SML3205

Sitagliptin

≥98% (HPLC)

• 別名: (2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, (3R)-3-Amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a ]pyrazin-7(8H )-yl]-4-(2,4,5-trifluorophenyl)-1-butanone,, MK 0431 free base, MK 431 free base, MK-0431 free base, MK-431 free base, MK0431 free base, MK431 free base
• 実験式（ヒル表記法）: C₁₆H₁₅F₆N₅O
• CAS番号: 486460-32-6
• 分子量: 407.31
• MDL番号: MFCD09838015
• UNSPSCコード: 51111800
• 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 -17 to -23°, c = 0.5 in chloroform-d
• 色: white to beige
• 溶解性: DMSO: 2 mg/mL, clear
• 保管温度: −20°C
• SMILES記法: FC(F)(F)c1[n]2c(nn1)CN(CC2)C(=O)C[C@H](N)Cc3c(cc(c(c3)F)F)F
• InChI: 1S/C16H15F6N5O/c17-10-6-12(19)11(18)4-8(10)3-9(23)5-14(28)26-1-2-27-13(7-26)24-25-15(27)16(20,21)22/h4,6,9H,1-3,5,7,23H2/t9-/m1/s1
• InChI Key: MFFMDFFZMYYVKS-SECBINFHSA-N

詳細

生物化学的／生理学的作用

Orally active, potent and selective dipeptidyl peptidase IV (DPP-IV; DPP4) inhibitor that improves glucose tolerance in vivo.

Sitagliptin is an orally active, potent and selective dipeptidyl peptidase IV (DPP4; DPP-IV) inhibitor (IC50 = 18 nM) with excellent selectivity over other proline-selective peptidases (IC50 = 48 μM/DPP8, >100 μM/DPP9 & QPP). Sitagliptin improves glucose tolerance in lean mice (23% and 55% reduction of blood glucose post 5 g dextrose/kg with 0.1 or 3 mg Sitagliptin/kg p.o. 60 min prior to dextrose challenge) and in DIO mice (68% and 90% reduction of blood glucose post 2 g dextrose/kg with 0.3 or 3 mg Sitagliptin/kg p.o.) as a result of DPP-IV inhibition and upregulated GLP-1 level in blood in vivo.

安全性情報

• ピクトグラム: GHS08,GHS07
• シグナルワード: Warning
• 危険有害性情報: H319,H373
• 注意書き: P260 - P264 - P280 - P305 + P351 + P338 - P314 - P337 + P313
• 危険有害性の分類: Eye Irrit. 2 - STOT RE 2
• ターゲットの組織: Liver
• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable