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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-INCB3284
INCB3284

Chemical Structure : INCB3284

CAS No.: 887401-92-5

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INCB3284 (INCB 3284, INCB003284)

货号: PC-20530Not For Human Use, Lab Use Only.

INCB3284 (INCB 3284, INCB003284) is a potent, selective and orally bioavailable hCCR2 antagonist with IC50 of 3.7 nM in antagonism of MCP-1 binding to hCCR2 and 4.7 nM in antagonism of chemotaxis activity.

规格 价格 库存 数量
25 mg ￥2580 In stock
50 mg ￥4280 In stock
100 g ￥6980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

INCB3284 (INCB 3284, INCB003284) is a potent, selective and orally bioavailable hCCR2 antagonist with IC50 of 3.7 nM in antagonism of MCP-1 binding to hCCR2 and 4.7 nM in antagonism of chemotaxis activity.
INCB3284 potently inhibited CCR2-mediated signaling events such as intracellular calcium mobilization and ERK phosphorylation with IC50 values of 6 and 2.6 nM, respectively.
INCB3284 showed no significant inhibitory activity at a concentration of 1 μM against a panel of >50 ion channels, transporters, chemokine receptors including CCR1, CCR3, CCR5, CXCR3, and CXCR5, and additional GPCRs.
INCB3284 abolished the high salt (HS)-induced increase in BP in KL(+/-) mice, also attenuated the increased renal expressions of serum glucocorticoid-regulated kinase 1, thiazide-sensitive NaCl cotransporter, and ATP synthase β along with the renal structural damage and functional impairment induced by HS loading.

物理化学性质&存储条件

分子量 520.55
分子式 C26H31F3N4O4
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

O=C(NCC(N[C@H]1CN([C@H]2CC[C@@](C3=CC=C(OC)N=C3)(O)CC2)CC1)=O)C4=CC=CC(C(F)(F)F)=C4

参考文献

1. Xue CB, et al. ACS Med Chem Lett. 2011 Mar 31;2(6):450-4.

2. Saika F, et al. Neurosci Lett. 2018 Feb 5;665:33-37.

3. Zhou X, et al. J Am Soc Nephrol. 2015 Jan;26(1):121-32.

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