Caplacizumab  (Synonyms: 卡拉西单抗; ALX-0681; ALX-0081)

Caplacizumab (ALX-0681) is a humanized anti-von Willebrand factor (vWF) nanobody. Caplacizumab inhibits the binding of vWF with platelet glycoprotein (GP) Ibα. Caplacizumab inhibits the vWF-mediated platelet adhesion and prevents further microthrombi formation. Caplacizumab can be used for the research of thrombotic thrombocytopenic purpura (TTP)^[1][2][3][4].

VH-VH

Human

VWF

Caplacizumab 可抑制血液样本中 VWF 与血小板糖蛋白 (GP) Ibα 的结合^[2]。
Caplacizumab (0.8 μg/mL) 可在高剪切速率 (>1500 s^-1) 下完全抑制血小板粘附于胶原表面^[4]。

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

Caplacizumab (预防组每日皮下注射 2.5 mg/kg，从第 1 天到第 5 天) 可完全预防狒狒获得性血栓性血小板减少性紫癜模型中严重血小板减少症和裂细胞性溶血性贫血的快速发生，并促进 TTP 诱导后血小板计数的恢复^[3]。
Caplacizumab (血浆浓度在 0.3-0.5 μg/mL 之间，静脉推注) 在狒狒改良的 Folts 模型中表现出强大的抗血栓作用^[4]。
Caplacizumab (总剂量 5 mg/kg，静脉和皮下注射；先静脉注射，然后皮下注射) 可在豚鼠大脑中动脉血栓形成模型中预防大脑中动脉血栓形成，并减轻脑损伤，不引起出血^[5]。

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

7450  [NCBI]

P04275

ELISA, FACS, Functional assay

Unconjugated

The product can be reconstituted/diluted with sterile PBS or saline.

29 kDa

915810-67-2

液体

Colorless to light yellow

卡拉西单抗

Shipping with dry ice.

Please store the product under the recommended conditions in the Certificate of Analysis.

• 
  VH-VH

• 
  Immobilized Human VWF-A1 (1260–1554aa)-Fc can bind Caplacizumab. The EC₅₀ for this effect is 7.442 ng/mL.

• [1]. Maëlle le Besnerais, et al. Caplacizumab: a change in the paradigm of thrombotic thrombocytopenic purpura treatment. Expert Opin Biol Ther. 2019 Nov;19(11):1127-1134.  [Content Brief]

  [2]. Nakayama M, et al. Effects of caplacizumab, a specific inhibitor of the A1 domain of von Willebrand factor binding with platelet membrane glycoprotein (GP) Ibα, on the length of platelet pseudopods supporting platelet adhesions on immobilized von Willebrand factor under blood flow condition. Journal of Biorheology, 2022, 36(2): 68-75.

  [3]. Callewaert F, et al. Evaluation of efficacy and safety of the anti-VWF Nanobody ALX-0681 in a preclinical baboon model of acquired thrombotic thrombocytopenic purpura. Blood. 2012 Oct 25;120(17):3603-10.  [Content Brief]

  [4]. Ulrichts H, et al. Antithrombotic drug candidate ALX-0081 shows superior preclinical efficacy and safety compared with currently marketed antiplatelet drugs. Blood. 2011 Jul 21;118(3):757-65.  [Content Brief]

  [5]. Momi S, et al. Reperfusion of cerebral artery thrombosis by the GPIb-VWF blockade with the Nanobody ALX-0081 reduces brain infarct size in guinea pigs. Blood. 2013 Jun 20;121(25):5088-97.  [Content Brief]