Capsazepine

For research use only.

Catalog No.S8137

2 publications

Capsazepine Chemical Structure

Molecular Weight(MW): 376.90

Capsazepine acts as a competitive antagonist of capsaicin and a transient receptor potential vanilloid type 1(TRPV1) antagonist.

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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.
Targets
TRPV1 [2]
()
Na,K-ATPase [3]
()
12 μM(EC50)
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 Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO cells NED3O5RHfW6ldHnvckBie3OjeR?= NWXzUWZlSW62YXfvcol{fCCjY4Tpeol1gSCjdDDoeY1idiCWUmDWNUBmgHC{ZYPz[YQhcW5iQ1jPJINmdGy|IHHzd4V{e2WmIHHzJIJtd2OtYXTlJI9nKGOjcIPhbYNqdi2rbnT1Z4VlKHKnY3XweI9zKGGldHn2ZZRqd25iYomgZYVyfW:{aX6gZoF{\WRiYYPzZZktKEmFNUC9NE4xOzlizszN MXyxO|Q5QTV5MB?=
HEK293 cells NFfKc3pHfW6ldHnvckBie3OjeR?= M{f0UWlvcGmkaYTpc44hd2ZiMUCwJI5OKGOjcIPhbYNqdiCnZn\lZ5Qhd25iaX70doFk\WyudXzhdkBcS2F{K22gZ49v[2WwdILheIlwdiCrbjDISWszQTNiY3XscJMh\XiycnXzd4lv\yCqdX3hckBVWlCYMTygTWM2OD1yLkC1OlIh|ryP NXWxdIJCOTZyMECwNFI>
T-REx HEK cells NGDOcIxHfW6ldHnvckBie3OjeR?= M3LibWFvfGGpb37pd5Qh[WO2aY\peJkh[WejaX7zeEBud3W|ZTDUVnBOQCCneIDy[ZN{\WRiaX6gWE1TTXhiSFXLJINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiY3;s[E1qdmS3Y3XkJIlv[3KnYYPlJIlvKGmwdILhZ4VtdHWuYYKgR4EzMyCjY3P1cZVt[XSrb36gdJJmNWmwY4XiZZRm\CCob4KgN{BucW6|IIDybY9zKHSxIHPvcIQhe3SrbYXsZZRqd25iYomgSox2dy12IFHNJIR6\SCkYYPl[EBndHWxcnXzZ4Vv[2ViYYPzZZk> NHnT[okzPTB3MkKwOi=>

... Click to View More Cell Line Experimental Data

In vivo In mice, the TRPV1 antagonist capsazepine blocks morphine tolerance and dependence in mice. Acute capsazepine treatment (5 mg/kg, i.p.) potentiates the antinociceptive effects of morphine, as measured by the hot-plate test. Repeated co-treatment of capsazepine (2.5 mg/kg, i.p.) with morphine attenuates the development of tolerance to the antinociceptive effect of morphine. The development of morphine dependence is also reduced by capsazepine (1.25 or 2.5 mg/kg, i.p.)[1]. Capsazepine (1 mg/kg/day) inhibits ovariectomy induced bone loss in mice and histomorphometric analysis shows inhibitory effects on indices of bone resorption and bone formation[4].

Protocol

Cell Research:[2]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Institute of Cancer Research mice(ICR mice)
  • Dosages: 1.25, 2.5, or 5 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 75 mg/mL (198.99 mM)
Ethanol 75 mg/mL (198.99 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 376.90
Formula

C19H21ClN2O2S

CAS No. 138977-28-3
Storage powder
in solvent
Synonyms N/A
Smiles OC1=CC2=C(CN(CCC2)C(=S)NCCC3=CC=C(Cl)C=C3)C=C1O

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID