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Turofexorate Isopropyl

产品编号 T6053 CAS 629664-81-9

别名: XL335, FXR-450, WAY-362450, 妥芬异丙酯

Turofexorate Isopropyl (XL335) 是一种口服有效的，选择性 FXR 激动剂，EC50为 4 nM。

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

Turofexorate Isopropyl Chemical Structure

Turofexorate Isopropyl, CAS 629664-81-9

规格	价格/CNY	货期
1 mg	￥ 233	现货
2 mg	￥ 329	现货
5 mg	￥ 538	现货
10 mg	￥ 745	现货
25 mg	￥ 1,490	现货
50 mg	￥ 2,320	现货
100 mg	￥ 3,480	现货
1 mL * 10 mM (in DMSO)	￥ 596	现货

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选择批次

纯度: 99.75%

纯度: 99.33%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Turofexorate Isopropyl (XL335) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM
靶点活性	FXR:4 nM(EC50)
体外活性	WAY-362450 binds to the ligand-binding domain (LBD) of human FXR. WAY-362450 resides in a predominately hydrophobic pocket with only a few polar atoms making contact with WAY-362450. WAY-362450 promotes transcription of the human BSEP, human SHP, and mouse IBABP genes utilizing reporter constructs with EC50 of 17, 230, and 33 nM, respectively in promoter assays. WAY-362450 at concentration of 1 μM significantly induces mRNAs encoding for BSEP, SHP, and IBABP in human cell cultures to 13-, 2-, and 20-fold, respectively. [1] WAY-362450 at concentration of 1 μM suppresses interleukin-6-induced CRP expression in human Hep3B hepatoma cells, and the inhibitory effect is attenuated when knockdown of FXR by short interfering RNA.
体内活性	WAY-362450 administrated intravenously or orally at does of 3 mg/kg in rats with a protracted half-life of 25 h, modest volume of distribution, and low clearance of 3.3 L/kg. WAY-362450 administered orally at dose of 10 mg/kg in normal C57bl/6 mice for a period of 7 days significantly lowers triglycerides to 62.0 ± 6.4 mg/dL and total cholesterol to 78.1 ± 5.0 mg/dL. WAY-362450 administered orally at dose of 1 and 3 mg/kg daily for 6 weeks in LDLR?/? mice, triglycerides is lowered by 19% and 39%, respectively, total cholesterol is lowered by 23% and 50%, respectively and lesion formation by 18% and 36%, respectively. [1] WAY-362450 intraperitoneally administrated at dose of 30 mg/kg daily for 4 days in wild type C57BL/6 mice attenuates lipopolysaccharide-induced serum amyloid P component and serum amyloid A3 mRNA levels in the liver. [3] WAY-362450 orally administered at dose of 30 mg/kg/day for 4 weeks in adult male C57BL/6 mice reduces in?ammatory cell in?ltration and hepatic ?brosis, the reduction in in?ammatory cell in?ltration correlates with deceased serum levels of keratinocyte derived chemokine (mKC) and MCP 1 and decreased hepatic gene expression of MCP-1 and VCAM-1, and the reduction of hepatic ?brosis by WAY-362450 treatment corresponded to a reduction in hepatic gene expression of ?brosis markers. [3] WAY-362450 administrated orally at dose of 30 mg/kg in LDLR?/? and apoE?/? mice blocks diet-induced hypertriglyceridemia and elevations of non-HDL cholesterol and produced a near complete inhibition of aortic lesion formation, WAY-362450 also induced small heterodimer partner (SHP) expression and repressed cholesterol 7α-hydroxylase (CYP7A1) and sterol 12 α-hydroxylase (CYP8B1) expression. [4]
激酶实验	Inhibition of p38α: Inhibition of p38α is determined using recombinant human p38α in a standard filter binding protocol using ATP[γ-33P] and EGFR 21-mer peptide as substrate. Functional inhibition of TNFα in murine peritoneal macrophages is determined using LPS stimulation in the presence of LY2228820. To assess p38α activity in cells more directly, RAW 264.7 cells are treated with LY2228820 and then stimulated with anisomycin. The level of p38α activity is detected using a phosphoMAPKAPK-2 (pMK2) (Thr 334) antibody which reacts with a residue specifically phosphorylated by p38α.
细胞实验	WAY-362450 is prepared in DMSO and stored, and then diluted with appropriate medium (DMSO 0.01%) before use[2]. Mouse AML12 cells are plated at 200,000 cells/well on the 24-well plate in 1 mL of growth medium [DMEM/F12 10% FBS, 1% penicillin and streptomycin, 1% insulin-transferrin-selenium-G supplement (ITS), 0.1% Dexamethasone (40 ng/mL)/well. The cells are treated with increasing concentrations of WAY-362450 (0.001, 0.01, 0.1, 1 and 10 μM) or GW4064 for 24 h. Total RNA is prepared and analyzed by real-time RT-PCR, and short heterodimer partner (SHP) expression is normalized to GAPDH and reported as fold induction vs. vehicle-treated cells. Preplated 24-well plates of human male primary hepatocytes with matrigel overlay are obtained from Cellz Direct. Cells are maintained in serum-free Williams medium E and supplemented with penicillin/streptomycin, dexamethasone, ITS, L-glutamine, and HEPES buffer. They are treated overnight with vehicle (0.01% DMSO) or increasing concentrations of WAY-362450 or GW4064. Total RNA is purified using the Qiagen RNeasy clean kit, and gene expression is quantified by real-time RT-PCR with the Qiagen Quantitech kit using an ABI 7900. The relative amount of mRNA is normalized to 18S ribosomal RNA, and data shown represent an average of two independent experiments[2].

别名	XL335, FXR-450, WAY-362450, 妥芬异丙酯
分子量	438.47
分子式	C25H24F2N2O3
CAS No.	629664-81-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 31 mg/mL (70.7 mM)

Ethanol: 2 mg/mL (4.56 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / Ethanol	1 mM	2.2807 mL	11.4033 mL	22.8066 mL	57.0164 mL
DMSO	5 mM	0.4561 mL	2.2807 mL	4.5613 mL	11.4033 mL
	10 mM	0.2281 mL	1.1403 mL	2.2807 mL	5.7016 mL
	20 mM	0.114 mL	0.5702 mL	1.1403 mL	2.8508 mL
	50 mM	0.0456 mL	0.2281 mL	0.4561 mL	1.1403 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Flatt B, et al. J Med Chem, 2009, 52(4), 904-907. 2. Zhang S, et al. J Hepatol, 2009, 51(2), 380-388. 3. Zhang S, et al. Biochem Biophys Res Commun, 2009, 379(2), 476-479. 4. Hartman HB, et al. J Lipid Res, 2009, 50(6), 1090-1100. 5. Zheng W, Lu Y, Tian S, et al. Structural insights into the heterodimeric complex of the nuclear receptors FXR and RXR[J]. Journal of Biological Chemistry. 2018 Aug 10;293(32):12535-12541.

文献引用

1. Zheng W, Lu Y, Tian S, et al. Structural insights into the heterodimeric complex of the nuclear receptors FXR and RXR. Journal of Biological Chemistry. 2018 Aug 10;293(32):12535-12541 2. Tschuck J, Theilacker L, Rothenaigner I, et al.Farnesoid X receptor activation by bile acids suppresses lipid peroxidation and ferroptosis.Nature Communications.2023, 14(1): 6908.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Turofexorate Isopropyl 629664-81-9 Autophagy Metabolism FXR WAY 362450 FXR 450 Inhibitor XL335 inhibit FXR450 FXR-450 WAY-362450 WAY362450 妥芬异丙酯 XL 335 NR1H4 XL-335 inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

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Turofexorate Isopropyl

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords