886362-95-4

Usage

Uses

Used in Pharmaceutical Industry:
1,8-NAPHTHYRIDIN-2-BUTYRIC ACID is used as a pharmaceutical agent for its potential anti-cancer properties, targeting the enzyme dihydrofolate reductase, which plays a crucial role in DNA synthesis and cell proliferation. This makes it a candidate for the development of cancer treatments.
1,8-NAPHTHYRIDIN-2-BUTYRIC ACID is also used as an anti-inflammatory agent due to its potential to modulate inflammatory responses, which can be beneficial in treating various inflammatory conditions.
Additionally, it is used in the research and development of treatments for autoimmune disorders, given its potential to target specific pathways involved in these diseases, offering a new avenue for therapeutic intervention.

InChI:InChI=1/C12H12N2O2/c15-11(16)5-1-4-10-7-6-9-3-2-8-13-12(9)14-10/h2-3,6-8H,1,4-5H2,(H,15,16)

Upstream product

• 7521-41-7 2-Aminonicotinaldehyde 
• 13984-57-1 ethyl 5-oxohexanoate 
• 193818-28-9 ethyl 4-(1,8-naphthyridin-2-yl)butanoate 

Downstream Products

• 1314796-26-3 C₂₄H₁₉F₄N₅O 
• 1314796-27-4 N-[{1-(4-fluoro-3-trifluoromethylphenyl)-1H-pyrazol-4-yl}methyl]-4-([1,8]naphthyridin-2-yl)butyramide 
• 1314796-28-5 C₂₂H₁₉ClN₄O₂ 
• 1314796-30-9 C₂₂H₁₈ClFN₄O₂ 
• 1314796-31-0 N-[{3-(3-trifluoromethyl-4-fluorophenyl)isoxazol-5-yl}methyl]-4-([1,8]naphthyridin-2-yl)butyramide 
• 1314796-33-2 C₂₂H₁₉ClN₄OS 
• 1314796-34-3 C₂₂H₁₉ClN₄OS 
• 1314796-35-4 C₂₂H₁₇F₄N₅O₂ 
• 1314796-36-5 C₂₂H₁₇F₄N₅OS 
• 1314796-77-4 C₂₅H₂₁ClN₄O₂ 
• 1314796-79-6 C₂₅H₂₀ClFN₄O₂ 
• 1314796-80-9 C₂₆H₂₁F₃N₄O₂ 
• 1314796-51-4 C₂₁H₂₃N₃O₂S 
• 1314796-76-3 C₃₄H₂₉ClFN₅O₂ 

Relevant academic research and scientific papers

Discovery of a potent and selective small molecule hGPR91 antagonist

GPR91, a 7TM G-Protein-Coupled Receptor, has been recently deorphanized with succinic acid as its endogenous ligand. Current literature indicates that GPR91 plays role in various pathophysiology including renal hypertension, autoimmune disease and retinal angiogenesis. Starting from a small molecule high-throughput screening hit 1 (hGPR91 IC50: 0.8 μM) - originally synthesized in Merck for Bradykinin B1 Receptor (BK1R) program, systematic structure-activity relationship study led us to discover potent and selective hGPR91 antagonists e.g. 2c, 4c, and 5g (IC50: 7-35 nM; >1000 fold selective against hGPR99, a closest related GPCR; >100 fold selective in Drug Matrix screening). This initial work also led to identification of two structurally distinct and orally bio-available lead compounds: 5g (%F: 26) and 7e (IC50: 180 nM; >100 fold selective against hGPR99; %F: 87). A rat pharmacodynamic assay was developed to characterize the antagonists in vivo using succinate induced increase in blood pressure. Using two representative antagonists, 2c and 4c, the GPR91 target engagement was subsequently demonstrated using the designed pharmacodynamic assay.