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Myr-Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白-蛋白相互作用的抑制剂。在10 µM的浓度下,该化合物能够约81%地抑制Cav2.2-CRMP2相互作用,并在大鼠初级背根神经节(DRG)神经元中抑制钾诱导的钙流入(IC50约为2.8 µM)。在20 µM的浓度下,Myr-Tat-CBD3能抑制钙电流,但不影响钠电流,在初级DRG神经元中表现出这种特性。经过脊髓内给药,myr-Tat-CBD3(20 µg/5 µl)能够防止大鼠脚掌撤回潜伏期因carrageenan注射而减少。此外,Myr-Tat-CBD3减少大鼠因线索引起的寻求可卡因行为的复发。
Myr-Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白-蛋白相互作用的抑制剂。在10 µM的浓度下,该化合物能够约81%地抑制Cav2.2-CRMP2相互作用,并在大鼠初级背根神经节(DRG)神经元中抑制钾诱导的钙流入(IC50约为2.8 µM)。在20 µM的浓度下,Myr-Tat-CBD3能抑制钙电流,但不影响钠电流,在初级DRG神经元中表现出这种特性。经过脊髓内给药,myr-Tat-CBD3(20 µg/5 µl)能够防止大鼠脚掌撤回潜伏期因carrageenan注射而减少。此外,Myr-Tat-CBD3减少大鼠因线索引起的寻求可卡因行为的复发。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 390 | 期货 | |
5 mg | ¥ 1,740 | 期货 | |
10 mg | ¥ 2,970 | 期货 | |
25 mg | ¥ 6,700 | 期货 |
产品描述 | Myr-Tat-CBD3 is a chemical compound that serves as an inhibitor of the protein-protein interaction between the N-type voltage-gated calcium channel Cav2.2 and collapsin response mediator protein 2 (CRMP2). This compound effectively disrupts the Cav2.2-CRMP2 interaction by about 81% at a 10 µM concentration and demonstrates an inhibitory concentration 50 (IC50) value of approximately 2.8 µM against potassium-induced calcium influx in primary rat dorsal root ganglion (DRG) neurons. Furthermore, at a concentration of 20 µM, Myr-Tat-CBD3 specifically inhibits calcium currents without affecting sodium currents in primary DRG neurons. Additionally, intrathecal administration of 20 µg/5 µl of Myr-Tat-CBD3 effectively mitigates carrageenan-induced declines in paw withdrawal latencies in rats, indicating its potential for pain relief. The compound also notably reduces cue-induced reinstatement of cocaine-seeking behavior in rats, suggesting therapeutic potential in addiction treatment. |
别名 | N-myristate-Tat-CBD3, Myr-Tat-Calcium Channel-binding Domain 3 |
分子量 | 3403.10 |
分子式 | C148H269N59O33.XCF3COOH |
存储 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度信息 | H2O: Soluble |
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