SML2985

AM-0902

≥98% (HPLC)

• Synonym(e): 1-((3-(4-Chlorophenethyl)-1,2,4-oxadiazol-5-yl)methyl)-7-methyl-1H-purin-6(7H)-one, 1-[[3-[2-(4-Chlorophenyl)ethyl]-1,2,4-oxadiazol-5-yl]methyl]-1,7-dihydro-7-methyl-6H-Purin-6-one, AM 0902, AMG0902
• Empirische Formel (Hill-System): C₁₇H₁₅ClN₆O₂
• CAS-Nummer: 1883711-97-4
• Molekulargewicht: 370.79
• UNSPSC-Code: 51111800
• NACRES: NA.77

Eigenschaften

• Qualitätsniveau: 100
• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: 2-8°C
• SMILES String: Clc1ccc(cc1)CCc2n[o]c(n2)C[n]3[c](c4[n](cnc4nc3)C)=O
• InChI: 1S/C17H15ClN6O2/c1-23-9-19-16-15(23)17(25)24(10-20-16)8-14-21-13(22-26-14)7-4-11-2-5-12(18)6-3-11/h2-3,5-6,9-10H,4,7-8H2,1H3
• InChIKey: AWJBWNUUODWOKQ-UHFFFAOYSA-N

Beschreibung

Biochem./physiol. Wirkung

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/rat IC50 = 24/20 nM by FLIPR) with little potency against human TRPV1/4, human CYP3A4/2D6, rat TRPV1/3, rat TRPM8, or mouse NaV1.7. AM-0902 effectively reduces AITC-induced flinching in a rat pain model (by 65% and 85%, respectively, with 10 or 30 mg/kg AM-0902 p.o. 1 hr prior to AITC injection) with good pharmacokinetic properties, oral availability and brain exposure (F = 60%, B/P = 0.2; 30 mg/kg p.o. in rats) in vivo.

Brain-penetrant, orally active, potent and selective transient receptor potential A1 (TRPA1) antagonist with efficacy against AITC-induced flinching in rats in vivo.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable