SML2905

Rovatirelin

≥98% (HPLC)

• 別名: 1-{N-[(4S,5S)-(5-methyl-2-oxooxazolidine-4-yl)carbonyl]-3-(thiazol-4-yl)-l-alanyl}-(2R)-2-methylpyrrolidine
• 実験式（ヒル表記法）: C₁₆H₂₂N₄O₄S
• CAS番号: 204386-76-5
• 分子量: 366.44
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• 品質水準: 100
• アッセイ: ≥98% (HPLC)
• フォーム: powder
• 色: white to beige
• 溶解性: DMSO: 2 mg/mL, clear
• 保管温度: 2-8°C
• SMILES記法: [s]1cnc(c1)C[C@H](NC(=O)[C@H]3NC(=O)O[C@H]3C)C(=O)N2[C@@H](CCC2)C
• InChI: 1S/C16H22N4O4S/c1-9-4-3-5-20(9)15(22)12(6-11-7-25-8-17-11)18-14(21)13-10(2)24-16(23)19-13/h7-10,12-13H,3-6H2,1-2H3,(H,18,21)(H,19,23)/t9-,10+,12+,13+/m1/s1
• InChI Key: WTXWDXWZGJGIHV-URBCHYCLSA-N

詳細

生物化学的／生理学的作用

Orally active and brain-penetrant thyrotropin-releasing hormone (TRH) mimetic with higher potency than taltirelin in vitro and in vivo.

Rovatirelin is an orally active and brain-penetrant thyrotropin-releasing hormone (TRH) mimetic with higher receptor affinity than taltirelin (K_i = 702 nM vs 3877 nM, repectively). Rovatirelin oral administration in rats (10 or 30 mg/kg p.o.) upregulates locus coeruleus (LC) c-Fos expression and medial prefrontal cortex (mPFC) extracellular noradrenaline (NA), being more potent than taltirelin in enhancing spontaneous firing activity of isolated rat LC noradrenergic neurons in vitro (10-1000 nM) and rat locomotor activity in vivo (10 or 30 mg/kg p.o.).

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable