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Cat. No.: HY-181876

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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.

For research use only. We do not sell to patients.

CAS No.: 3124701-00-1
Formula: C₂₇H₂₅ClN₂O₆S₂
Molecular Weight:573.08

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

F44-S101 Chemical Structure

CAS No.: 3124701-00-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
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Bioz

Biological Activity

Description

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.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	V_ss	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.

Chemical Information

CAS No. 3124701-00-1
Molecular Weight 573.08
Formula C₂₇H₂₅ClN₂O₆S₂
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

Handling Instructions (2659 KB)

References

[1]. Su L, et al. Discovery of N-Ethyl Sulfonamide Derivatives as Potent Intestinal-Restricted Farnesoid X Receptor Antagonists for the Treatment of Metabolic Disorders. J Med Chem. 2026;69(5):5749-5786. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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