目录号 | 产品详情 | 靶点 | |
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T12251 | Others | ||
NR1H4 activator 1 is a potent and selective agonist of Famesoid X Receptor (FXR). | |||
T69686 | |||
BMS-986318 是一种有效的非胆汁酸FXR 激动剂,在FXRGal4 和 SRC-1 募集试验中的EC50分别为 53 和 350 nM。 BMS-986318 具有合适的 ADME 特性,并在肝胆汁淤积和纤维化的小鼠胆管结扎模型中具有效果。BMS-986318 可用于非酒精性脂肪性肝炎 (NASH)的研究。 | |||
T27492 | |||
GSK-8062 is an agonist of farnesoid X receptor (FXR). | |||
TN4628 | FXR | ||
Nelumol A, and nelumal A show a potency comparable to the endogenous ligand, they may as a valuable potential novel lead compound in the search for FXR agonists. | |||
T81030 | FXR | ||
Tauro-β-muricholic acid (TβMCA) 为一种具有三羟基结构的胆汁酸,是FXR的竞争性、可逆拮抗剂,IC50值为40 μM。此外,Tauro-β-muricholic acid 能够通过维持线粒体膜电位来阻抑胆汁酸引起的肝细胞凋亡,发挥抗凋亡功能。 | |||
T11661 | FXR GPCR19 | ||
INT-767 是一种高效的法尼类固醇 X 受体 (FXR)/TGR5 双激动剂,可预防 NASH 并促进内脏脂肪棕色脂肪生成和线粒体功能,可用于研究非酒精性脂肪性肝炎。 | |||
T63818 | |||
Omesdafexor 是 FXR 激动剂,能够用于研究肝病或代谢性炎症引起的疾病。 | |||
T37414 | |||
CAY10771 is a dual agonist of farnesoid X receptor (FXR) and peroxisome proliferator-activated receptor δ (PPARδ).1It activates FXR and PPARδ in reporter assays using HEK293T cells (EC50s = 0.94 and 1.5 μM, respectively) and is selective for these receptors over retinoic acid receptor α (RARα), retinoid X receptor α (RXRα), PPARα, PPARγ, and liver X receptor α (LXRα) at 10 μM. 1.Schierle, S., Neumann, S., Heitel, P., et al.Design and structural optimization of dual FXR/PPARδ activatorsJ. Med. Chem.63(15)8369-8379(2020) | |||
T78910 | FXR | ||
ZLY28,一种高效的肠道限制性FXR与FABP1双重调节剂,并具备口服活性。作为新型抗NASH药物,ZLY28应用于非酒精性脂肪性肝炎(NASH)的研究。 | |||
T36563 | |||
Bile acids are essential for solubilization and transport of dietary lipids, are the major products of cholesterol catabolism, and are physiological ligands for farnesoid X receptor (FXR), a nuclear receptor that regulates genes involved in lipid metabolism.1They are also inherently cytotoxic, as physiological imbalance contributes to increased oxidative stress.2,3Bile acid-controlled signaling pathways are promising novel targets to treat such metabolic diseases as obesity, type II diabetes, hyperlipidemia, and atherosclerosis.Guggulsterone, derived from resin of the guggul tree, is a competitive antagonist of FXR bothin vitroandin vivo.4Thecisstereoisomer of guggulsterone, (E)-guggulsterone, decreases chenodeoxycholic acid (CDCA)-induced FXR activation with an IC50value of 15 μM.5,6By inhibiting CDCA-induced transactivation of FXR, guggulsterone lowers low-density lipoprotein cholesterol and triglyceride levels in rodents fed a high cholesterol diet.4 1.Makishima, M., Okamoto, A.Y., Repa, J.J., et al.Identification of a nuclear receptor for bile acidsScience2841362-1365(1999) 2.Barbier, O., Torra, I.P., Sirvent, A., et al.FXR induces the UGT2B4 enzyme in hepatocytes: A potential mechanism of negative feedback control of FXR activityGastroenterology1241926-1940(2003) 3.Tan, K.P., Yang, M., and Ito, S.Activation of nuclear factor (erythroid-2 like) factor 2 by toxic bile acids provokes adaptive defense responses to enhance cell survival at the emergence of oxidative stressMol. Pharmacol.72(5)1380-1390(2007) 4.Urizar, N.L., Liverman, A.B., Dodds, D.T., et al.A natural product that lowers cholesterol as an anatagonist ligand for FXRScience296(5573)1703-1706(2002) 5.Cui, J., Huang, L., Zhao, A., et al.Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pumpThe Journal of Biological Chemisty278(12)10214-10220(2003) 6.Wu, J., Xia, C., Meier, J., et al.The hypolipidemic natural product guggulsterone acts as an antagonist of the bile acid receptorMolecular Endocrinology16(7)1590-1597(2002) |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-06768 | NR1H4 Protein, Human, Recombinant (His) | Human | E. coli | ||
NR1H4 Protein, Human, Recombinant (His) is expressed in E. coli with His tag. The predicted molecular weight is 27.83 kDa. Accession number: Q96RI1-1
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TMPY-06756 | NR1H4 Protein, Mouse, Recombinant (His) | Mouse | E. coli | ||
NR1H4 Protein, Mouse, Recombinant (His) is expressed in E. coli with His tag. The predicted molecular weight is 27.80 kDa.
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TMPH-01355 | FXR1 Protein, Human, Recombinant (His) | Human | E. coli | ||
RNA-binding protein required for embryonic and postnatal development of muscle tissue. May regulate intracellular transport and local translation of certain mRNAs.
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TMPY-02987 | Vitamin D Receptor/VDR Protein, Mouse, Recombinant (His) | Mouse | Baculovirus-Insect Cells | ||
VDR (vitamin D (1,25- dihydroxyvitamin D3) receptor), also known as NR1I1, belongs to the NR1I family, NR1 subfamily. It is composed of three domains: a modulating N-terminal domain, a DNA-binding domain and a C-terminal ligand-binding domain. Vitamin D receptors (VDRs) are members of the NR1I family, which also includes pregnane X (PXR) and constitutive androstane (CAR) receptors, that form heterodimers with members of the retinoid X receptor family. VDRs repress expression of 1alpha-hydroxylase (the proximal activator of 1,25(OH)2D3) and induce expression of the 1,25(OH)2D3 inactivating enzyme CYP24. Also, it has recently been identified as an additional bile acid receptor alongside FXR and may function to protect gut against the toxic and carcinogenic effects of these endobiotics. VDR is expressed in the intestine, thyroid and kidney and has a vital role in calcium homeostasis. It is the nuclear hormone receptor, also called transcription factor that mediates the action of vitamin D3. Inherited mutations in the VDR gene leads to rickets.
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TMPY-02706 | Vitamin D Receptor/VDR Protein, Human, Recombinant (His) | Human | Baculovirus-Insect Cells | ||
VDR (vitamin D (1,25- dihydroxyvitamin D3) receptor), also known as NR1I1, belongs to the NR1I family, NR1 subfamily. It is composed of three domains: a modulating N-terminal domain, a DNA-binding domain and a C-terminal ligand-binding domain. Vitamin D receptors (VDRs) are members of the NR1I family, which also includes pregnane X (PXR) and constitutive androstane (CAR) receptors, that form heterodimers with members of the retinoid X receptor family. VDRs repress expression of 1alpha-hydroxylase (the proximal activator of 1,25(OH)2D3) and induce expression of the 1,25(OH)2D3 inactivating enzyme CYP24. Also, it has recently been identified as an additional bile acid receptor alongside FXR and may function to protect gut against the toxic and carcinogenic effects of these endobiotics. VDR is expressed in the intestine, thyroid and kidney and has a vital role in calcium homeostasis. It is the nuclear hormone receptor, also called transcription factor that mediates the action of vitamin D3. Inherited mutations in the VDR gene leads to rickets.
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