Home 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 Chemical Structure

Capsazepine Chemical Structure

CAS No. 138977-28-3

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Capsazepine Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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
CHO Function assay Antagonist activity towards rat TRPV1 expressed in CHO cells, Ki=0.52μM 15993063
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 for rat TRPV1 expressed in CHO cells, Ki=0.52μM 16005215
CHO Function assay In vitro binding affinity for rat TRPV1 expressed in CHO cells using [3H]-RTX, Ki=1.3μM 16005215
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 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
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 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 acid-induced receptor activation by [45Ca2+] uptake assay, IC50=0.069μM 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 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 [45Ca2+] uptake assay, IC50=0.887μM 17489570
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 Displacement of [3H]RTX from rat TRPV1 receptor expressed in CHO cells, Ki=1.3μM 18072720
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
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
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
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 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
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
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Biological Activity

Description 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].
Cell Research Cell lines Murine macrophage cell line RAW 264.7
Concentrations 94.2 µg/ml
Incubation Time 72 h
Method

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).

Chemical Information & Solubility

Molecular Weight 376.90 Formula

C19H21ClN2O2S
CAS No. 138977-28-3 SDF Download Capsazepine SDF
Smiles C1CC2=CC(=C(C=C2CN(C1)C(=S)NCCC3=CC=C(C=C3)Cl)O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : Insoluble ( Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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