シビネチド

シビネチド 化学特性,用途語,生産方法

• 効能

  鎮痛薬, 抗炎症薬

• 説明

  Cibinetide, also known as ARA-290, is a synthetic 11-mer peptide that binds the tissue-protective receptor. ARA290 inhibits high glucose-induced apoptosis of NRK-52E cells. Cibinetide Protects Isolated Human Islets in a Stressful Environment and Improves Engraftment in the Perspective of Intra Portal Islet Transplantation. Cibinetide Improves Corneal Nerve Fiber Abundance in Patients With Sarcoidosis-Associated Small Nerve Fiber Loss and Neuropathic Pain. ARA 290 relieves pathophysiological pain by targeting TRPV1 channel: Integration between immune system and nociception.

• 生物活性

  Cibinetide (ARA 290) is an engineered peptide that mimics the 3 dimensional structure of the helix B surface domain of erythropoietin (EPO). It is designed to bind selectively to the non-hematopoietic EPO receptor (sometimes referred to as the innate repair receptor or IRR), that is believed to be a heterodimer of EPOR and the cytokine family beta common receptor (βCR, CD131). Non-hematopoietic EPO ligands have potential tissue protective and anti-inflammatory actions. The IRR is suggested to be a point of integration between the immune system and pain signalling (via nociception) .

• in vitro

  Cibinetide (ARA290) enhances the proliferation, migration, and resistance to H2O2-induced apoptosis of endothelial colony-forming cells (ECFCs)[1]. Cibinetide (ARA290) is an EPO-analog peptide without hematopoietic side-effects but may have neurotrophic and antidepressant effects.

• in vivo

  After ECFC transplantation to mice with CLI, a single Cibinetide (ARA290) injection enhances the ischemic/non-ischemic ratio of hindlimb blood flow and capillary density after 28 days and the homing of radiolabeled transplanted cells to the ischemic leg 4?h after transplantation. Cibinetide (ARA290; 30 μg/kg, s.c.) prevents progressive worsening of glucose control without affecting the body weight of rats. Cibinetide significantly decreases glucose AUCs in IPGTT in GK rats. Low-dosage Cibinetide (35 μg/kg, i.p.) treatment slightly attenuates the EAE severity in rats. Cibinetide-treating group (70 μg/kg, i.p.) significantly delays the onset, decreases the neurologic severity, and shortens the duration of EAE in a dose-dependent way.

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