DX600 TFA 

DX600 TFA is a selective ACE2 specific inhibitor (K_D: 1.3 nM), and does not cross-react with ACE. DX600 TFA exacerbates diabetes-induced cardiovascular dysfunction and the increase in cardiac and renal NOX activity^[1][2][3].

DX600 (1 μM)TFA 可抑制 47% 的 rhACE2 活性，pIC₅₀ 为 8.0^[4]。
DX600 (10 μM) TFA 可抑制 42% 的人类 MNC (单核细胞) 中 ACE2 活性^[4]。
DX600 (100 nM，4 小时) TFA 会降低 NR 8383 细胞的生长，并增加上清液中 TNF-a 和 IL-6 的含量 (在存在 LPS 和 osthole 的情况下)^[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

DX600 (5 μg/kg/天，腹膜内注射，每天持续 4 周) TFA 会加剧 Streptozotocin (HY-13753) 处理的糖尿病大鼠中由糖尿病引起的心血管功能障碍^[2]。
DX600 (0.1 µmol/L/kg，静脉注射) TFA 在大鼠血栓形成模型中，使血栓重量增加 30%^[5]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

3074.33 (free acid)

C₁₄₁H₁₈₅N₃₅O₄₀S₂.xC₂HF₃O₂

固体

White to off-white

Ac-Gly-Asp-Tyr-Ser-His-Cys-Ser-Pro-Leu-Arg-Tyr-Tyr-Pro-Trp-Trp-Lys-Cys-Thr-Tyr-Pro-NH2 ( Disulfide bridge: Cys6-Cys17)

Ac-GDYSHCSPLRYYPWWKCTYPDPEGGG-NH2 ( Disulfide bridge: Cys6-Cys17)

Room temperature in continental US; may vary elsewhere.

Sealed storage, away from moisture and light, under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light, under nitrogen)

• [1]. Liao K, et al. Development of an enzymatic assay for the detection of neutralizing antibodies against therapeutic angiotensin-converting enzyme 2 (ACE2).J Immunol Methods. 2013 Mar 29;389(1-2):52-60.  [Content Brief]

  [2]. Yousif MH, et al. Characterization of Angiotensin-(1-7) effects on the cardiovascular system in an experimental model of type-1 diabetes. Pharmacol Res. 2012 Sep;66(3):269-75.  [Content Brief]

  [3]. Svilenov HL, et al. Extrinsic stabilization of antiviral ACE2-Fc fusion proteins targeting SARS-CoV-2. Commun Biol. 2023 Apr 8;6(1):386.  [Content Brief]

  [4]. Joshi S, et al. Angiotensin converting enzyme versus angiotensin converting enzyme-2 selectivity of MLN-4760 and DX600 in human and murine bone marrow-derived cells. Eur J Pharmacol. 2016 Mar 5;774:25-33.  [Content Brief]

  [5]. Fraga-Silva RA, et al. ACE2 activation promotes antithrombotic activity. Mol Med. 2010 May-Jun;16(5-6):210-5.  [Content Brief]