SML1977
J113863, cis isomer
>97% (HPLC)
别名:
1,4-cis-1-(1-Cycloocten-1-ylmethyl)-4-[[(2,7-dichloro-9H-xanthen-9-yl)carbonyl]amino]-1-ethylpiperidinium iodide, Piperidinium, 1-(1-cycloocten-1-ylmethyl)-4-[[(2,7-dichloro-9H-xanthen-9-yl)carbonyl]amino]-1-ethyl-, iodide (1:1), cis-
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About This Item
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方案
>97% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
InChI
1S/C30H36Cl2N2O2.HI/c1-2-34(20-21-8-6-4-3-5-7-9-21)16-14-24(15-17-34)33-30(35)29-25-18-22(31)10-12-27(25)36-28-13-11-23(32)19-26(28)29;/h8,10-13,18-19,24,29H,2-7,9,14-17,20H2,1H3;1H/b21-8+;/t24-,34+;
InChI key
FOAFBMYSXIGAOX-KEKKVSGZSA-N
生化/生理作用
High affinity antagonist for CCR1 and CCR3 receptors, agonist at CCR2 and CCR5 receptors
J113863 is a high affinity antagonist for CCR1 and CCR3 receptors. Also both J113863 and its enantiomer c exhibit low binding affinity toward CCR2 and CCR5 where they activate three Gi and two G0 protein isoforms. J113863 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.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
María Llorián-Salvador et al.
Basic & clinical pharmacology & toxicology, 119(1), 32-40 (2015-12-15)
Chemokines are chemotactic cytokines whose involvement in nociceptive processing is being increasingly recognized. Based on the previous description of the involvement of CC chemokine receptor type 1 (CCR1) in pathological pain, we have assessed the participation of CCR1 and its
I Sabroe et al.
The Journal of biological chemistry, 275(34), 25985-25992 (2000-06-16)
We describe a small molecule chemokine receptor antagonist, UCB35625 (the trans-isomer J113863 published by Banyu Pharmaceutical Co., patent WO98/04554), which is a potent, selective inhibitor of CCR1 and CCR3. Nanomolar concentrations of UCB35625 were sufficient to inhibit eosinophil shape change
Jenny Corbisier et al.
The Journal of biological chemistry, 292(2), 575-584 (2016-11-30)
Biased agonism at G protein-coupled receptors constitutes a promising area of research for the identification of new therapeutic molecules. In this study we identified two novel biased ligands for the chemokine receptors CCR2 and CCR5 and characterized their functional properties.
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