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 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.

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F44-A13 Chemical Structure

F44-A13 Chemical Structure

CAS No. : 1338190-14-9

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F44-A13 Related Antibodies

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Description

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

 

In Vitro

F44-A13 demonstrates high selectivity towards various nuclear receptors, including retinoic acid receptor α/β/γ (RARα/β/γ), retinoid X receptor α/β/γ (RXRα/β/γ), pregnane X receptor (PXR), peroxisome proliferators-activated receptors α/β (PPARα/β), thyroid hormone receptor β (THRβ), and retinoic acid receptor-related orphan receptors γ (RORγ)[1].
F44-A13 (50 μM, 24 h) inhibites FXR transcriptional activity in a dose-dependent manner in the presence of 50 μM CDCA (HY-76847) with an IC50 value of 3.0 μM. F44-A13 is a low-toxicity, highly selective FXR antagonist[1].
F44-A13 (F44-A13: 3, 10, 30 μM; CDCA: 100 μM; 24 hours) can improve cholesterol metabolism and reduce cholesterol activity by inducing the expression of CYP7A1. F44-A13 can decrease the expression level of Shp and Bsep, and increase the expression level of CYP7A1[1].

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

F44-A13 Related Antibodies

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.
In Vivo

F44-A13 (20, 40 mg/kg; Oral gavage (p.o.) and Intraperitoneal injection (i.p.); 4 days) effectively reduces the levels of TC, TG and LDL-C in a C57BL/6 mice model[1].

MedChemExpress (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%.
Molecular Weight

544.71

Formula

C28H40N4O5S
CAS No.
SMILES

CCN(C1=CC(OS(=O)(C2=CC=C(C=C2)NC(C)=O)=O)=C(C=C1)CN(C(NC(C)(C)C)=O)CC3CC3)CC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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F44-A13 Related Classifications

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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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