1384516-10-2

Upstream product

• 4521-33-9 5-nitro-2-thiophenecarboxaldehyde 
• 104-88-1 4-chlorobenzaldehyde 
• 104-86-9 4-chlorobenzylamine 

Downstream Products

• 1384516-15-7 C₂₀H₁₆ClF₃N₂O₂S 
• 1384516-16-8 C₂₀H₁₆ClN₃O₂S₂ 
• 1384516-18-0 C₂₁H₁₉ClN₂O₄S 
• 1384516-31-7 C₂₄H₂₆ClN₃O₂S 
• 1384516-32-8 C₁₉H₂₂ClN₃O₃S 
• 1384516-33-9 C₂₄H₂₄ClN₃O₄S 
• 1379686-30-2 SR₉₀₀₉ 
• 1384516-34-0 C₂₁H₂₄ClN₃O₄S 
• 1384516-35-1 C₂₄H₂₅ClN₄O₃S 
• 1384516-36-2 C₂₂H₂₉ClN₄O₃S 
• 1384516-37-3 C₂₄H₂₄ClN₅O₅S 
• 1384516-38-4 C₁₈H₂₂ClN₃O₄S₂ 
• 1384516-39-5 C₂₄H₂₆ClN₃O₄S₂ 
• 1384516-40-8 C₂₄H₂₆ClN₃O₄S₂ 

Relevant academic research and scientific papers

Compound with high affinity with orphan nuclear hormone receptor [alpha], and preparation method and application thereof

The invention provides a compound with high affinity with an orphan nuclear hormone receptor [alpha], and a preparation method and application thereof, and belongs to the field of organic synthesis. The structural formula of the compound with high affinity with the orphan nuclear hormone receptor [alpha] is shown as a formula I, wherein A is an ester group. The compound with high affinity with the orphan nuclear hormone receptor [alpha] not only has high affinity with the orphan nuclear hormone receptor [alpha], but also can reduce cell viability, change cell metabolism, change gene transcription in hepatocytes and embryonic stem cells lacking REV-ERB[alpha]. The preparation method of the compound with high affinity with the orphan nuclear hormone receptor [alpha] is simple, raw materials are easy to obtain, and the compound can be used for treating various diseases related to the orphan nuclear hormone receptor [alpha] and has a wide application prospect.

Optimized chemical probes for REV-ERBα

REV-ERBα has emerged as an important target for regulation of circadian rhythm and its associated physiology. Herein, we report on the optimization of a series of REV-ERBα agonists based on GSK4112 (1) for potency, selectivity, and bioavailability.(1) Potent REV-ERBα agonists 4, 10, 16, and 23 are detailed for their ability to suppress BMAL and IL-6 expression from human cells while also demonstrating excellent selectivity over LXRα. Amine 4 demonstrated in vivo bioavailability after either iv or oral dosing.

Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erbα

The structure-activity relationship study of a small molecule Rev-erbα agonist is reported. The potency and efficacy of the agonists in a cell-based assay were optimized as compared to the initial lead. Modest mouse pharmacokinetics coupled with an improved in vitro profile make 12e a suitable in vivo probe to interrogate the functions of Rev-erbα in animal models of disease.