STL1267

Modify Date: 2024-04-08 09:55:43

STL1267 Structure
STL1267 structure
Common Name STL1267
CAS Number 1429024-58-7 Molecular Weight 322.75
Density N/A Boiling Point N/A
Molecular Formula C17H11ClN4O Melting Point N/A
MSDS N/A Flash Point N/A

 Use of STL1267


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].

 Names

Name STL1267

 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
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
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