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Capsazepine

CAS号

138977-28-3

分子式

C19H21ClN2O2S

主要靶点

Apoptosis|TRP/TRPV Channel

仅限科研使用

Cat No : CM06799

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Synonyms

辣椒平|TRPV Channel|TRPChannel|TRPVChannel|Transient receptor potential channels|TRP Channel|TRPA1|inhibit|Inhibitor|Capsazepine|Apoptosis

验证数据展示

  • CAS No.: 138977-28-3

    Capsazepine
    CAS#: 138977-28-3

产品信息

CAS号 138977-28-3
分子式 C19H21ClN2O2S
主要靶点 Apoptosis|TRP/TRPV Channel
主要通路 离子通道|凋亡
分子量 376.9
纯度 99.64%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 辣椒平|TRPV Channel|TRPChannel|TRPVChannel|Transient receptor potential channels|TRP Channel|TRPA1|inhibit|Inhibitor|Capsazepine|Apoptosis

靶点活性

TRPA1:562 nM

体内活性

Capsazepine是一种合成的capsaicin类似物，能够作为TRPV1的拮抗剂。Capsazepine对包括前列腺癌、乳腺癌、结直肠癌、口腔癌和骨肉瘤在内的多种癌症生长和存活展现出多样化的效应，且可用于治疗其他重大疾病，如结肠炎、胰腺炎、疟疾和癫痫。Capsazepine已被报道在多种肿瘤细胞线上展示出多效性抗癌作用。它能够调节Janus活化激酶(JAK)/信号转导和转录激活因子(STAT)通路、细胞内Ca2+浓度，以及反应性氧种类(ROS)-JNK-CCAAT/增强子结合蛋白同源蛋白(CHOP)通路。Capsazepine能够抑制细胞增殖、转移，并诱导凋亡。此外，Capsazepine通过下调脂多糖(LPS)诱导的核转录因子-κB(NF-κB)以及阻断瞬时受体电位阳离子通道家族V成员1(TRPV1)和瞬时受体电位阳离子通道家族A成员1 (TRPA1)的激活，发挥抗炎效应[1]。

溶解度

DMSO:55 mg/mL (145.93 mM)

参考文献

1.Yang MH, Jung SH, Sethi G,et al.Pleiotropic Pharmacological Actions of Capsazepine, a Synthetic Analogue of Capsaicin, against Various Cancers and Inflammatory Diseases[J].Molecules. 2019 Mar 12;24(5). pii: E995.
2.Sung B , Prasad S , Ravindran J , et al. Capsazepine, a TRPV1 antagonist, sensitizes colorectal cancer cells to apoptosis by TRAIL through ROS–JNK–CHOP-mediated upregulation of death receptors[J]. Free radical biology & medicine, 2012, 53(10).

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