Name: Capsazepine
Brand: Selleck Chemicals
SKU: S8137
Availability: InStock
Rating: 5 (9 reviews)

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Quality Control

Batch: Purity: 99.66%

99.66

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor ATPase GluR
Other TRP Channel Inhibitors	2-APB (2-Aminoethyl Diphenylborinate) SKF96365 AMG-517 GSK2193874 GSK1016790A HC-030031 EIPA (L593754) HC-067047 SB705498 ML-SI3

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : Insoluble
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (3.32mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (13.27mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	376.90	Formula	C₁₉H₂₁ClN₂O₂S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	138977-28-3	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1CC2=CC(=C(C=C2CN(C1)C(=S)NCCC3=CC=C(C=C3)Cl)O)O

Mechanism of Action

Targets/IC₅₀/Ki	TRPV1 Na,K-ATPase 12 μM(EC50)
In vitro	Capsazepine(CPZ) at a concentration of 94.2 µg/ml (IC50 concentration of this compound) exhibits a statistically significant inhibition of osteoclast growth and proliferation. This compound converts the NKA into Na-ATPase. It 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+. This chemical also inhibits para-nitrophenyl phosphatase activity, albeit with a lower affinity. It strongly reduces the steady-state EP level and the Na+ affinity for phosphorylation decreased 3-fold after CPZ treatment. In summary, this compound blocks an Na+/K+ cycle in the NKA but leaves an Na+ cycle intact, reducing the transport stoichiometry of the pump. This chemical inhibits osteoclast formation and bone resorption in a dose dependent manner in bone marrow-osteoblast co-cultures and RANKL generated osteoclast cultures. It 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.
In vivo	Capsazepine pre-treatment prevents the increase in respiratory system resistance and decreases the increase in tissue damping during endotoxemia. This compound also attenuates lung injury by a reduction in the collapsed area of the lung parenchyma induced by lipopolysaccharide (LPS).
References	[1] https://pubmed.ncbi.nlm.nih.gov/27090778/ [2] https://www.wjrr.org/download_data/WJRR0206034.pdf376.90 [3] http://www.pnas.org/content/105/5/1757.full [4] https://pubmed.ncbi.nlm.nih.gov/20096813/

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Capsazepine TRP Channel antagonist

Chemical Structure

Molecular Weight: 376.90