2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Cell Cycle/DNA Damage
  3. FXR Cytochrome P450 RAR/RXR PPAR ROR
  4. F44-A13

F44-A13 是一种具有口服活性、高选择性的 farnesoid X receptor (FXR) 拮抗剂，IC50 值为 1.1 μM。F44-A13 通过诱导 CYP7A1 的表达，能优化胆固醇代谢并降低其活性。F44-A13 能降低小鼠模型中胆固醇、甘油三酯和低密度脂蛋白胆固醇 (LDL-C) 的水平。F44-A13 可用于伴有脂质紊乱的代谢性疾病的研究。

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F44-A13 Chemical Structure

F44-A13 Chemical Structure

CAS No. : 1338190-14-9

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F44-A13 相关抗体

Top Publications Citing Use of Products

查看 Cytochrome P450 亚型特异性产品:

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CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

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PPARα PPARβ/δ PPARγ PPAR PPARδ

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RORγ RORα RORβ

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders[1].

IC50 & Target

PPARα

 

PPARβ

 

RXR α

 

RXRβ

 

RXRγ

 

RORγ

 

体外研究
(In Vitro)

F44-A13 对多种核受体具有高度选择性，包括视黄酸受体 α/β/γ (RARα/β/γ)，视黄酮 X 受体 α/β/γ，(RXRα/β/γ)，孕烷 X 受体 (PXR)，过氧化物酶体增殖激活受体 α/β (PPARα/β)，甲状腺激素受体 β (THRβ)，以及与视黄酸受体相关的孤儿受体 γ (RORγ)[1]。
F44-A13 (50 μM, 24 小时) 在 50 μM CDCA (HY-76847) 的存在下，以剂量依赖性方式抑制 FXR 的转录活性，IC50 值为 3.0 μM，F44-A13 为低毒性、高选择性的 FXR 拮抗剂[1]。
F44-A13 (F44-A13: 3, 10, 30 μM; CDCA: 100 μM; 24 小时) 能通过诱导 CYP7A1 的表达改善胆固醇代谢，降低胆固醇的活性。F44-A13 能使 Shp 和 Bsep 的表达水平降低，CYP7A1 的表达水平升高[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

F44-A13 相关抗体:

Cell Viability Assay[1]

Cell Line: HepG2 , HEK293A cells
Concentration: 100 μM
Incubation Time: 24h
Result: Was not cytotoxic to HepG2 and HEK293A cells

RT-PCR[1]

Cell Line: HepG2 cells
Concentration: F44-A13: 3, 10, 30 μM; CDCA: 100 μM
Incubation Time: 24h
Result: Was able to reverse the regulation of FXR downstream target genes Shp, Bsep and Cyp7a1 by CDCA in a dose-dependent manner.
Decreased the expression level of Shp and Bsep, and increased the expression level of Cyp7a1.
体内研究
(In Vivo)

F44-A13 (20, 40 mg/kg; 口服和腹腔注射; 4 天) 在 C57BL/6 mice 小鼠模型中能有效地降低总胆固醇 (TC)，甘油三酯 (TG) 和低密度脂蛋白胆固醇 (LDL-C) 的水平[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice[1]
Dosage: 20, 40 mg/kg
Administration: Intraperitoneal injection (i.p.) and Oral gavage (p.o.); 4 days
Result: Intraperitoneal injection significantly reduced TC levels by more than 28%, and oral administration significantly reduced TC levels in a dose-dependent manner.
Reduced TG levels by more than 30% at both 20 and 40 mg/kg orally, while intraperitoneal injection did not significantly reduce TG levels.
Oral doses of 20 and 40 mg/kg were effective in reducing LDL-C levels by 12% and 23%, and intraperitoneal injections by 38%.
分子量

544.71

Formula

C28H40N4O5S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

F44-A13 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

F44-A131338190-14-9FXRCytochrome P450RAR/RXRPPARRORNR1H4CYPsRetinoic acid receptorsRetinoid X receptorsPeroxisome proliferator-activated receptorsRAR-related orphan receptorP-acetylaminobenzene sulfonate derivativesLipid-lowering activity C57BL/6 miceCYP7A1CDCAInhibitorinhibitorinhibit

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