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Chemical Structure : INCB3284
CAS No.: 887401-92-5
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 25 mg | $258 | In stock | |
| 50 mg | $428 | In stock | |
| 100 g | $698 | In stock | |
| 1 g | Get quote |
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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.
| M.Wt | 520.55 | |
| Formula | C26H31F3N4O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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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