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Art. -Nr.: HY-175422

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K-833

K-833 is a GPR119 agonist with EC₅₀ values of 39.8 nM (human), 100nM (mouse), 75.4 nM (rat) and 12.6 nM (dog). K-833 demonstrates a modest increase in GLP-1 secretion and leads to a synergistic increase in GLP-1 levels when combined with AM-5262 (HY-16619) in acute gut peptide secretion assays in mice. K-833 can be used in studies on weight loss.

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CAS. Nr.: 2639936-77-7
Formel: C₃₀H₄₃ClFN₅O₇
Molecular Weight:640.14

Speicherung:

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

Data Sheet (264 KB)

K-833 Chemical Structure

CAS. Nr.: 2639936-77-7

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

Biologische Aktivität
- Beschreibung
- In Vitro
- Parmacokinetics
- In Vivo
- Clinical Trial
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

In Vitro

K-833 shows modest antagonism of the human M1 receptor (IC₅₀ = 4.5 μM), inhibition of agonist binding to the human nonselective sigma receptors (IC₅₀ = 2.7 μM) and moderate reversible inhibition of the CYP2B6 (IC₅₀ = 8.6 μM)^[1].

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

Parmacokinetics

Species	Dose	Route	CL	V_dss	T_1/2	C_max	F
Dog^[1]	1/2 mg/kg	p.o.	1.8 mL/min/kg	0.39 L/kg	4.7 h	0.154 μM	5 %
Mice^[1]	1/3 mg/kg	p.o.	1.5 mL/min/kg	0.42 L/kg	3.5 h	0.054 μM	1.5 %
Rat^[1]	1/5 mg/kg	p.o.	9.0 mL/min/kg	0.50 L/kg	3.8 h	0.011 μM	0.2 %

In Vivo

K-833 (30 mg/kg, i.g., single dose) demonstrates a modest increase in GLP-1 secretion in acute gut peptide secretion assays in mice^[1].

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

Animal Model:

Male 10-12 week old C57BL/6J mice^[1]
Dosage:

30 mg/kg or combined with AM-5262 (HY-16619) (30 mg/kg)
Administration:

i.g. for a single dose
Result:

Led to a modest increase in GLP-1 secretion.
Led to a synergistic increase in GLP-1 levels when combined with AM-5262.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 2639936-77-7
Molecular Weight 640.14
Formel C₃₀H₄₃ClFN₅O₇
SMILES

OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)CNCC1CN(C(CC2=CC=C(OCCCC3CCN(C4=NC=C(Cl)C=N4)CC3)C=C2F)=O)C1
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 (264 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]. Moyes CR, et al. Discovery of Gut-Targeted GPR40 Agonist K-757 and GPR119 Agonist K-833, a Combination Treatment for Metabolic Disorders. J Med Chem. 2025 Jul 24. [Content Brief]

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.

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MOQ

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100 mg

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