[CAS NO. 1208315-24-5]  N6022

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PRODUCTS SPECIFICATIONS [1208315-24-5]

Catalog
HY-14984
Brand
MCE
CAS
1208315-24-5

DESCRIPTION [1208315-24-5]

Overview

MDLMFCD22123247
Molecular Weight414.46
Molecular FormulaC24H22N4O3
SMILESOC(CCC1=CC=C(N1C2=CC=C(C(N)=O)C=C2C)C(C=C3)=CC=C3N4C=CN=C4)=O

For research use only. We do not sell to patients.


Summary

N6022 is a potent, selective, reversible, and efficacious S-Nitrosoglutathione reductase(GSNOR) inhibitor with IC 50 of 8 nM.


IC50 & Target

IC50: 8 nM (GSNOR) [2]


In Vitro

N6022 shows concentration-dependent binding to rat plasma proteins. N6022 has more effect on ATP at lower drug concentrations (20 μM) than on GSH [1] . N6022 binds in the GSNO substrate binding pocket like a competitive inhibitor with an IC 50 of 8 nM and a K i of 2.5 nM. N6022 is uncompetitive with cofactors NAD + and NADH [2] .

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


In Vivo

N6022 (50 mg/kg)-treated rats show a slight increase in the incidence of granulomas. In serum, N6022 remains in solution up to 5 mg/mL [1] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT01746784 Nivalis Therapeutics, Inc.
Cystic Fibrosis
February 2014 Phase 1
NCT01147406 Nivalis Therapeutics, Inc.
Healthy
August 2010 Phase 1

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 46 mg/mL ( 110.99 mM )

H 2 O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4128 mL 12.0639 mL 24.1278 mL
5 mM 0.4826 mL 2.4128 mL 4.8256 mL
10 mM 0.2413 mL 1.2064 mL 2.4128 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.03 mM); Clear solution

* All of the co-solvents are available by MCE.