| Identification | Back Directory | [Name]
1(4H)-Cycloheptapyrazoleacetic acid, 5,6,7,8-tetrahydro-3-[4-(trifluoromethyl)phenyl]-, ethyl ester | [CAS]
2765255-93-2 | [Synonyms]
1(4H)-Cycloheptapyrazoleacetic acid, 5,6,7,8-tetrahydro-3-[4-(trifluoromethyl)phenyl]-, ethyl ester | [Molecular Formula]
C19H21F3N2O2 | [MOL File]
2765255-93-2.mol | [Molecular Weight]
366.38 |
| Chemical Properties | Back Directory | [Boiling point ]
462.2±45.0 °C(Predicted) | [density ]
1.28±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
1.52±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
JNJ-28583113 is an TRPM2 antagonist with brain permeability. JNJ-28583113 inhibits TRPM2 blocked phosphorylation of GSK3α and β subunits. JNJ-28583113 protects cells from oxidative stress induced cell death. JNJ-28583113 also suppresses cytokine release in response to pro-inflammatory stimuli in microglia[1]. | [in vivo]
JNJ-28583113 (10 mg/kg, 2?ml/kg; sc; single dose) is brain penetrant, and achieves 400?ng/mL in the brain compartment[1]. | Animal Model: | Harlan Sprague Dawley Rats (400 g)[1] | | Dosage: | 10 mg/kg, 2?mL/kg | | Administration: | SC; sampled at 0.5, 2, or 6?h post dosing | | Result: | Quickly metabolized in the plasma, while it showed high levels in plasma and low levels in the brain. |
| [IC 50]
TRPM2 | [References]
[1] Fourgeaud L, et al. Pharmacology of JNJ-28583113: A novel TRPM2 antagonist. Eur J Pharmacol. 2019 Jun 15;853:299-307. DOI:10.1016/j.ejphar.2019.03.043 |
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