SML3804

PMX205 trifluoroacetate

≥98% (HPLC)

• 别名: Hydrocinnamate (HC)-[OP(D-Cha)WR] trifluoroacetate, (5→1)-lactam-N2-(1-oxo-3-phenylpropyl)-L-ornithyl-L-prolyl-3-cyclohexyl-D-alanyl-L-tryptophyl-L-arginine trifluoroacetate, HC-[OP(D-Cha)WR] trifluoroacetate, HC-[Orn-Pro-dCha-Trp-Arg] trifluoroacetate, Hydrocinnamate-(L-ornithine-proline-D-cyclohexylalanine-tryptophan-arginine) trifluoroacetate;, Hydrocinnamate-(OPdChaWR) trifluoroacetate, Hydrocinnamate-[OP(D-Cha)WR] trifluoroacetate, PMX 205 trifluoroacetate, PMX-205 trifluoroacetate, c[Arg-Trp-D-Cha-Pro-Orn]-Hca trifluoroacetat
• 经验公式（希尔记法）: C₄₅H₆₂N₁₀O₆ · xC₂HF₃O₂
• 分子量: 839.04 (free base basis)
• MDL號碼: MFCD31735786
• 分類程式碼代碼: 51111800
• 分類程式碼代碼: 12352200
• NACRES: NA.21

属性

• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: (Powder or Lyophilized powder or film)
• 儲存條件: desiccated
• 顏色: white to off-white
• 儲存溫度: -10 to -25°C

说明

生化／生理作用

PMX205 is a blood-brain barrier (BBB)-permeable and orally active cyclic hexapeptide that acts as a high-affinity and potent antagonist against complement C5a receptor C5aR1. Unlike its structural analog PMX53, PMX205 is resistant to intestinal metabolism and shows 10-30-times higher in vivo efficacy when administered orally (mortality rate = 1/9 with 0.1 mg/kg/day PMX205 vs. 2/10 with 1 mg/kg/day PMX53 in a rat colitis model) despite similar in vitro potency (PMX205/PMX53 pIC50 = 6.50/6.38 against 50 pM C5a by competitive binding, 9.03/8.24 against C5a-induced human PMN MPO release). PMX205 shows in vivo efficacy in animal models of AD (3-6 mg/kg/day p.o., mice), ALS (1 mg/kg/day p.o., rats), and HD (10 mg/kg/day p.o., rats).

注意

Hygroscopic

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable