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Art. -Nr.: HY-183919

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ACC2-IN-1

ACC2-IN-1 is an orally active, selective inhibitor of acetyl-CoA carboxylase 2 (ACC2), with an IC₅₀ of 1.9 nM against human targets. ACC2-IN-1 acts as a reducing agent to decrease malonyl-CoA levels in skeletal muscle and exhibits a favorable CYP450 inhibition profile. ACC2-IN-1 can be used in the research of type 2 diabetes.

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CAS. Nr.: 2237229-78-4
Formel: C₂₀H₂₀ClN₃O₃S
Molecular Weight:417.91

Speicherung:

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

ACC2-IN-1 Chemical Structure

CAS. Nr.: 2237229-78-4

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

CYP2C19

18 μM (IC₅₀)

CYP2C9

13 μM (IC₅₀)

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen :

In Vitro

ACC2-IN-1 (compound 2e) potently inhibits human ACC2 with an IC₅₀ of 1.9 nM and is 1026-fold selective over human ACC1^[1].
ACC2-IN-1 (30 min) exhibits high metabolic stability, with 91% and 100% remaining after incubation in human and rat liver microsomes, respectively^[1].
ACC2-IN-1 has an acceptable CYP450 inhibition profile, with no inhibition of CYP1A2, CYP2D6, or CYP3A4 at concentrations up to 20 μM, and IC₅₀ values of 18 μM for CYP2C19 and 13 μM for CYP2C9^[1].

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

Parmacokinetics

Species	Dose	Route	CL_total	AUC	C_max	Bioavailability
Mice^[1]	0.2 mg/kg	i.v.	0.354 mL/min/kg	/	/	/
Mice^[1]	2.5 mg/kg	p.o.	/	99800 ng·h/mL	4230 ng/mL	83.5 %

In Vivo

ACC2-IN-1 (compound 2e) (1.0-2.5 mg/kg; p.o.; single dose) produces dose-dependent reductions in skeletal muscle malonyl-CoA levels in C57BL/6 mice^[1].

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

Animal Model:

C57BL/6^[1]
Dosage:

1.0 mg/kg; 2.5 mg/kg
Administration:

p.o.; single dose
Result:

Reduced skeletal muscle malonyl-CoA levels by 20%.
Reduced skeletal muscle malonyl-CoA levels by 41%.
Achieved corresponding plasma drug levels of 1130 ng/mL and 2621 ng/mL for the 1.0 mg/kg and 2.5 mg/kg doses, respectively.

Chemical Information

CAS. Nr. 2237229-78-4
Molecular Weight 417.91
Formel C₂₀H₂₀ClN₃O₃S
SMILES

ClC1=C2C(N=C(S2)OCC)=CC=C1OC3=CC=C(C=N3)/C=C/[C@H](C)NC(C)=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

Handling Instructions (2659 KB)

Verweise

[1]. Nishiura Y, et al. Discovery of a novel olefin derivative as a highly potent and selective acetyl-CoA carboxylase 2 inhibitor with in vivo efficacy. Bioorg Med Chem Lett. 2018;28(14):2498-2503. [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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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
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ACC2-IN-1

Alle Cytochrome P450 Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

ACC2-IN-1 Related Classifications

HY-183919 Related Classifications