| Chemical Properties | Back Directory | [Melting point ]
148-150 °C | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [color ]
white to beige | [InChIKey]
FOAFBMYSXIGAOX-MUMZCOSOSA-N |
| Hazard Information | Back Directory | [Uses]
trans-J-113863 is a potent chemokine CCR1 and CCR3 receptor antagonist, and inhibits MIP-1α-induced chemotaxis in CCR1 transfectants and eotaxin-induced chemotaxis in CCR3 transfectants with IC50 of 9.57 and 93.8 nM,respectively[1][2]. | [Biological Activity]
UCB35625 is a high affinity antagonist for CCR1 and CCR3 receptors. Also both UCB35625 and its enantiomer J113863 exhibit low binding affinity toward CCR2 and CCR5 where they activate three Gi and two G0 protein isoforms. UCB35625 does not activate G12 protein isoform. J113863 binding to CCR2 and CCR5 induce the recruitment of b-arrestin 2 whereas UCB35625 did not. J113863 and UCB35625 are biased ligands for the chemokine receptors CCR2 and CCR5. | [References]
[1] Sabroe I, et al. A small molecule antagonist of chemokine receptors CCR1 and CCR3. Potent inhibition of eosinophil function and CCR3-mediated HIV-1 entry. J Biol Chem. 2000;275(34):25985-25992. DOI:10.1074/jbc.M908864199
[2] de Mendon?a FL, et al. Site-directed mutagenesis of CC chemokine receptor 1 reveals the mechanism of action of UCB 35625, a small molecule chemokine receptor antagonist. J Biol Chem. 2005;280(6):4808-4816. DOI:10.1074/jbc.M412267200 |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
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