FXR
- 抑制剂选择性比较
- 溶解性比较
| 目录号 | 产品目录 | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | 酒精 | ||
| S3736 | Fondaparinux Sodium | 100 mg/mL | 1 mg/mL | <1 mg/mL |
| S3792 | Guggulsterone E&Z | -1 mg/mL | 62 mg/mL | -1 mg/mL |
| S2782 | GW4064 | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S2694 | Turofexorate Isopropyl (XL335) | <1 mg/mL | 33 mg/mL | 2 mg/mL |
| S1843 | Chenodeoxycholic Acid | <1 mg/mL | 79 mg/mL | 79 mg/mL |
| S4003 | Lithocholic acid | <1 mg/mL | 75 mg/mL | 47 mg/mL |
| S8733 | Tropifexor (LJN452) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S7660 | Obeticholic Acid | <1 mg/mL | 84 mg/mL | 84 mg/mL |
- FXR抑制剂（8）
- 新FXR产品
| 产品目录 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S3736New |
Fondaparinux SodiumFondaparinux是一种合成的喃葡萄糖，具有抗血栓形成的活性。它能选择性地结合抗凝血酶 III，从而加强对活化Factor Xa的中和。它是Factor Xa的合成型抑制剂。 |
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| S3792New |
Guggulsterone E&ZGuggulsterone is one of the active constituent of Commiphora mukul. It occurs in two isomeric forms, namely Z-GS and E-GS. Guggulsterone act as antagonist ligands for the bile acid receptor, farnesoid X receptor, and as active ingredients responsible for the hypolipidemic activity. |
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| S2782 |
GW4064GW4064是一种farnesoid X receptor (FXR)激动剂，CV1细胞系中EC50为65 nM。浓度达到1 μM时，对其他核受体没有活性。 |
FXR agonist GW4064 reduced the association between β-Catenin/TCF4 complex and the TCF binding sites from Cyclin D1 promoter. ChIP analysis was carried out using antibodies against TCF4, β-Catenin, or normal IgG in lysates from Huh7 cells.
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| S2694 |
Turofexorate Isopropyl (XL335)Turofexorate Isopropyl (XL335)是一种有效的，选择性的FXR激动剂，EC50为4 nM，高选择性作用于其他核受体，如LXR， PPAR， ER等，Phase 1。 |
(B) FXR agonists repressed β-Catenin mediated transcriptional activity. HEK293 cells were transfected with TOPflash reporter and pRLTK plasmid, and then treated with FXR agonists, GW4064 or WAY-36240, ranging from 1–4 μM. Luciferase activity was measured 12-24 hours post treatment. TOPflash/FOPflash activity was normalized to that of the controls. |
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| S1843 |
Chenodeoxycholic AcidChenodeoxycholic acid 是一种天然存在的人体胆汁酸。 |
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| S4003 |
Lithocholic acidLithocholic acid是一种胆汁酸，可以溶解脂肪用于吸收。 |
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| S8733New |
Tropifexor (LJN452)Tropifexor (LJN452) is a novel and highly potent agonist of FXR with EC50 of 0.2 nM in HTRF assay. It shows no significant off-target activity against a broad panel of enzyme, ion channel, nuclear receptor, and GPCR (>10000-fold selectivity for FXR). |
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| S7660 |
Obeticholic AcidObeticholic Acid是一种有效的选择性farnesoid X receptor (FXR)兴奋剂，EC50为99 nM。Phase 3。 |
(D) Expression of hepatic FXR target genes, n = 3. Data are expressed as mean ± SD, ###P < 0.001 versus group 1, *P < 0.05, **P < 0.01, and ***P b 0.001 versus group 2, sP < 0.05, ssP < 0.01, and sssP < 0.001 versus group 3
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