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Art. -Nr.: HY-16443

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S-4048

S-4048 is a glucose-6-phosphate translocase modulator and hypoglycemic agent. S-4048 is taken up by hepatocytes via OATP-1 and is rapidly eliminated via the hepatobiliary system in rats. S-4048 blocks glucose-6-phosphate translocase, prevents glucose-6-phosphate from entering the endoplasmic reticulum, and thereby interferes with the glucose-6-phosphatase system (i.e., the final step of hepatic gluconeogenesis and glycogenolysis) to regulate hepatic glucose production. S-4048 completely inhibits glucose production from pyruvate in GLUT2-deficient hepatocytes without affecting the release of cytoplasmic glucose. S-4048 effectively reduces blood glucose levels in rats and has been used in studies related to type 2 diabetes.

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CAS. Nr.: 173534-37-7
Formel: C₃₂H₃₀ClN₃O₇
Molecular Weight:604.05

Speicherung:

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

Data Sheet (285 KB)

S-4048 Chemical Structure

CAS. Nr.: 173534-37-7

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50：9.4 nM for rat microsomes.

In Vitro

S-4048 (10 μM; 30-60 min) does not inhibit the release of cytosolic glucose from GLUT2^-/- mouse hepatocytes, indicating this minor glucose release pathway does not require glucose re-entry into the endoplasmic reticulum via glucose-6-phosphate translocase^[1].

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

In Vivo

S-4048 (30-50 mg/kg; i.v.) reduces blood glucose levels in starved male Wistar rats, with a short-acting effect after 50 mg/kg i.v. bolus injection and sustained 50% reduction during 30 mg/kg/h i.v. infusion^[2].
S-4048 (10 mg/kg; i.v. bolus injection) undergoes rapid hepatobiliary elimination in male Wistar rats, with 57% of the 10 mg/kg i.v. bolus dose excreted as parent compound in bile within 30 minutes, driving a high plasma clearance^[2].
S-4048 (10-50 mg/kg; i.v. bolus injection) exhibits a short blood glucose lowering effect and comparable hepatobiliary elimination in male mrp-2 deficient GY/TR3 rats relative to Wistar rats^[2].

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

Animal Model:

Wistar (male, 280-360 g, starved for 24 hours prior to experiments)^[2]
Dosage:

50 mg/kg (blood glucose reduction); 30 mg/kg/h (sustained blood glucose reduction)
Administration:

i.v. bolus injection; i.v. infusion
Result:

Reduced blood glucose to maximum at 45 minutes, with levels returning to control values within 60 minutes after 50 mg/kg i.v. bolus injection.
Stabilized blood glucose levels at approximately 50% of the control group level after 60 minutes during constant 30 mg/kg/h i.v. infusion.

Animal Model:

Wistar (male, 280-360 g, starved for 24 hours prior to experiments)^[2]
Dosage:

10 mg/kg
Administration:

i.v. bolus injection
Result:

Recovered 57% of the total administered dose as parent compound in bile within the first 30 minutes after administration.
Reached initial plasma concentrations of approximately 14 μmol/l, with a plasma clearance of about 80 mL/min/kg and an estimated half-life of about 10 minutes.

Animal Model:

GY/TR3 (male, 280-360 g, mrp-2 deficient mutant Wistar strain, starved for 24 hours prior to experiments)^[2]
Dosage:

50 mg/kg (blood glucose study); 10 mg/kg (hepatobiliary elimination study)
Administration:

i.v. bolus injection
Result:

Lowered blood glucose with effect lasting as short as in Wistar rats, with levels returning to control values within 60-90 minutes after 50 mg/kg i.v. bolus injection.
Exhibited hepatobiliary elimination profile similar to that in Wistar rats after 10 mg/kg i.v. bolus injection.

Chemical Information

CAS. Nr. 173534-37-7
Molecular Weight 604.05
Formel C₃₂H₃₀ClN₃O₇
SMILES

O=C([C@]1(OC[C@H]2[C@@H](C3=CC=C(Cl)C=C3)C2)C[C@@H](O)[C@@H](O)[C@H](OC(/C=C(N4C=NC5=NC=CC=C54)/C6=CC=CC=C6)=O)C1)O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (285 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Hosokawa M, et al. Glucose release from GLUT2-null hepatocytes: characterization of a major and a minor pathway. Am J Physiol Endocrinol Metab. 2002;282(4):E794-E801. [Content Brief]

[2]. Herling A W, et al. Prolonged blood glucose reduction in mrp-2 deficient rats (GY/TR−) by the glucose-6-phosphate translocase inhibitor S 3025[J]. Biochimica et Biophysica Acta (BBA)-General Subjects, 2002, 1569(1-3): 105-110.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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