SML3077

Teneligliptin hydrobromide hydrate

≥98% (HPLC)

• 別名: 3-[(2S,4S)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine, hydrobromide, hydrate, [(2S,4S)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl)-1-piperazinyl]-2-pyrrolidinyl]-3-thiazolidinylmethanone, hydrobromide (1:x), hydrate (1:x), [(2S,4S)-4-[4-(3-Methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-yl](1,3-thiazolidin-3-yl)methanone, hydrobromide, hydrate
• 実験式（ヒル表記法）: C₂₂H₃₀N₆OS · xHBr · yH₂O
• 分子量: 426.58 (anhydrous free base basis)
• 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
• 光学活性: [α]/D -28 to -36°, c = 0.5 in methanol
• 保管条件: desiccated
• 色: white to very dark gray
• 溶解性: H₂O: 2 mg/mL, clear
• 保管温度: −20°C
• SMILES記法: CC1=NN(C(N2CCN(CC2)[C@@]3(CN[C@@H](C3)C(N4CSCC4)=O)[H])=C1)C5=CC=CC=C5.[xHBr].[yH2O]

詳細

生物化学的／生理学的作用

Orally active, substrate-competitive, highly potent and selective dipeptidyl peptidase IV inhibitor with therapeutic efficacy against type 2 diabetes in vivo.

Teneligliptin is an orally active, substrate-competitive, highly potent and selective dipeptidyl peptidase IV inhibitor (IC50 in nM = 0.889/hrDPP-IV,1.75/human plasma, 1.35/rat plasma; 700- and 1500-fold selectivity over DPP-8 and DPP-9, respectively). Teneligliptin inhibits plasma DDP-IV activtiy (ED50 = 0.41mg/kg p.o. in Wistar rats) with therapeutic efficacy against type 2 diabetes in Zucker fa/fa rats in vivo (0.1-1 mg/kg p.o.).

安全性情報

• ピクトグラム: GHS07
• シグナルワード: Warning
• 危険有害性情報: H302
• 注意書き: P264 - P270 - P301 + P312 - P501
• 危険有害性の分類: Acute Tox. 4 Oral
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable