ホームページ Transmembrane Transporters TRP Channel antagonist Capsazepine For research use only.

Capsazepine

Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist. If you want to do cell experiments, please select batch 01.

Capsazepine化学構造

CAS No. 138977-28-3

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫なし(納期7~10日)
JPY 22000 国内在庫なし(納期7~10日)
JPY 59500 国内在庫あり
JPY 149500 国内在庫なし(納期7~10日)
JPY 448500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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Capsazepine関連製品

TRP Channel阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
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
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生物活性

製品説明 Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist. If you want to do cell experiments, please select batch 01.
Targets
TRPV1 [2] Na,K-ATPase [3]
12 μM(EC50)
In Vitro
In vitro

Capsazepine(CPZ) at a concentration of 94.2 µg/ml (IC50 concentration of capsazepine) exhibits a statistically significant inhibition of osteoclast growth and proliferation[2]. Capsazepine converts the NKA into Na-ATPase. CPZ inhibits K+-dependent activity but allows Na-ATPase associated with Na+ transport. CPZ has no effect on Na-ATPase measured in the absence of K+. CPZ also inhibits para-nitrophenyl phosphatase activity, albeit with a lower affinity. CPZ strongly reduces the steady-state EP level and the Na+ affinity for phosphorylation decreased 3-fold after CPZ treatment. In summary, CPZ blocks an Na+/K+ cycle in the NKA but leaves an Na+ cycle intact, reducing the transport stoichiometry of the pump[3]. Capsazepine inhibits osteoclast formation and bone resorption in a dose dependent manner in bone marrow-osteoblast co-cultures and RANKL generated osteoclast cultures. Capsazepine also suppresses RANKL induced IκB and ERK1/2 phosphorylation and causes apoptosis of mature osteoclasts and also inhibits alkaline phosphatase activity and bone nodule formation in calvarial osteoblast cultures[4].
細胞実験 細胞株 Murine macrophage cell line RAW 264.7
濃度 94.2 µg/ml
反応時間 72 h
実験の流れ

The cells are plated and treated with different concentrations of the test compounds and allowed to proliferate for 72 h. After 72 h of proliferation the cells are fixed in 10% formalin saline (50 μl/well) for 30 min. Then the cells are stained with crystal violet (0.05% w/v) for 30 min. The wells are then washed thoroughly with distilled water to remove any unbound dye and destained with Sorenson's buffer (0.1 M sodium citrate in 50% ethanol, pH 4.2). The absorbance of the extracted stain is measured at 540 nm.
In Vivo
In Vivo

Capsazepine pre-treatment prevents the increase in respiratory system resistance and decreases the increase in tissue damping during endotoxemia. Capsazepine also attenuates lung injury by a reduction in the collapsed area of the lung parenchyma induced by lipopolysaccharide (LPS).

化学情報

分子量 376.90 化学式

C19H21ClN2O2S
CAS No. 138977-28-3 SDF Download Capsazepine SDFをダウンロードする
Smiles C1CC2=CC(=C(C=C2CN(C1)C(=S)NCCC3=CC=C(C=C3)Cl)O)O
保管

In vitro
Batch:

DMSO : Insoluble ( 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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