Welcome to Shanghai Probechem Biochemicals Co Ltd !Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : Nurr1 agonist 29
Catalog No.: PC-20768Not For Human Use, Lab Use Only.
Nurr1 agonist 29 is a potent, selective nuclear receptor related 1 (Nurr1, NR4A2) agonist with EC50 of 0.11 uM.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Nurr1 agonist 29 is a potent, selective nuclear receptor related 1 (Nurr1, NR4A2) agonist with EC50 of 0.11 uM.
Nurr1 agonist 29 displays selectivity over DHODH as well as the Nurr1 related receptors Nur77 and NOR1.
Nurr1 agonist 29 exhibits high-affinity binding to the Nurr1 LBD in ITC (Kd = 0.3 μM) and activates full-length human Nurr1 on the monomer (NBRE, EC50=0.22 μM) and the RXR-heterodimer (DR5, EC50=0.36 μM) response elements.
Nurr1 agonist 29 induces mRNA expression of the Nurr1-regulated genes tyrosine hydroxylase (TH) and vesicular amino acid transporter 2 (VMAT2) in Nurr1-expressing human astrocytes (T98G), demonstrating cellular target engagement.
Nurr1 agonist 29 shows no cytotoxic effects in a multiplex toxicity assay in COS-7 cells.
Nurr1 agonist 29 (5 mg/kg) produced a very favorable pharmacokinetic profile in rats with a 4.4 h half-life, 56 μM peak plasma concentration, and 89% bioavailability.
| M.Wt | 379.39 | |
| Formula | C22H18FNO4 | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
10 mM in DMSO |
|
1. Jan Vietor, et al. Journal of Medicinal Chemistry, April 26, 2023
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
