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Merck
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Documenti

SML1977

Sigma-Aldrich

J113863, cis isomer

>97% (HPLC)

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C30H37Cl2IN2O2
Numero CAS:
202796-41-6
Peso molecolare:
655.44
Numero MDL:
MFCD09971133
Codice UNSPSC:
12352200
NACRES:
NA.77

Saggio

>97% (HPLC)

Forma fisica

powder

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear

Temperatura di conservazione

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+;
FOAFBMYSXIGAOX-KEKKVSGZSA-N

Azioni biochim/fisiol

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.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable

Certificati d'analisi (COA)

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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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