FXR
Farnesoid X receptor (FXR; NR1H4), a member of the nuclear receptor (NR) superfamily, was identified as a receptor of bile acids (BAs). As a ligand-activated transcription factor, FXR binds to DNA (i.e., FXR response elements) as a monomer or as a heterodimer with a common partner for NRs, retinoid X receptor (RXR; NR2B1), in order to regulate the expression of the diverse genes involved in the metabolism of BAs, lipids, and carbohydrates. There are two known FXR genes (i.e., FXRα (NR1H4) and FXRβ (NR1H5)). A single FXRα gene in human and rodents encodes four different isoforms (FXRα1, FXRα2, FXRα3, and FXRα4), resulting from different promoters and RNA splicing. FXR is mainly expressed in various tissues including the liver, intestine, kidney, and adrenal gland, with much lesser extents in the adipose tissue and heart. FXR has been identified as a promising therapeutic target for the management of liver and/or metabolic diseases, allowing the pharmacological approaches to develop FXR modulators.
References
1.Han CY. Int J Mol Sci. 2018;19(7):2069.
References
1.Han CY. Int J Mol Sci. 2018;19(7):2069.
Metabolic Enzyme/Protease
11β-HSD(15)
15-PGDH(1)
ACC(10)
ACE(15)
AChE(47)
Adenylate Cyclase(12)
ALDH(14)
Aldose Reductase(5)
Aminopeptidase(19)
BACE(19)
Casein Kinase(51)
CAT(5)
Cathepsin(9)
CETP(13)
COMT(2)
CPG2(1)
CYPs(6)
Decarboxylase(3)
Dehydrogenase(131)
DGAT(4)
Dopamine beta-hydroxylase(2)
DPP(32)
Elastase(6)
FAAH(28)
Factor Xa(31)
Fatty Acid Synthase(17)
Ftase(2)
FXR(26)
Glucokinase(1)
GSNOR(2)
Guanylate Cyclase(13)
HMGCR(17)
IDH(7)
IDO(20)
IMPDH(2)
LDH(2)
LDL(8)
Lipase(17)
Lipid(12)
MAGL(6)
MAO(72)
MMP(78)
NAMPT(12)
Neprilysin(7)
Other Targets(10)
P450(112)
PAI-1(9)
Phosphatase(95)
Phospholipase(65)
PPAR(115)
Protein Phosphatase/PTP(6)
Renin(8)
Retinoid Receptor(37)
SCD(6)
Steroid Sulfatase (STS)(2)
Thioredoxin(1)
TPH(5)
Transferase(37)
Vitamin(44)
Xanthine Oxidase (XAO)(11)
FXR
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Osocimab
产品货号 : M36825
cas no: 2056878-75-0
Osocimab (BAY 1213790) 是一种抗 FXIa 抗体 (Ki=2.4 nM;EC50=0.2 nM)。而 FXI 抑制有可能降低血栓形成风险。Osocimab 抑制凝血酶生成,并延长活化的部分凝血活酶时间。Osocimab 具有抗凝血作用。 -
Chenodeoxycholic Acid sodium salt
产品货号 : M35851
cas no: 2646-38-0
Chenodeoxycholic acid sodium 是一种疏水初级胆汁酸,能够活化核受体 FXR,该受体与胆固醇代谢有关。 -
NDB
产品货号 : M35688
cas no: 1660153-08-1
NDB 是一种选择性人 FXRα (hFXRα) 拮抗剂,可有效调节 FXRα 下游基因的转录。NDB可用于抗糖尿病研究。 -
Gly-β-MCA
产品货号 : M32942
cas no: 66225-78-3
Gly-β-MCA 是一种胆汁酸,是有效的、稳定的、肠特异性的以及具有口服生物活性的法尼酯X受体 (FXR) 抑制剂,可用于代谢障碍的研究。 -
Ursodeoxycholic acid sodium
产品货号 : M27933
cas no: 2898-95-5
熊去氧胆酸钠是一种天然存在的次级胆汁酸,具有抗炎和细胞保护活性。熊去氧胆酸钠作为信号分子,通过与胆汁酸激活受体相互作用发挥作用,