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CXCR6 inhibitor 81

  Cat. No.:  DC70333   Featured
Chemical Structure
2579689-85-1
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More than 5000 active chemicals with high quality for research!
Field of application
CXCR6 inhibitor 81 is a potent (EC50=40 nM) and selective orally bioavailable small molecule antagonist of human CXCR6 receptor; Compound 81 displays >10-fold improvement in potency in both the β-arrestin and cAMP assays (IC50 =40 and 540 nM, respectively) compared to ML339. CXCR6 inhibitor 81 inhibits migration of SK-HEP-1 hepatoma cells in a dose dependent manner. Compound 81 has promising oral DMPK data, significantly decreases tumor growth in a 30-day mouse xenograft model of HCC.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2579689-85-1
Chemical Name: Benzamide, 3,4,5-trimethoxy-N-[(3-exo)-9-[[4-(trifluoromethyl)-2-benzothiazolyl]methyl]-9-azabicyclo[3.3.1]non-3-yl]-
Synonyms: Benzamide, 3,4,5-trimethoxy-N-[(3-exo)-9-[[4-(trifluoromethyl)-2-benzothiazolyl]methyl]-9-azabicyclo[3.3.1]non-3-yl]-
SMILES: C(NC1CC2N(CC3=NC4=C(C(F)(F)F)C=CC=C4S3)C(CCC2)C1)(=O)C1=CC(OC)=C(OC)C(OC)=C1
Formula: C27H30F3N3O4S
M.Wt: 549.605016231537
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC73409 YM-344031 YM-344031 is a potent, selective, brain-penetrable CCR3 antagonist with binding IC50 of 3.0 nM, inhibits ligand-induced Ca(2+) flux with IC50 of 5.4 nM.
DC73393 alpha-NETA alpha-NETA (α-NETA) is a small molecule antagonist of chemerin receptor chemokine-like receptor 1 (CMKLR1), inhibits chemerin-stimulated β-arrestin2 association with CMKLR1 with IC50 of 4.9 uM.
DC72882 MR120 MR120 (CCR6 antagonist 1b) is a potent, selective CCR6 antagonist, disrupts the CCL20-induced chemotaxis of CCR6+CD4+ T cells.
DC72766 PF-07054894 PF-07054894 is a potent CCR6 antagonist. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease.
DC72524 FLX475 FLX475 is a potent CCR4 antagonist that blocks regulatory T cells that interfere with effective antitumor immune responses and has antitumor activity.
DC72110 RPT193 RPT193 is an orally active inhibitor of CCR4, blocks the recruitment of Th2 inflammatory immune cells into inflamed tissues. RPT193 can be used for allergic inflammation in atopic dermatitis, asthma, and other diseases research.
DC70817 SX-682 SX-682 (SX682) is a potent, allosteric, orally bioavailable inhibitor of CXCR1 and CXCR2.SX-682 enhances tumor infiltration, activation, and the therapeutic efficacy of adoptively transferred NK cells.SX-682 significantly inhibits trafficking of PMN-MDSCs without altering CXCR2 ligand expression.SX-682 enhances T cell-based immunotherapeutic efficacy.
DC70602 ML339 ML 339 is a potent and selective hCXCR6 antagonist (IC50 = 140 nM), 100-fold less active at the murine CXCR6 receptor (IC50 = 18 uM); ML 339 exhibits selectivity over CXCR5, CXCR4, CCR6 and APJ receptors.
DC70333 CXCR6 inhibitor 81 CXCR6 inhibitor 81 is a potent (EC50=40 nM) and selective orally bioavailable small molecule antagonist of human CXCR6 receptor; Compound 81 displays >10-fold improvement in potency in both the β-arrestin and cAMP assays (IC50 =40 and 540 nM, respectively) compared to ML339. CXCR6 inhibitor 81 inhibits migration of SK-HEP-1 hepatoma cells in a dose dependent manner. Compound 81 has promising oral DMPK data, significantly decreases tumor growth in a 30-day mouse xenograft model of HCC.
DC70292 CCR4-IN-38 CCR4-IN-38 (CCR4-351) is a potent, selective, orally bioavailable CCR4 antagonist with IC50 of 50 nM (Chemotaxis inhibition).CCR4-IN-38 inhibits the recruitment of Treg into the tumor microenvironment (TME).CCR4-IN-38 elicits antitumor responses as a single agent or in combination with an immune checkpoint blockade.
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