Benzamide, N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxy- - Names and Identifiers
Benzamide, N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxy- - Physico-chemical Properties
Molecular Formula | C15H8ClF6NO2
|
Molar Mass | 383.67 |
Density | 1.561 |
Boling Point | 323.1±42.0 °C(Predicted) |
Solubility | Solubility: DMSO (5 mg/ml) or Ethanol (1 mg/ml). |
Appearance | White solid |
pKa | 7.61±0.43(Predicted) |
Storage Condition | -20°C |
Sensitive | Light Sensitive |
MDL | MFCD00218820 |
Use | IMD-0354 |
In vitro study | IMD-0354 (< 5 μm) in HMC-1 cells inhibits expression of NF-κB and its movement into the nucleus. IMD-0354 inhibits HMC-1 cell proliferation with time-and dose-dependent properties. IMD-0354 (0.5 μm) almost inhibited IC-2. The IMD-0354 of 10 μg/mL in HepG2 cells could inhibit the activity of NF-κB by 98.5%. IMD-0354 (1 μm) when TNFα (6 nM) and insulin (100 nM) were administered simultaneously in 3T3-L1 adipocytes after 12 h of serum starvation it can promote the decrease of adiponectin concentration induced by TNF α and restore the decreased Akt phosphorylation level after TNF α treatment. Inhibition of IκBα phosphorylation and TNF-α-induced NF-κB nuclear translocation by IMD-0354 (1 μm) in cultured cardiomyocytes, significantly inhibited the production of interleukin-1β and monocyte chemoattractant protein -1 induced by TNF-α. |
In vivo study | In the lungs of OVA-sensitized mice, 5 mg/kg IMD-0354 can significantly reduce NF-κB but the degree of reduction is less than 20 mg/kg IMD-0354, in addition IMD-0354 (20 mg/kg) it can improve airway hyperresponsiveness and reduce the number of bronchial eosinophils and mucous cells, and IMD-0354 (20 mg/kg) can reduce the total number of cells and eosinophils in bronchoalveolar lavage fluid. IMD-0354 (20 mg/kg) inhibits the production of Th2 cytokines such as interleukin (IL) in the airways and lungs in OVA-sensitized mice -5 and IL-13 and eotaxin but did not affect the recovery of Th1 cytokines such as IL-12 and interferon under the same conditions. IMD-0354 (20 mg/kg) caused a local decrease in the serum concentration of IgE. IMD-0354 can significantly lower blood glucose concentrations in KKAy mice fed a high-fat diet and has a dose-dependent profile without affecting body weight. IMD-0354 (10 mg/kg) resulted in a significant and dose-dependent decrease in the ratio of infarct size to total area, while the fractional shortening ratio remained unchanged. |
Benzamide, N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxy- - Risk and Safety
Hazard Symbols | Xi - Irritant
|
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin.
|
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
S36 - Wear suitable protective clothing.
|
WGK Germany | 3 |
HS Code | 29242990 |
Benzamide, N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxy- - Preparation solution concentration reference
| 1mg | 5mg | 10mg |
---|
1 mM | 2.606 ml | 13.032 ml | 26.064 ml |
5 mM | 0.521 ml | 2.606 ml | 5.213 ml |
10 mM | 0.261 ml | 1.303 ml | 2.606 ml |
5 mM | 0.052 ml | 0.261 ml | 0.521 ml |
Last Update:2024-01-02 23:10:35
Benzamide, N-[3,5-bis(trifluoromethyl)phenyl]-5-chloro-2-hydroxy- - Reference Information
biological activity | IMD-0354 (IKK2 Inhibitor V) is an IKKβ Inhibitor that acts on the NF-Delta β pathway, inhibition of IκBα phosphorylation. |
Target | Value |
Last Update:2024-04-09 19:05:17