264W94

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264W94 is a potent ileal bile acid transporter (IBAT) inhibitor and a new cholesterol lowering agent. 264W94 has CYP7A1 induction, and antilipemic action.

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

264W94 Chemical Structure

CAS No. : 178961-24-5

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Description

264W94 is a potent ileal bile acid transporter (IBAT) inhibitor and a new cholesterol lowering agent. 264W94 has CYP7A1 induction, and antilipemic action^[1].

IC₅₀ & Target

IBAT^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	180 nM Compound: 1, 264W94	Inhibition of human ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis Inhibition of human ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis	[PMID: 23678871]
HEK293	IC₅₀	22 nM Compound: 1, 264W94	Inhibition of rat ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis Inhibition of rat ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis	[PMID: 23678871]
HEK293	IC₅₀	3 nM Compound: 1, 264W94	Inhibition of mouse ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis Inhibition of mouse ASBT expressed in HEK293 cells assessed as inhibition of [3H]-taurocholate uptake after 90 mins by scintillation counting analysis	[PMID: 23678871]

In Vitro

264W94 (0, 0.1, 0.25, 0.5 μM) inhibits human IBAT-specific transport of 5 μM TC by 14% to 75% in a concentration-dependent manner with IC₅₀ of 0.25 μM in CHO-hIBAT cells^[1].

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

In Vivo

264W94 (orally; 0.03-1.0 mg/kg; twice a day for 3.5 days) dose-dependently attenuates diet-induced increases in serum LDL+VLDL-C, as well as the decrease in HDL-C^[1].
264W94 (orally; 0.003, 0.01, 0.03, 0.1 mg/kg; twice a day for 2 days) increases fecal excretion of ⁷⁵SeHCAT in a dose-dependent manner^[1].
264W94 (0.001, 0.01, 0.1, 1, and 10 mg/kg; twice a day for 2 weeks) reduces dose-dependently plasma glucose in male ZDF (ZDF/GmiCrl-fa/fa) rats. Treatment of 264W94 prevents the decline of insulin dose-dependently without an increase in proinsulin levels^[2].

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

Animal Model:	Male Sprague Dawley rats (CD, Charles River, 270-310 gm)^[1]
Dosage:	0.03, 0.1, 0.3, 1.0 mg/kg
Administration:	Orally; twice a day (9:00 am and 3:30 pm) for 3.5 days
Result:	Dose-dependently attenuated diet-induced increases in serum LDL+VLDL-C, as well as the decrease in HDL-C.

Molecular Weight

417.56

Formula

C₂₃H₃₁NO₄S

CAS No.

178961-24-5

SMILES

COC1=C(OC)C=C(C2=C1)[C@@H](C3=CC=CC=C3)N[C@](CC)(CCCC)CS2(=O)=O

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]. Root C, et al. Ileal bile acid transporter inhibition, CYP7A1 induction, and antilipemic action of 264W94. J Lipid Res. 2002 Aug;43(8):1320-30. [Content Brief]

[2]. Chen L, et al. Inhibition of apical sodium-dependent bile acid transporter as a novel treatment for diabetes. Am J Physiol Endocrinol Metab. 2012 Jan 1;302(1):E68-76. [Content Brief]

264W94 Related Classifications

Metabolic Disease

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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:

264W94178961-24-5Apical Sodium-Dependent Bile Acid TransporterASBTIleal Bile Acid TransporterIBATSLC10A2Inhibitorinhibitorinhibit

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