Molecular Formula | C19H21ClN2O2S |
Molar Mass | 376.9 |
Density | 1.350±0.06 g/cm3(Predicted) |
Melting Point | 155-157°C |
Boling Point | 581.1±60.0 °C(Predicted) |
Solubility | methanol: soluble |
Appearance | solid |
Color | off-white |
pKa | 9.73±0.20(Predicted) |
Storage Condition | 2-8°C |
MDL | MFCD00153778 |
Use | Capsazepine |
In vitro study | Capsazepine(CPZ) at 94.2 µg/ml had a significant inhibition of osteoclast growth and proliferation. Capsazepine turns NKA into Na-ATPase. CPZ inhibits K-dependent activity but does not affect Na-ATPase associated with Na transport. In the absence of K, CPZ has no effect on Na-ATPase. CPZ also inhibits P-Nitro phosphatase activity, although with a weaker affinity. CPZ significantly reduced steady state EP levels. In summary, CPZ blocks the Na /K cycle in NKA, but keeps the Na cycle intact and reduces pump transport stoichiometry. Capsazepine dose-dependently inhibited osteoclast formation and bone resorption in mixed cultures of bone marrow-osteoblasts and RNKL-producing osteoclasts. Capsazepine also inhibits RANKL-induced phosphorylation of IκB and ERK1/2, leading to apoptosis in mature osteoclasts. Alkaline phosphatase activity and bone nodule formation are also inhibited in cranial osteoblasts. |
In vivo study | In mice, the TRPV1 antagonist capsazepine prevents morphine tolerance and dependence. Acute treatment with capsazepine (5 mg/kg, I. p.) potentiated the analgesic effect of morphine. Repeated combination therapy with capsazepine (2.5 mg/kg, I. p.) and morphine reduced the development of tolerance to morphine analgesia. The development of morphine dependence was also reduced by capsazepine (1.25 or 2.5 mg/kg, I. p.). Capsazepine (1 mg/kg/day) inhibited ovariectomy-induced osteoporosis, bone resorption index and bone formation in mice. |
Hazard Symbols | Xn - Harmful |
Risk Codes | R20/21/22 - Harmful by inhalation, in contact with skin and if swallowed. R36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. S36 - Wear suitable protective clothing. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. |
UN IDs | 2811 |
WGK Germany | 3 |
Hazard Class | 6.1(a) |
Packing Group | II |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.653 ml | 13.266 ml | 26.532 ml |
5 mM | 0.531 ml | 2.653 ml | 5.306 ml |
10 mM | 0.265 ml | 1.327 ml | 2.653 ml |
5 mM | 0.053 ml | 0.265 ml | 0.531 ml |
biological activity | Capsazepine is an antagonist of capsainin and an antagonist of TRPV1. |
Target | Value |
TRPV1 () | |
Na,K-ATPase () | 12 μM(EC50) |