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Merck
모든 사진(1)

Key Documents

SML1977

Sigma-Aldrich

J113863, cis isomer

>97% (HPLC)

동의어(들):

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

실험식(Hill 표기법):
C30H37Cl2IN2O2
CAS Number:
Molecular Weight:
655.44
MDL number:
UNSPSC 코드:
12352200

분석

>97% (HPLC)

형태

powder

색상

white to beige

solubility

DMSO: 2 mg/mL, clear

저장 온도

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

생화학적/생리학적 작용

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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문서 라이브러리에서 최근에 구매한 제품에 대한 문서를 찾아보세요.

문서 라이브러리 방문

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.
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
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

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