Capsazepine

中文名称：辣椒平

目录号：S8137 Purity: 99.66%

Capsazepine是capsaicin的拮抗剂，是TRPV1的拮抗剂。细胞实验请选择01批次。

Capsazepine Chemical Structure

CAS: 138977-28-3

规格	价格	库存
10mM (1mL in DMSO)	1040.13	现货
10mg	795.21	现货
50mg	3251.75	现货
200mg	8165.89	现货
1g	24488.59	现货
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产品质控

批次：纯度： 99.66%

99.66

Capsazepine相关产品

相关靶点	TRPV TRPA TRPC TRPM TRPML	点击展开
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相关化合物库	FDA药物库天然产物库离子通道配体库外泌体分泌相关化合物库钙通道阻滞剂库	点击展开

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
HEK293T	Function assay	100 uM		Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of proton-induced intracellular Ca2+ influx at 100 uM by fluorescence-based assay	24484240
HEK T-REx cells	Function assay	>50 uM		Antagonist at TRPM8 isolated from mouse dorsal root ganglion cells expressed in HEK T-REx cells assessed as inhibition of icilin-induced intracellular Ca2+ influx at >50 uM by fluorescence-based assay	24484240
HEK293T	Function assay	10 uM		Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of proton-induced intracellular Ca2+ influx at 10 uM by fluorescence-based assay	24484240
T-REx HEK cells	Function assay		3 mins	Antagonist activity against human TRPV1 expressed in T-REx HEK cells assessed as inhibition of capsaicin-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to capsaicin stimulation by Fluo-4 AM dye based fluorescence assay, IC50=0.068μM	25052206
T-REx HEK cells	Function assay		3 mins	Antagonist activity against mouse TRPM8 expressed in T-REx HEK cells assessed as inhibition of cold-induced increase in intracellular Ca2+ accumulation pre-incubated for 3 mins prior to cold stimulation by Fluo-4 AM dye based fluorescence assay	25052206
HeLa	Antiproliferative assay		24 hrs	Antiproliferative activity against human HeLa cells after 24 hrs by cell titer 96 aqueous non-radioactive cell proliferation assay, IC50=30μM	30528162
HEK293T	Function assay			Antagonist activity at human brain TRPV1 expressed in HEK293T cells assessed as inhibition of CAP-induced intracellular Ca2+ influx by fluorescence-based assay, IC50=0.15μM	24484240
HEK293	Function assay			Antagonist activity at human TRPV1 expressed in tetracycline-stimulated HEK293 cells assessed as inhibition of capsaicin-induced intracellular calcium levels by fluorimetric assay, EC50=2.51189μM	20381363
CHO	Function assay			Displacement of [3H]RTX from rat TRPV1 receptor expressed in CHO cells, Ki=1.3μM	18072720
CHO	Function assay			Antagonist activity at rat TRPV1 receptor expressed in CHO cells assessed as calcium 45 uptake, Ki=0.52μM	18072720
CHO	Function assay			Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay, IC50=0.887μM	17489570
CHO	Function assay			Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by aequorin based assay, IC50=0.32μM	17489570
CHO	Function assay			Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assay, IC50=0.22μM	17489570
CHO	Function assay			Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay, IC50=0.069μM	17489570
CHO	Function assay			Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay, IC50=0.053μM	17489570
CHO	Function assay			Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by aequorin based assay, IC50=0.039μM	17489570
CHO	Function assay			Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of calcium uptake, Ki=0.52μM	17035013
CHO	Function assay			Displacement of [3H]RTX from rat TRPV1 expressed in CHO cells, Ki=1.3μM	17035013
human TRPV1 expressing cells	Function assay			Inhibition of calcium influx evoked by capsaicin in human TRPV1 expressing cells by fluorescence assay, IC50=0.334μM	16420034
CHO	Function assay			In vitro binding affinity for rat TRPV1 expressed in CHO cells using [3H]-RTX, Ki=1.3μM	16005215
CHO	Function assay			Antagonist activity for rat TRPV1 expressed in CHO cells, Ki=0.52μM	16005215
CHO	Function assay			In vitro inhibition of [3H]RTX binding to rat TRPV1 expressed in CHO cells, Ki=1.3μM	15993063
HEK293	Function assay			Inhibition of 100 nM capsaicin effect on intracellular [Ca2+] concentration in HEK293 cells expressing human TRPV1, IC50=0.0562μM	16000002
CHO	Function assay			Antagonist activity towards rat TRPV1 expressed in CHO cells, Ki=0.52μM	15993063
CHO	Function assay			Inhibition of capsaicin-induced [Ca2+] uptake by Rat Vanilloid receptor 1 (VR1) expressing CHO cells, Ki=0.52μM	12825950
CHO	Function assay			Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells, IC50=0.42μM	15634002
点击查看更多细胞系数据

生物活性

产品描述

Capsazepine是capsaicin的拮抗剂，是TRPV1的拮抗剂。细胞实验请选择01批次。

靶点

TRPV1 ^[2]	Na,K-ATPase ^[3]
	12 μM(EC50)

体外研究(In Vitro)
体外研究活性	94.2 µg/ml的Capsazepine(CPZ)对破骨细胞的生长和增殖具有显著的抑制^[2]。 Capsazepine将NKA转变为Na-ATPase。CPZ抑制K+依赖性活性，但不影响Na+转运相关的Na-ATPase。在没有K+的情况下，CPZ对Na-ATPase没有作用。CPZ还能抑制对硝基磷酸酶活性，尽管亲和力比较弱。CPZ显著地减少稳态EP水平。总之，CPZ阻滞NKA中Na+/K+循环，但保持Na+循环完整、减少泵的运输化学计量^[3]。Capsazepine在骨髓-成骨细胞混合培养物及生成RNKL的破骨细胞中，剂量依赖性地抑制破骨细胞形成和骨吸收。Capsazepine还抑制RANKL诱导的IκB和ERK1/2的磷酸化，导致成熟破骨细胞的凋亡。在颅骨成骨细胞中还抑制碱性磷酸酶活性和骨结节形成^[4]。
细胞实验	细胞系	小鼠巨噬细胞细胞株RAW 264.7
	浓度	94.2 µg/ml
	孵育时间	72 h
	方法	将细胞铺于细胞培养板中，并用不同浓度的化合物进行处理，使得增殖72小时。72小时后，用10% formalin saline (50μl/well)固定细胞30分钟。然后用crystal violet(0.05% w/v)对细胞进行染色，染色时间为30分钟。染色结束后，用蒸馏水冲洗几遍，将未结合上的染料洗去，用Sorenson’s buffer进行脱色。540 nm处测定其吸光值。

体内研究(In Vivo)
体内研究活性	Capsazepine预处理可防止内毒素血症期间呼吸系统阻力的增加并减少组织阻尼的增加。 Capsazepine 还可通过减少脂多糖 (LPS) 引起的肺实质塌陷面积来减轻肺损伤。

参考文献
[1] Cabral LDM, et al. Basic Clin Pharmacol Toxicol. 2016 Nov;119(5):421-427. [2] Mohan Gowda C.M, et al. World Journal of Research and Review (WJRR). 2016, 2(6):71-75. [3] Yasser A. Mahmmoud. PNAS. 2007, 105(5):1757-1761. [4] Idris AI, et al. Bone. 2010, 46(4):1089-99. + 展开

参考文献

[4] Idris AI, et al. Bone. 2010, 46(4):1089-99.

+ 展开

化学信息&溶解度

分子量	376.90	分子式	C₁₉H₂₁ClN₂O₂S
CAS号	138977-28-3	SDF	Download Capsazepine SDF
Smiles	C1CC2=CC(=C(C=C2CN(C1)C(=S)NCCC3=CC=C(C=C3)Cl)O)O
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : Insoluble ( ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 75 mg/mL ( (198.99 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 75 mg/mL (198.99 mM)

Water : Insoluble

DMSO : 75 mg/mL ( (198.99 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 38 mg/mL (100.82 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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