INCB3284 bismesylate

Chemical Structure : INCB3284 bismesylate

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货号: PC-20531Not For Human Use, Lab Use Only.

规格	价格	库存	数量
50 mg		Get quote
100 mg		Get quote
200 mg		Get quote
1 g		Get quote

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生物&药学活性

INCB3284 bismesylate (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	712.75
分子式	C28H39F3N4O10S2
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.CS(=O)(O)=O.CS(=O)(O)=O

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.