purity: | >98 % |
| Solubility: | DMSO : 37.5 mg/mL (ultrasonic;warming;heat to 60°C) |
CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC50 of 103 nM. IC50 & Target: IC50: 103 nM (CCR2)[1] In Vitro: The chemokine receptor CCR2 is a G protein-coupled receptor that is involved in many diseases characterized by chronic inflammation, and therefore a large variety of CCR2 small molecule antagonists has been developed. CCR2-RA-[R] displaces [125I]CCL2 from CCR2 with an pIC50 value of 6.1. The pKD of CCR2-RA-[R] for CCR2 and CCR5 is 8.8±0.1 and 7.0±0.1, respectively[2]. CCR2-RA-[R] inhibits CCR2 non-competitively by blocking activation-associated conformational changes and formation of the G protein-binding interface. The binding pocket of CCR2-RA-[R] is highly enclosed and possesses a balanced combination of hydrophobic and polar features, all of which favors pocket “druggability”[3].
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