SML2225

RO5263397

≥98% (HPLC), TAAR1 agonist, powder

• 別名: (S)-4-(3-Fluoro-2-methyl-phenyl)-4,5-dihydro-oxazol-2-ylamine
• 実験式（ヒル表記法）: C₁₀H₁₁FN₂O
• CAS番号: 1357266-05-7
• 分子量: 194.21
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD28405323
• Assay: ≥98% (HPLC)
• Form: powder

特性

• 製品名: RO5263397, ≥98% (HPLC)
• assay: ≥98% (HPLC)
• form: powder
• optical activity: [α]/D +77 to +88°, c = 1.0 in methanol
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: 2-8°C
• SMILES string: NC1=N[C@@H](C2=CC=CC(F)=C2C)CO1
• InChI: 1S/C10H11FN2O/c1-6-7(3-2-4-8(6)11)9-5-14-10(12)13-9/h2-4,9H,5H2,1H3,(H2,12,13)/t9-/m1/s1
• InChI key: IOHOUWIYOVWGHV-SECBINFHSA-N

詳細

Biochem/physiol Actions

Orally available, potent and selective partial TAAR1 agonist with similar in vivo efficacy as the full agonist RO5256390.

RO5256390 is an orally available partial agonist that targets trace amine-associated receptor 1 (TAAR1) with high affinity (Ki in nM = 0.9/mouse, 4.1/human, 9.1/rat, 24/monkey TARR1), potency (EC50 in nM/relative efficacy with respect to β-phenylethylamine = 1.3/0.59/mouse, 17/0.81/human, 47/0.76/rat, 251/0.85/monkey TARR1-dependent cellular cAMP production), and selectivity (by a 112-receptor/channel/transporter and a 42-enzyme panel), without agonistic activity toward mouse TAAR4-expressing cells even at a high concentration of 30 μM. When applied via oral administration (0.003-1 mg/kg), RO5256390 exhibits similar in vivo efficacy as the full agonist RO5256390 in blocking psychostimulants-induced hyperlocomotion in mice.

安全性情報

• 保管分類: 11 - Combustible Solids
• 一体何が起きているの？: WGK 3
• 引火点 (F): Not applicable
• 引火点（°C）: Not applicable