生理活性の詳細Potent and selective CCR1 antagonist (IC50 = 8.4 μM). Ki values are 0.04 nM (CCR1) and >10 nM (CCR5, CXCR2 and CXCR4). Displays inverse agonist activity for US28, a HCMV-encoded receptor. Able to produce concentration-dependent inhibition of MIP-1α and Ca2+ mobilization.
保存方法Store at +4°C. Store under Desiccating conditions. The product can be stored for up to 12 months.
溶解性Soluble in DMSO to 100 mM and in ethanol to 50 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Casarosa P et al. Identification of the first nonpeptidergic inverse agonist for a constitutively active viral-encoded G protein-coupled receptor. J Biol Chem278:5172-8 (2003).
Read more (PubMed: 12456673) »
Hesselgesser J et al. Identification and characterization of small molecule functional antagonists of the CCR1 chemokine receptor. J Biol Chem273:15687-92 (1998).
Read more (PubMed: 9624164) »