| Bioactivity | 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]. | ||||||||||||
| Target | Ki: 0.16 µM (REV-ERBα) | ||||||||||||
| Invitro | 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: | ||||||||||||
| 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: | ||||||||||||
| Name | STL1267 | ||||||||||||
| CAS | 1429024-58-7 | ||||||||||||
| Formula | C17H11ClN4O | ||||||||||||
| Molar Mass | 322.75 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |