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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Calcium Channel -CBD3063
CBD3063

Chemical Structure : CBD3063

CAS No.: 1281060-70-5 (Racemic)

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CBD3063 (CBD 3063, CBD-3063)

货号: PC-21384Not For Human Use, Lab Use Only.

CBD3063 is a selective, first-in-class inhibitor of Cav2.2-CRMP2 (ollapsin response mediator protein 2) interaction, suppresses surface trafficking of Cav2.2, and N-type (Cav2.2) calcium currents.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    CBD3063 is a selective, first-in-class inhibitor of Cav2.2-CRMP2 (ollapsin response mediator protein 2) interaction, suppresses surface trafficking of Cav2.2, and N-type (Cav2.2) calcium currents.
    CBD3063 (20 µM) reduces Cav2.2 protein association with CRMP2 by ~35% in mouse neuronal line expressing both CRMP2 and Cav2.2, also decreases the closeness of Cav2.2–CRMP2 in neurons by the proximity ligation assay (PLA).
    CBD3063 does not affect the voltage dependence of activation or inactivation of Cav1 (L-type), Cav2.1 (P/Q-type), Cav2.3 (R-typeI channels.
    CBD3063 decreases spinal cord excitability and excitatory neurotransmitter release.
    CBD3063 administration (i.p.) dose-dependently mitigates SNI-induced mechanical allodynia with ED50 of 1.50 mg/kg.
    CBD3063 (10 mg/kg) effectively paralleled the antinociceptive strength of GBP (30 mg/kg) in alleviating the behavioral signs of neuropathic pain.
    CBD3063 (9 mg/kg, i.p.) reverses PAC-induced mechanical and cold hypersensitivity, effectively alleviates pain-like behavior through multiple routes of administration.

    物理化学性质&存储条件

    分子量 319.41
    分子式 C16H25N5O2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    (R)-3-acetamido-N-(3-(pyridin-2-ylamino)propyl)piperidine-1-carboxamide

    参考文献

    1. Kimberly Gomez, et al. Proc Natl Acad Sci U S A. 2023 Nov 21;120(47):e2305215120.

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