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[CAS NO. 1208315-24-5] N6022
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-14984 |
| Brand: | MCE |
| CAS: | 1208315-24-5 |
Overview
| MDL | MFCD22123247 |
|---|---|
| Molecular Weight | 414.46 |
| Molecular Formula | C24H22N4O3 |
| SMILES | OC(CCC1=CC=C(N1C2=CC=C(C(N)=O)C=C2C)C(C=C3)=CC=C3N4C=CN=C4)=O |
9 Publications Citing Use of MCE
- [1]Food Chem. 2022 May 24;392:133299.
- [2]Cell Death Dis. 2019 May; 10(5): 329.
- [3]Free Radic Biol Med. 2017 Apr 15;108:445-451.
- [4]Mol Pharmacol. 2016 Oct;90(4):418-26.
- [5]Pediatr Pulm. 2019 Dec;54(12):1989-1996.
- [6]Patent. US20200206195A1
- [7]Patent. US20170209419A1.
- [8]Department of Chemistry and Biochemistry. University of Windsor. 2017 Apr.
- [9]Case Western Reserve University. 2016 Aug.
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
DMSO : ≥ 46 mg/mL ( 110.99 mM )
H 2 O : < 0.1 mg/mL (insoluble)
* "≥" means soluble, but saturation unknown.
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 |
-
1.
-
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
References
- [1] Sun X, et al. Structure-activity relationships of pyrrole based S-nitrosoglutathione reductase inhibitors: pyrrole regioisomers and propionic acid replacement. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3671-5.
- [2] Colagiovanni DB, et al. A nonclinical safety and pharmacokinetic evaluation of N6022: a first-in-class S-nitrosoglutathione reductase inhibitor for the treatment of asthma. Regul Toxicol Pharmacol. 2012 Feb;62(1):115-24.
- [3] Green LS, et al. Mechanism of inhibition for N6022, a first-in-class drug targeting S-nitrosoglutathione reductase. Biochemistry. 2012 Mar 13;51(10):2157-68.
- [4] Thomas M. Raffay, et al. Methods of treating respiratory disorders. Patent. US 20170209419 A1.
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