| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized Powder |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: (R)‑(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro‑1H‑imidazo[4,5‑c]pyridine-5(4H)‑yl)methanone.
- Also known as: (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridine-5(4H)-yl)methanone
- CAS number: 1627900-41-7
- Molecular formula: C20F4H15N4OCl.
- Purity: >99% (HPLC)
- Concentration: 10 nM - 1 µM.
- Form: Lyophilized Powder
- Solubility: Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).
- Reconstitution: Soluble in DMSO. Centrifuge all products before handling (10000 x g 5 min).
- Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
- Target: P2X7 receptors
- Source: Synthetic
- Activity: JNJ-54166060 is a novel, potent and selective antagonist of purinergic P2X7 receptors, with IC50 of 4 nM on human receptors. Orally bioavailable, with an ED50 of 2.3 mg/kg and a brain/plasma ratio of close to 3 in rats1.
- Alternative names: (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridine-5(4H)-yl)methanone
Scientific background
JNJ-54166060 is a potent and selective antagonist of P2X7 receptors, displaying IC50 values of 4 nM for human P2X71. JNJ-54166060 has a high oral bioavailability with low-moderate clearance in preclinical species, and acceptable safety margins in rats1.P2X receptors are a family of ion channels gated by ATP, a ubiquitous energy donor and receptor ligand in living cells. P2X receptors are ubiquitously expressed, including expression in neuronal, muscular, epithelial and immune cells and play a pivotal role in models of various pain conditions. P2X7 is responsible for mediating the release of proinflammatory cytokines known to have roles in inflammatory/immune conditions and pain2,3.
Lead time: 1-2 Business Days
Country of origin: Israel/IL
Applications key
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Bioassay tested: Yes
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- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
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