FXR
抑制剂选择性比较
FXR产品
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S4129 |
Sevelamer HClSevelamer是一种磷酸盐结合的药物，用于治疗慢性肾脏疾病的高磷酸盐血症。 |
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| S3736 |
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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| S2449 |
Colforsin (Forskolin)Colforsin (Forskolin, Coleonol) 在各种各样细胞类型中，是一种普遍存在的真核细胞腺苷酸环化酶（AC）激活剂，在细胞生理学研究中，通常用来提高cAMP水平。Forskolin 还可激发 PXR 和 FXR的活性而诱导自噬。 |
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| S3792 |
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。GW4064在MCF-7细胞中可刺激自噬。 |
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 (Chenodiol) 是一种天然存在的人体胆汁酸。 |
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| S7076 |
T0901317T0901317 是一种有效的，选择性的LXR和FXR激动剂，EC50分别约为50 nM和5 μM。T0901317 是 RORα 和 RORγ 的双重反向激动剂，对应的Ki值分别为132 nM和51 nM。T0901317 可显着抑制细胞增殖并诱导凋亡。 |
(C) Cells were pretreated with DMSO or T0901317 (5 μM), then incubated with 100 mg/L ox-LDL for 6 h. |
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| S6547New |
Cilofexor (GS‐9674)Cilofexor is a farnesoid X receptor (FXR) agonist. |
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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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| S8733 |
Tropifexor (LJN452)Tropifexor (LJN452)是一种新型有效的FXR激动剂，在HTRF实验中，EC50为0.2 nM。它对其他酶、离子通道、核受体和GPCR没有显著的脱靶效应，对FXR的选择性是对其他靶标的10000倍以上。 |
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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。Obeticholic Acid 可抑制自噬。Phase 3。 |
(c) Functional bile canaliculi or lack thereof in PHHs within MPTCs (12 d of drug treatment) as visualized by transport of fluorescent (green) dye into the canaliculi between PHHs. DMSO-treated MPCC control image is shown to the far right. (d) Neutral lipid (Nile red, green) staining of PHHs within MPTCs (12 d of drug treatment). DMSO-treated MPCC control image is shown to the far right. (e) NR1I2 (PXR) gene expression in drug-treated MPTCs relative to DMSOtreated MPTC controls (12 d of treatment). (f) ABCC2 (MRP2) gene expression in drug-treated MPTCs relative to DMSO-treated MPTC controls (12 d of treatment). (g) IL-6 levels in drug-treated MPTC supernatants (6 d of treatment). In all panels, statistical significance is displayed relative to DMSO-treated MPTCs. *p r 0.05, **p r 0.01, ***p r 0.001, and ****p r 0.0001. Scale bars on images represent 80 mm. |
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| S6413 |
fexaramineFexaramine是一种有效的、选择性farnesoid X receptor (FXR)激动剂，EC50为25 nM。它对hRXRα, hPPARα, hPPARγ, hPPARδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ和hVDR受体没有活性。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S4129 |
Sevelamer HClSevelamer是一种磷酸盐结合的药物，用于治疗慢性肾脏疾病的高磷酸盐血症。 |
||
| S3736 |
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。 |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S2449 |
Colforsin (Forskolin)Colforsin (Forskolin, Coleonol) 在各种各样细胞类型中，是一种普遍存在的真核细胞腺苷酸环化酶（AC）激活剂，在细胞生理学研究中，通常用来提高cAMP水平。Forskolin 还可激发 PXR 和 FXR的活性而诱导自噬。 |
|
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| S3792 |
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. |
| 目录号 | 产品描述 | 文献引用 | 实验数据 |
|---|---|---|---|
| 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。GW4064在MCF-7细胞中可刺激自噬。 |
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.
|
|
| 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. |
|
| S1843 |
Chenodeoxycholic AcidChenodeoxycholic Acid (Chenodiol) 是一种天然存在的人体胆汁酸。 |
||
| S7076 |
T0901317T0901317 是一种有效的，选择性的LXR和FXR激动剂，EC50分别约为50 nM和5 μM。T0901317 是 RORα 和 RORγ 的双重反向激动剂，对应的Ki值分别为132 nM和51 nM。T0901317 可显着抑制细胞增殖并诱导凋亡。 |
(C) Cells were pretreated with DMSO or T0901317 (5 μM), then incubated with 100 mg/L ox-LDL for 6 h. |
|
| S6547New |
Cilofexor (GS‐9674)Cilofexor is a farnesoid X receptor (FXR) agonist. |
||
| S4003 |
Lithocholic acidLithocholic acid是一种胆汁酸，可以溶解脂肪用于吸收。 |
||
| S8733 |
Tropifexor (LJN452)Tropifexor (LJN452)是一种新型有效的FXR激动剂，在HTRF实验中，EC50为0.2 nM。它对其他酶、离子通道、核受体和GPCR没有显著的脱靶效应，对FXR的选择性是对其他靶标的10000倍以上。 |
||
| S7660 |
Obeticholic AcidObeticholic Acid是一种有效的选择性farnesoid X receptor (FXR)兴奋剂，EC50为99 nM。Obeticholic Acid 可抑制自噬。Phase 3。 |
(c) Functional bile canaliculi or lack thereof in PHHs within MPTCs (12 d of drug treatment) as visualized by transport of fluorescent (green) dye into the canaliculi between PHHs. DMSO-treated MPCC control image is shown to the far right. (d) Neutral lipid (Nile red, green) staining of PHHs within MPTCs (12 d of drug treatment). DMSO-treated MPCC control image is shown to the far right. (e) NR1I2 (PXR) gene expression in drug-treated MPTCs relative to DMSOtreated MPTC controls (12 d of treatment). (f) ABCC2 (MRP2) gene expression in drug-treated MPTCs relative to DMSO-treated MPTC controls (12 d of treatment). (g) IL-6 levels in drug-treated MPTC supernatants (6 d of treatment). In all panels, statistical significance is displayed relative to DMSO-treated MPTCs. *p r 0.05, **p r 0.01, ***p r 0.001, and ****p r 0.0001. Scale bars on images represent 80 mm. |
|
| S6413 |
fexaramineFexaramine是一种有效的、选择性farnesoid X receptor (FXR)激动剂，EC50为25 nM。它对hRXRα, hPPARα, hPPARγ, hPPARδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ和hVDR受体没有活性。 |
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