Carboxyatractyloside  (Synonyms: CATR)

Carboxyatractyloside (CATR) is a tight-binding inhibitor of adenine nucleotide translocase, and represents the major toxic component of Xanthium sibiricum. Carboxyatractyloside competes with ADP for binding to the translocase, blocks the translocation of ADP/ATP across the inner mitochondrial membrane, and thereby inhibits ADP-stimulated respiration. In the presence of Cyclosporin A (HY-B0579), Carboxyatractyloside still induces permeability transition in liver mitochondria of aged rats, exhibiting significant hepatotoxicity and nephrotoxicity. Carboxyatractyloside is widely used in studies related to hepatotoxicity, nephrotoxicity and Alzheimer's disease^[1][2][3].

Carboxyatractyloside (CATR) (0.07-0.4 μM) 可强效抑制 Vigna sinensis 下胚轴线粒体中由 ADP 刺激的呼吸作用 (腺嘌呤核苷酸转运的替代指标)，在 0.4 μM 时抑制作用达到最大，IC₅₀ 为 0.16 μM (ADP) 或 0.21 μM (CATR)，在特定浓度范围内的表观竞争性抑制常数为 0.115 μM^[2]。
Carboxyatractyloside (2 μM) 可从新鲜制备的大鼠肝线粒体中快速诱导 Ca²⁺外流^[3]。
Carboxyatractyloside (0.5 μM) 可诱导老年大鼠肝脏线粒体中的 Ca²⁺ 外流，即使这些线粒体预先经 CSA 或 BSA 处理以维持 Ca²⁺ 滞留^[3]。
Carboxyatractyloside (2 μM) 不会从预先负载 Sr²⁺的老年大鼠肝线粒体中诱导 Sr²⁺外流^[3]。
Carboxyatractyloside (0.5 μM) 可诱导老年大鼠肝线粒体肿胀，即使线粒体预先用 CSA 处理以降低基础肿胀^[3]。
Carboxyatractyloside (0.5 μM) 可诱导老年大鼠肝线粒体跨膜电位快速崩溃，即使这些线粒体预先用 CSA 处理以稳定电位^[3]。
Carboxyatractyloside (2 μM) 可使预先装载 Sr²⁺的老年大鼠肝线粒体发生跨膜电位的缓慢下降^[3]。

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

770.82

C₃₁H₄₆O₁₈S₂

35988-42-2

Room temperature in continental US; may vary elsewhere.

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

• [1]. Pan H, et al. Simultaneous quantification of atractyloside and carboxyatractyloside in rat plasma by LC‐MS/MS: Application to a pharmacokinetic study after oral administration of Xanthii Fructus extract[J]. Journal of separation science, 2020, 43(3): 590-597.

  [2]. Lima M S, et al. The effect of atractyloside and carboxyatractyloside on adenine nucleotide translocation in mitochondria of Vigna sinensis (L.) Savi cv. serido[J]. Archives of Biochemistry and Biophysics, 1979, 193(2): 368-372.

  [3]. García N, et al. Cyclosporin A is unable to inhibit carboxyatractyloside-induced permeability transition in aged mitochondria. Comp Biochem Physiol C Toxicol Pharmacol. 2009;149(3):374-381.  [Content Brief]