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Cat. No.: HY-182454

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GPR119 agonist 4

GPR119 agonist 4 is a GPR119 agonist and oral glucose-lowering agent with a human GPR119 EC₅₀ of 42 nM.GPR119 agonist 4 activates GPR119.GPR119 agonist 4 reduces blood glucose area under the curve in an oral glucose tolerance test.GPR119 agonist 4 exhibits improved clearance in liver microsomes.GPR119 agonist 4 can be used for the research of type 2 diabetes mellitus.

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CAS No.: 1353004-92-8
Formule: C₂₄H₂₃ClN₆O₃S
Masse moléculaire:511.00

Stockage:

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

GPR119 agonist 4 Chemical Structure

CAS No.: 1353004-92-8

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Fluorescent Dye

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

Activité biologique
- Description
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
CHO-K1	IC₅₀	10 μM Compound: 26	Cytotoxicity in CHOK1 cells by CCK8 assay Cytotoxicity in CHOK1 cells by CCK8 assay	[PMID: 28648463]

In Vitro

GPR119 agonist 4 (Compound 26) has improved metabolic stability, with clearance values of 113 μL/min/mg/protein in human liver microsomes and 108 μL/min/mg/protein in mouse liver microsomes^[1].

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

Parmacokinetics

Species	Dose	Route	CL_plasma	V_ss	T_1/2	C_max	AUC	Bioavailability
Mice^[1]	0.5 mg/kg	i.v.	6.5 mL/min/kg	2.3 L/kg	5.1 h	/	/	/
Mice^[1]	10 mg/kg	p.o.	/	/	/	2015 ng/mL	9386 ng·h/mL	37 %

In Vivo

GPR119 agonist 4 (Compound 26) (10 mg/kg; p.o.; single dose) induces a 33% reduction in blood glucose AUC_0-t at a dose of 10 mg/kg in an oral glucose tolerance test in C57BL/6N mice^[1].

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

Animal Model:

C57BL/6N mice^[1]
Dosage:

10 mg/kg
Administration:

p.o.; single dose
Result:

Induced a 33% reduction in blood glucose area under the curve (AUC) during the oral glucose tolerance test.

Chemical Information

CAS No. 1353004-92-8
Masse moléculaire 511.00
Formule C₂₄H₂₃ClN₆O₃S
SMILES

O=S(C1=CC=C2C(CCN2C3=NC=NC4=C3OC=C4C5CCN(CC5)C6=NC=C(C=N6)Cl)=C1)(C)=O
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Koshizawa T, et al. Optimization of a novel series of potent and orally bioavailable GPR119 agonists. Bioorg Med Chem Lett. 2017;27(15):3249-3253. [Content Brief]

Calculators

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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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