XCT790

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 ERRα 反向激动剂，在瞬时转染测定中 IC50 为 300-500 nM。

A potent and selective ERRα inverse agonist with IC50 of 300-500 nM in transient transfection assays; shows no significant antagonist activity on related nuclear receptors (ERRγ or ERα, LXRα, LXRβ, FXR, PPARα, PPARδ, PPARγ, Nurr1, RARα, RORα, and RXRα) at 10 uM; inhibits PGC-1α regulation of ERRα and ERRα target gene expression; inhibits proliferation in cellular models of breast cancer.(In Vitro):XCT-790 (0-40 μM; 48 hours and 72 hours) reduces the viability of MES-SA, MES-SA/DX5, and HepG2 cells in a dose-dependent manner.XCT-790 (10 μM; 24 hours and 48 hours) reduces the protein levels of ERRα in HepG2 and R-HepG2 cell lines after 24 hours and maintains these reduced levels after 48 hours.XCT-790 (10 μM; 48 hours) induces apoptosis in the two cell lines with HepG2 being more sensitive compared to R-HepG2.(In Vivo):XCT-790 (XCT790; 4 mg/kg; intravenous injection; every three days; for 3 weeks; BALB/c mice) significantly inhibits tumor growth and angiogenesis, and induces apoptosis without a reduction in body weight, in xenograft models.

XCT-790 (0-40 μM; 48 hours and 72 hours) reduces the viability of MES-SA, MES-SA/DX5, and HepG2 cells in a dose-dependent manner.XCT-790 (10 μM; 24 hours and 48 hours) reduces the protein levels of ERRα in HepG2 and R-HepG2 cell lines after 24 hours and maintains these reduced levels after 48 hours.XCT-790 (10 μM; 48 hours) induces apoptosis in the two cell lines with HepG2 being more sensitive compared to R-HepG2. Cell Viability Assay Cell Line:MES-SA, MES-SA/DX5, HepG2 and R-HepG2 cells Concentration:0 μM, 5 μM, 10 μM, 20 μM, and 40 μM Incubation Time:48 hours and 72 hours Result:The cells proliferation were decreased in a dose-dependent fashion.Western Blot Analysis Cell Line:HepG2 and R-HepG2 cells Concentration:10 μM Incubation Time:24 hours and 48 hours Result:Reduced the protein levels of ERRα.Apoptosis AnalysisCell Line:HepG2 and R-HepG2 cells Concentration:10 μM Incubation Time:48 hours Result:Induced apoptosis in HepG2 and R-HepG2 cells.

XCT-790 (XCT790; 4 mg/kg; intravenous injection; every three days; for 3 weeks; BALB/c mice) significantly inhibits tumor growth and angiogenesis, and induces apoptosis without a reduction in body weight, in xenograft models. Animal Model:Female BALB/c mice (4 weeks of age) with HEC-1A xenograft Dosage:4 mg/kg Administration:Intravenous injection; every three days; for 3 weeks Result:Suppressed endometrial cancer growth and angiogenesis, and induced apoptosis.

XCT 790 | XCT-790

Endocrinology/Hormones

Estrogen Receptor/ERR

ERRα

Cancer

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725247-18-7

596.4249

C23H13F9N4O3S

>98% (HPLC)

DMSO: 21 mg/mL

O=C(NC1=NN=C(C(F)(F)F)S1)/C(C#N)=C/C2=CC=C(OCC3=CC=C(C(F)(F)F)C=C3C(F)(F)F)C(OC)=C2

2-Propenamide, 3-[4-[[2,4-bis(trifluoromethyl)phenyl]methoxy]-3-methoxyphenyl]-2-cyano-N-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]-

(-20℃)

With Ice Pack

≥ 2 years