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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-KAND567
KAND567

Chemical Structure : KAND567

CAS No.: 911715-90-7

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KAND567 (AZD8797, KAND-567)

货号: PC-21011Not For Human Use, Lab Use Only.

KAND567 (AZD8797) is a potent, selective and orally available C-X3-C motif chemokine receptor 1 (CX3CR1, fractalkine receptor) antagonist with binding Ki of 3.9 nM (human CX3CR1), 720-fold selectivity over CXCR2.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

KAND567 (AZD8797) is a potent, selective and orally available C-X3-C motif chemokine receptor 1 (CX3CR1, fractalkine receptor) antagonist with binding Ki of 3.9 nM (human CX3CR1), 720-fold selectivity over CXCR2.
KAND567 shows 246-fold selectivity versus hCCR1 and 187-fold versus hCCR2 and no significant antagonism of the CCR4, CCR5, CCR6, CXCR3, and CXCR5 receptor.
KAND567 also does not show significant interactions with the majority of the targets in a broad screen with 65 different receptors, enzymes, or ion channels.
KAND567 exhibits fractalkine stimulated GTPγS binding in the low nanomolar range, potent inhibition of human peripheral blood monocyte adhesion to a FKN-coated surface, and potent inhibition of soluble FKN-induced monocyte migration.
KAND567 inhibits FKN-induced actin polymerization in monocytes from human and rat blood.
KAND567 reverses clinical symptoms, reduces spinal cord neuroinflammation and demyelination in the rat experimental autoimmune encephalomyelitis (EAE) disease model of MS.

物理化学性质&存储条件

分子量 403.56
分子式 C19H25N5OS2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

CC(C)C[C@@H](NC1=C(SC(N)=N2)C2=NC(S[C@H](C3=CC=CC=C3)C)=N1)CO

参考文献

1. Sofia Karlströ, et al. J Med Chem. 2013 Apr 25;56(8):3177-90.

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