2. Metabolic Enzyme/Protease
  3. FXR
  4. F44-S101

F44-S101 is an orally active, potent, and selective gut-restricted FXR antagonist with an IC50 of 0.48 μM and lipid-lowering activity. F44-S101 selectively antagonizes intestinal FXR, feedback-activates hepatic FXR, promotes cholesterol metabolism and reduces lipid accumulation. F44-S101 decreases total cholesterol, triglyceride and low-density lipoprotein cholesterol levels. F44-S101 can be used in studies related to hyperlipidemia.

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F44-S101

F44-S101 Chemical Structure

CAS No. : 3124701-00-1

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F44-S101 Related Antibodies

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Description

F44-S101 is an orally active, potent, and selective gut-restricted FXR antagonist with an IC50 of 0.48 μM and lipid-lowering activity. F44-S101 selectively antagonizes intestinal FXR, feedback-activates hepatic FXR, promotes cholesterol metabolism and reduces lipid accumulation. F44-S101 decreases total cholesterol, triglyceride and low-density lipoprotein cholesterol levels. F44-S101 can be used in studies related to hyperlipidemia[1].

In Vitro

F44-S101 is a potent and selective intestine-restricted FXR
antagonist with an IC50 value of 0.48 μM[1].

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

F44-S101 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t Vss CL F
Rat[1] 1 mg/kg i.v. 1.60 h 0.08 h 119.24 ng/mL 47.77 ng·h/mL 24.04 L/kg 20.09 L/h/kg /
Rat[1] 10 mg/kg p.o. 2.05 h 0.33 h 160.25 ng/mL 119.50 ng·h/mL / / 25.02 %
In Vivo

F44-S101 (10-100 mg/kg; intragastric; single dose) dose-dependently reduces serum TC, TG, and LDL-C levels, and reverses liver enzyme elevations in Triton-induced hyperlipidemic male C57BL/6 mice, with the 100 mg/kg dose decreasing serum TC by 18.9% and TG by 32.2%[1].
F44-S101 (10-100 mg/kg; intragastric; 4 weeks) dose-dependently reduces serum TC, hepatic TC, serum LDL-C, inguinal adipose mass, and serum ceramide levels in HFD-induced hyperlipidemic male C57BL/6 mice, with the 100 mg/kg dose decreasing serum TC by 25.6% and hepatic TC by 17.3%[1].

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

Animal Model: C57BL/6 (male, 8 weeks old; Triton WR-1339-induced acute hyperlipidemia)[1]
Dosage: 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration: intragastric
Result: Significantly decreased serum total cholesterol (TC) by 18.9% and serum triglycerides (TG) by 32.2% at 100 mg/kg compared to vehicle controls.
Significantly reduced serum low-density lipoprotein cholesterol (LDL-C) levels by over 38% across all dose groups compared to vehicle controls.
Reversed Triton-induced elevations in plasma alanine transaminase (ALT) and aspartate transaminase (AST) levels.
Animal Model: C57BL/6 (male, adult; high-fat diet-induced hyperlipidemia)[1]
Dosage: 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration: intragastric; 4 weeks
Result: Significantly reduced serum TC by 25.6% and hepatic TC by 17.3% at 100 mg/kg compared to vehicle controls.
Significantly reduced plasma LDL-C concentrations by 30.8% at 100 mg/kg compared to vehicle controls, with LDL-C levels approaching control group levels.
Dose-dependently reduced inguinal adipose tissue mass and the ratio of inguinal adipose tissue to body weight; showed a significant reduction in inguinal fat weight at 100 mg/kg compared to vehicle controls.
Significantly reduced serum ceramide levels in a dose-dependent manner compared to vehicle controls.
Had no significant effect on ALT, AST, brown adipose tissue weight, or epididymal fat weight.
Molecular Weight

573.08

Formula

C27H25ClN2O6S2
CAS No.
SMILES

CCN(S(=O)(C1=CC2=C(SC(C(O)=O)=C2)C=C1)=O)C3=CC=C(C=C3CN(C(C4CC4)=O)CC5=CC=CO5)Cl
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-S101 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-S1013124701-00-1FXRNR1H4male C57BL/6 miceFarnesoid X receptorTriton-induced hyperlipidemic micelipid accumulationlipid metabolic disordersHFD-induced hyperlipidemic micehyperlipidemiaintestinal FXRhepatic FXRcholesterol metabolismInhibitorinhibitorinhibit

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