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- 2x SYBR Green qPCR Master Mix
- 2x SYBR Green qPCR Master Mix(Low ROX)
- 2x SYBR Green qPCR Master Mix(High ROX)
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- 磁力架
- Poly DYKDDDDK Tag多肽
- 蛋白酶抑制劑Cocktail
- 蛋白酶抑制劑Cocktail(DMSO儲(chǔ)液)
- 磷酸酶抑制劑Cocktail
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- Cell Counting Kit-8 (CCK-8)
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GW4064
GW4064是一種farnesoid X receptor (FXR)激動(dòng)劑，CV1細(xì)胞系中EC50為65 nM。濃度達(dá)到1 μM時(shí)，對(duì)其他核受體沒(méi)有活性。GW4064在MCF-7細(xì)胞中可刺激自噬。
GW4064 Chemical Structure
CAS: 278779-30-9
產(chǎn)品質(zhì)控
批次：
純度：
99.80%
99.80
GW4064相關(guān)產(chǎn)品
| 相關(guān)產(chǎn)品 | Guggulsterone E&Z Turofexorate Isopropyl (XL335) | 點(diǎn)擊展開(kāi) |
|---|---|---|
| 相關(guān)化合物庫(kù) | 代謝化合物庫(kù) 抗癌代謝化合物庫(kù) 谷氨酰胺代謝化合物庫(kù) 糖代謝化合物庫(kù) 脂代謝化合物庫(kù) | 點(diǎn)擊展開(kāi) |
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類(lèi)型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息 |
|---|---|---|---|---|---|
| HepG2 | Function assay | 1 uM | 18 hrs | Decrease in CYP7A1 gene expression in human HepG2 cells at 1 uM after 18 hrs by RT-PCR | 17963371 |
| Caco-2 | Function assay | 1 uM | 6 days | Activation of IBABP gene expression in human Caco-2 cells at 1 uM after 6 days by RT-PCR | 17963371 |
| HepG2 | Function assay | 1 uM | 18 hrs | Activation of BSEP gene expression in human HepG2 cells at 1 uM after 18 hrs by RT-PCR | 17963371 |
| Huh7 | Function assay | 1 uM | 18 hrs | Activation of SHP gene expression in human Huh7 cells at 1 uM after 18 hrs by RT-PCR | 17963371 |
| Huh7 | Function assay | 1 uM | 18 hrs | Activation of BSEP gene expression in human Huh7 cells at 1 uM after 18 hrs by RT-PCR | 17963371 |
| HepG2 | Function assay | 10 uM | 10 mins | Induction of FXR-mediated Akt-phosphorylation at S473 site in serum-starved human HepG2 cells at 10 uM measured after 10 mins by western blot analysis | 27372840 |
| HepG2 | Function assay | 10 uM | 10 mins | Induction of FXR-mediated Akt-phosphorylation in serum-starved human HepG2 cells assessed as increase in GSK-3beta-phosphorylation at 10 uM measured after 10 mins by western blot analysis | 27372840 |
| HepG2 | Function assay | 10 uM | Induction of FXR-mediated SHP mRNA expression in serum-starved human HepG2 cells at 10 uM measured after overnight incubation by qPCR analysis | 27372840 | |
| HepG2 | Function assay | 10 uM | Activation of FXR in human HepG2 cells assessed as upregulation of SHP mRNA expression at 10 uM by RT-PCR method | 30031618 | |
| HepG2 | Function assay | 10 uM | Activation of FXR in human HepG2 cells assessed as upregulation of FXR mRNA expression at 10 uM by RT-PCR method | 30031618 | |
| HepG2 | Function assay | 10 uM | Activation of FXR in human HepG2 cells assessed as downregulation of SREBP-1c mRNA expression at 10 uM by RT-PCR method | 30031618 | |
| 3T3L1 | Function assay | 10 uM | Reduction in lipid accumulation in mouse 3T3L1 cells at 10 uM by Oil Red O staining-based absorbance method relative to control | 30342957 | |
| HeLa | Function assay | 24 hrs | Agonist activity at human full length FXR expressed in HeLa cells cotransfected with pSG5-human RXR after 24 hrs by Dual-Glo luciferase reporter gene assay, EC50 = 0.51 μM. | 25934227 | |
| insect cells | Function assay | 1 hr | Agonist activity at recombinant human GST-tagged FXR ligand binding domain (193 to 472 residues) expressed in baculovirus infected insect cells assessed as induction of interaction with biotin labelled SRC-1 after 1 hr by HTRF assay, EC50 = 0.019 μM. | 29148806 | |
| HEK293T | Function assay | 24 hrs | Agonist activity at human FXR expressed in HEK293T cells assessed as BSEP promoter driven cellular transcriptional activity after 24 hrs by luciferase reporter gene assay, EC50 = 0.095 μM. | 29148806 | |
| HEK293 | Function assay | Agonist activity at human GST-fused FXR LBD expressed in HEK293 cells coexpressing GAL4-DNA bindig domain and pFRluc by mammalian one-hybrid assay, EC50 = 0.035 μM. | 20638278 | ||
| HEK293 | Function assay | Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct reporter cellular assay, EC50 = 0.03 μM. | 20638278 | ||
| CV1 | Function assay | Increase in human FXR-mediated transient transcription of luciferase reporter gene transfected in african green monkey CV1 cells, EC50 = 0.065 μM. | 19586769 | ||
| CV1 | Function assay | Agonist activity at human FXR transfected in african green monkey CV1 cells by luciferase reporter gene transient transfection assay, EC50 = 0.065 μM. | 19410460 | ||
| CV1 | Function assay | Agonist activity at FXR expressed in african green monkey CV1 cells by luciferase reporter transient transfection assay, EC50 = 0.065 μM. | 18621523 | ||
| HEK293 | Function assay | Agonistic activity at FXR in HEK293 cells by GAL4 transactivation activity, EC50 = 0.07 μM. | 17292610 | ||
| CV-1 | Function assay | Agonist activity at human FXR LBD iexpressed in monkey CV-1 cells assessed as transactivation of luciferase reporter gene expression, EC50 = 0.065 μM. | 21256005 | ||
| CV1 | Function assay | Agonist activity at human FXR LBD transfected in african green monkey CV1 cells after overnight incubation by luciferase reporter gene assay, EC50 = 0.065 μM. | 21890356 | ||
| HEK293 | Function assay | Agonist activity at human recombinant FXR expressed in HEK293 cells coexpressing CMX-GAL4N by luciferase reporter gene assay, EC50 = 0.07 μM. | 22583617 | ||
| HEK293 | Function assay | Agonist activity at human FXR expressed in HEK293 cells by luciferase reporter gene assay, EC50 = 0.026 μM. | 25305688 | ||
| CV1 | Function assay | Agonist activity at FXR (unknown origin) transfected into african green monkey CV1 cells assessed as ligand-mediated transcription by luciferase reporter/ transient transfection assay, EC50 = 0.065 μM. | 25499883 | ||
| HEK293 | Function assay | Agonist activity at human FXR transfected in HEK293 cells assessed as transcriptional activity by luciferase reporter gene assay, EC50 = 0.373 μM. | 26568144 | ||
| HEK-293 | Function assay | Agonist activity at C-terminal Gal4-tagged human FXR (187 to 472 residues) expressed in HEK-293 cells co-expressing pFRluc by mammalian one hybrid assay, EC50 = 0.035 μM. | 27268696 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | GW4064是一種farnesoid X receptor (FXR)激動(dòng)劑，CV1細(xì)胞系中EC50為65 nM。濃度達(dá)到1 μM時(shí)，對(duì)其他核受體沒(méi)有活性。GW4064在MCF-7細(xì)胞中可刺激自噬。 | ||
|---|---|---|---|
| 靶點(diǎn) |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | GW 4064是一種完全激動(dòng)劑，在轉(zhuǎn)染有鼠源和人源FXR表達(dá)載體以及確定的報(bào)告基因的CV-1細(xì)胞中， EC50分別為80和90。GW 4064直到1 μM濃度對(duì)其它核受體也沒(méi)有活性，包括維甲酸受體。因此, GW 4064是一種強(qiáng)有效和選擇性的非類(lèi)固醇FXR激動(dòng)劑[2]。 |
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|---|---|---|---|---|
| 實(shí)驗(yàn)圖片 | 檢測(cè)方法 | 檢測(cè)指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot | PTEN / p-AKT / AKT p-EGFR / EGFR / p-ERK / ERK / p-Src / Src SOCS3 / p21 / p-STAT3 / STAT3 |
|
25187826 | |
| Growth inhibition assay | Cell proliferation |
|
25187826 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 大鼠體內(nèi)藥代動(dòng)力學(xué)實(shí)驗(yàn)顯示GW 4064口服生物利用度為10%，t1/2 = 3.5小時(shí)。 Fisher大鼠按劑量填喂給藥。7天之后, GW 4064處理的大鼠血清甘油三酯下降并具有劑量依賴特性，ED50 = 20 mg/kg[2]。 |
|
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | Fisher大鼠 |
| Dosages | 0-100 mg/kg | |
| Administration | 口服, 一天兩次 | |
化學(xué)信息&溶解度
| 分子量 | 542.84 | 分子式 | C28H22Cl3NO4 |
| CAS號(hào) | 278779-30-9 | SDF | Download GW4064 SDF |
| Smiles | CC(C)C1=C(C(=NO1)C2=C(C=CC=C2Cl)Cl)COC3=CC(=C(C=C3)C=CC4=CC(=CC=C4)C(=O)O)Cl | ||
| 儲(chǔ)存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 100 mg/mL ( (184.21 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | ||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
g
μL
只
第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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