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Art. -Nr.: HY-182021

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NNMT-IN-8

NNMT-IN-8 is a non-SAM-mimicking bisubstrate inhibitor and a selective methyltransferase NNMT inhibitor, with IC₅₀ values of 0.0084 μM and 0.0085 μM against human NNMT, and an IC₅₀ of 0.0072 μM against mouse NNMT. NNMT-IN-8 exhibits prominent renal distribution characteristics and moderate bioavailability in rodents. NNMT-IN-8 dose-dependently inhibits renal NNMT in renal fibrosis models, thereby exerting antifibrotic effects. NNMT-IN-8 can be used to investigate the mechanisms of renal fibrosis.

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CAS. Nr.: 3124204-81-2
Formel: C₂₃H₂₅FN₄O₂S
Molecular Weight:440.53

Speicherung:

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

NNMT-IN-8 Chemical Structure

CAS. Nr.: 3124204-81-2

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Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

Alle Amine N-methyltransferase Isoform-spezifische Produkte anzeigen :

PNMT
NNMT

In Vitro

NNMT-IN-8 (compound 16) inhibits NNMT activity in cells overexpressing human NNMT, with an IC₅₀ of 0.25 μM^[1].
NNMT-IN-8 exhibits metabolic stability in human liver microsomes, rat liver microsomes, and mouse liver microsomes, with 79%, 34%, and 23% remaining after 30 min of incubation^[1].
NNMT-IN-8 (3 μM) inhibits hERG current by 15%, indicating a low risk of cardiotoxicity^[1].

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

In Vivo

In rat pharmacokinetic studies, NNMT-IN-8 (compound 16) exhibits moderate total clearance (C_Ltot=32 mL/min/kg), a half-life (t_1/2) of 1.7 h, a maximum plasma concentration (C_max) of 38 nM, and a relatively high serum free fraction (f_u= 30%/20%). NNMT-IN-8 also shows significant renal distribution with a kidney/plasma partition coefficient of 16, as well as moderate oral bioavailability (F=26%)^[1].

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

Chemical Information

CAS. Nr. 3124204-81-2
Molecular Weight 440.53
Formel C₂₃H₂₅FN₄O₂S
SMILES

O=C1SC2=C(NCC34CCC(CC3)(C4)NCC5=C(F)C(C(N)=O)=CC=C5)C=CC=C2N1
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]. Yoshida S, et al. Structure-Based Drug Discovery of Non-SAM-Mimetic Bisubstrate Inhibitors against Nicotinamide N-Methyltransferase[J]. ACS Medicinal Chemistry Letters, 2026.

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.

Keywords

100 mg

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