| Identification | Back Directory | [Name]
AM-0902 | [CAS]
1883711-97-4 | [Synonyms]
AM0902
AM-0902
CS-2717
AM-0902
(AM 0902
1-[[3-[2-(4-chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-7-methylpurin-6-one
1-[[3-[2-(4-Chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-1,7-dihydro-7-methyl-6H-purin-6-one
1-({3-[2-(4-Chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl}methyl)-7-methyl-1,7-dihydro-6H-purin-6-one
6H-Purin-6-one, 1-[[3-[2-(4-chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-1,7-dihydro-7-methyl- | [Molecular Formula]
C17H15ClN6O2 | [MDL Number]
MFCD31579854 | [MOL File]
1883711-97-4.mol | [Molecular Weight]
370.79 |
| Chemical Properties | Back Directory | [Melting point ]
190 - 197°C | [Boiling point ]
657.3±65.0 °C(Predicted) | [density ]
1.51±0.1 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO (Slightly), Methanol (Very Slightly) | [form ]
Solid | [pka]
2.36±0.50(Predicted) | [color ]
White to Off-White |
| Hazard Information | Back Directory | [Uses]
AM 0902 is a potent, selective antagonist of TRPA1 (transient receptor potential A1), which has been shown to play a large role in biological pathways associated with pain. | [Biological Activity]
AM-0902 (AMG0902) is a potent and selective transient receptor potential A1 (TRPA1) antagonist (rat/human TRPA1 IC50 = 71/131 nM against AITC-induced 45Ca2+ influx in respective CHO transfectants with [AITC] = EC90 = 3 μM/hTRPA1 or 35 μM/rTRPA1; human/r at IC50 = 24/20 nM by FLIPR) with little potency against human TRPV1/4human CYP3A4/2D6r at TRPV1/3r at TRPM8or mouse NaV1.7. AM-0902 effectively reduces AITC-induced flinching in a r at pain model (by 65% and 85%respectivelywith 10 or 30 mg/kg AM-0902 p.o. 1 hr prior to AITC injection) with good pharmacokinetic propertiesoral availability and brain exposure (F = 60%B/P = 0.2; 30 mg/kg p.o. in rats) in vivo. | [in vivo]
AM-0902 is a potent, selective antagonist of TRPA1 in vivo. AM-0902 has moderate terminal elimination half-life (t1/2=0.6 h and 2.8 h for rat (0.5 mg/kg, iv), rat (30 mg/kg, oral)). A dose-dependent reduction of allyl isothiocyanate (AITC)-induced flinching is observed for AM-0902, with a significant reduction in flinching observed postdosing of 10 and 30 mg/kg. The unbound plasma concentrations (Cu) at 1 h for the 1, 3, 10, and 30 mg/kg doses are 0.051±0.024 (n=8), 0.19±0.11 (n=8), 0.58±0.35 (n=8), and 2.2±0.40 (n=8) μM, covering the in vitro rat TRPA1 45Ca2+ IC50 at 0.72, 2.7, 8.2, and 30.3 fold, respectively. A good exposure-response relationship is observed in this target coverage model. An unbound in vivo IC50 of 0.35 μM, which is in good agreement with the in vitro rat TRPA1 45Ca2+ IC50, and unbound in vivo IC90 of 1.7 μM are determined. It is noteworthy that at a dose of 30 mg/kg, AM-0902 engages TRPA1 at concentrations that exceed the in vivo IC90, making it a useful tool for exploration of in vivo models of acute pain[1]. | [storage]
Store at -20°C |
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