STL1267

Names

[ Name ]:
STL1267

Biological Activity

[Description]:

STL1267 is a potent and cross-the-blood-brain barrier REV-ERB agonist with a Ki value of 0.16 µM for REV-ERBα. STL1267 shows no cytotoxicity. STL1267 inhibits the gene expression of BMAL1[1].

[Related Catalog]:

Research Areas >> Cancer

Research Areas >> Inflammation/Immunology

Research Areas >> Metabolic Disease

[Target]

Ki: 0.16 µM (REV-ERBα)[1]

[In Vitro]

STL1267 (5 µM; 24 h) 在 HepG2 细胞中降低 BMAL1 的表达并增加 Mtnd1、Mtco1、Vicad、Lcad、Scad、Lkb1、Sirt1、Nampt、Ppargc1a 的基因表达[1]。 Cell Viability Assay[1] Cell Line: HepG2, C2C12 cells Concentration: 0-20 µM Incubation Time: 24 h Result: Showed no adverse effects on cell viability up to the maximum dose examined 20 µM. RT-PCR[1] Cell Line: HepG2 cells Concentration: 5 µM Incubation Time: 24 h Result: Decreased the gene expression of BMAL1, increased the gene expression of Mtnd1, Mtco1, Vicad, Lcad, Scad, Lkb1, Sirt1, Nampt, Ppargc1a.

[In Vivo]

STL1267 (50 mg/kg; i.p.; once) 在小鼠体内有效抑制 BMAL1 的表达[1]。 Animal Model: 6-8 weeks, male C57Bl/6 J mice[1] Dosage: 50 mg/kg Administration: I.p.; once Result: Showed a plasma half-life of 1.6 h, effectively suppressed BMAL1 expression in the liver at 12 h post-administration.

[References]

[1]. Murray MH, et al. Structural basis of synthetic agonist activation of the nuclear receptor REV-ERB. Nat Commun. 2022 Nov 21;13(1):7131.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₇H₁₁ClN₄O

[ Molecular Weight ]:
322.75

Related Compounds

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