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Capsazepine

Capsazepine 是一种 TRPV1 受体的拮抗剂， IC50值为 562 nM。 它可阻断由激活 TRPV1 离子通道的辣椒素引起的热痛感，是辣椒素拮抗剂。

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

验证数据展示

  • CAS No.: 138977-28-3

    Capsazepine
    CAS#: 138977-28-3

产品信息

Capsazepine is an antagonist of TRPV1 receptor ( IC50 : 562 nM). Capsazepine blocks the painful sensation of heat caused by capsaicin (the active ingredient of chilli pepper) which activates the TRPV1 ion channel. It is therefore considered to be a capsaicin antagonist.

CAS号 138977-28-3
分子式 C19H21ClN2O2S
主要靶点 Apoptosis|TRP/TRPV Channel
主要通路 凋亡|离子通道
分子量 376.9
纯度 98.00%， 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 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

TRPA1:562 nM

体内活性

Capsazepine is a synthetic analogue of capsaicin that can function as an antagonist of TRPV1.?Capsazepine can exhibit diverse effects on cancer (prostate cancer, breast cancer, colorectal cancer, oral cancer, and osteosarcoma) growth and survival, and can be therapeutically used against other major disorders such as colitis, pancreatitis, malaria, and epilepsy.?Capsazepine has been reported to exhibit pleiotropic anti-cancer effects against numerous tumor cell lines.?Capsazepine can modulate Janus activated kinase (JAK)/signal transducer and activator of the transcription (STAT) pathway, intracellular Ca2+ concentration, and reactive oxygen species (ROS)-JNK-CCAAT/enhancer-binding protein homologous protein (CHOP) pathways.?It can inhibit cell proliferation, metastasis, and induce apoptosis.?Moreover, capsazepine can exert anti-inflammatory effects through the downregulation of lipopolysaccharide (LPS)-induced nuclear transcription factor-kappa B (NF-κB), as well as the blockage of activation of both transient receptor potential cation channel subfamily V member 1 (TRPV1) and transient receptor potential cation channel, subfamily A, and member 1 (TRPA1)[1].

溶解度

DMSO:50 mg/mL (132.66 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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