SML3972
Azeliragon
≥98% (HPLC)
别名:
PF-04494700, PF04494700, 3-(4-{2-Butyl-1-[4-(4-chlorophenoxy)-phenyl]-1H-imidazole-4-yl}-phenoxy)-propyl]-diethylamine 1, 3-[4-[2-Butyl-1-[4-(4-chlorophenoxy)phenyl]imidazol-4-yl]phenoxy]-N,N-diethylpropan-1-amine), PF 04494700, TTP 488, TTP-488, TTP488
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About This Item
价格与库存信息目前不能提供
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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
, White to light brown
溶解性
DMSO: 2 mg/mL, clear
储存温度
room temp
SMILES字符串
Clc1ccc(cc1)Oc2ccc(cc2)[n]3c(nc(c3)c4ccc(cc4)OCCCN(CC)CC)CCCC
InChI
1S/C32H38ClN3O2/c1-4-7-9-32-34-31(25-10-16-28(17-11-25)37-23-8-22-35(5-2)6-3)24-36(32)27-14-20-30(21-15-27)38-29-18-12-26(33)13-19-29/h10-21,24H,4-9,22-23H2,1-3H3
InChI key
KJNNWYBAOPXVJY-UHFFFAOYSA-N
生化/生理作用
Orally active, brain-penetrant, selective receptor for advanced glycation end products (RAGE) antagonist in vitro and in vivo.
Azeliragon (PF-04494700; TTP488) is an orally active, brain-penetrant, selective receptor for advanced glycation end products (RAGE) antagonist (Kd = 12.7 nM using sRAGE; little affinity toward >100 receptors/transporters) that blocks known RAGE ligands binding (S100b, amphoterin, carboxymethyl-lysine, and Aβ1-42). Azeliragon (0.3-3 mg/kg/day p.o.) reduces brain amyloid (Aβ1-40 & Aβ1-42) and inflammatory markers (TNF-α, TGF-β and IL-1), while increases plasma Aβ in tgAPPSWE/LON mice, a mouse model with Swedish and London mutations that over-express human APP.
Azeliragon (PF-04494700; TTP488) is an orally active, brain-penetrant, selective receptor for advanced glycation end products (RAGE) antagonist (Kd = 12.7 nM using sRAGE; little affinity toward >100 receptors/transporters) that blocks known RAGE ligands binding (S100b, amphoterin, carboxymethyl-lysine, and Aβ1-42). Azeliragon (0.3-3 mg/kg/day p.o.) reduces brain amyloid (Aβ1-40 & Aβ1-42) and inflammatory markers (TNF-α, TGF-β and IL-1), while increases plasma Aβ in tgAPPSWE/LON mice, a mouse model with Swedish and London mutations that over-express human APP.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
Targeting the Receptor for Advanced Glycation Endproducts (RAGE): A Medicinal Chemistry Perspective
Journal of Medicinal Chemistry, 60(17), 7213-7232 (2017)
Development of Azeliragon, an Oral Small Molecule Antagonist of the Receptor for Advanced Glycation Endproducts, for the Potential Slowing of Loss of Cognition in Mild Alzheimer's Disease
The journal of prevention of Alzheimer's disease, 5(2), 149-154 (2018)
Melinda Magna et al.
NPJ breast cancer, 9(1), 59-59 (2023-07-14)
Triple-negative breast cancer (TNBC) is a highly aggressive and metastatic cancer subtype, which is generally untreatable once it metastasizes. We hypothesized that interfering with the Receptor for Advanced Glycation End-products (RAGE) signaling with the small molecule RAGE inhibitors (TTP488/Azeliragon and
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