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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
CGP37157 is identified as a potent and selective inhibitor of the Na+/Ca2+ exchanger, particularly effective in blocking Na+-induced Ca2+-release from guinea-pig heart mitochondria at an IC50 of 0.8 μM. At a concentration of 10 μM, CGP37157 inhibits the mitochondrial Na+/Ca2+ exchanger in cortical neurons, managing intracellular Ca2+ levels by dampening voltage-gated calcium channels and mitigating NMDA-induced rises in cytosolic and mitochondrial Ca2+. Additionally, CGP37157 at this concentration diminishes NMDA-triggered excitotoxicity through the reduction of mitochondrial damage and calpain activity in neurons[2]. CGP37157 (10 μM) combined with salomycin significantly decreased the viability of FaDu and HLaC79 cells, and increased cell apoptosis. In addition, CGP37157 had no inhibitory effect on the tumor toxicity of salomycin [3].
体外研究
CGP37157 is identified as a potent and selective inhibitor of the Na+/Ca2+ exchanger, particularly effective in blocking Na+-induced Ca2+-release from guinea-pig heart mitochondria at an IC50 of 0.8 μM.
At a concentration of 10 μM, CGP37157 inhibits the mitochondrial Na+/Ca2+ exchanger in cortical neurons, managing intracellular Ca2+ levels by dampening voltage-gated calcium channels and mitigating NMDA-induced rises in cytosolic and mitochondrial Ca2+. Additionally, CGP37157 at this concentration diminishes NMDA-triggered excitotoxicity through the reduction of mitochondrial damage and calpain activity in neurons[2].
CGP37157 (10 μM) combined with salomycin significantly decreased the viability of FaDu and HLaC79 cells, and increased cell apoptosis. In addition, CGP37157 had no inhibitory effect on the tumor toxicity of salomycin [3].
CGP37157 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Rat islet cells
0.1 μM
CGP37157 restored mitochondrial calcium signaling, ATP generation, and glucose-stimulated insulin secretion in Pdx1-deficient islets
Cell Metab. 2009 Aug;10(2):110-8.
hippocampal slices
10 μM
4 h
To evaluate the neuroprotective effect of CGP37157 in the glutamate excitotoxicity model. Results showed that CGP37157 increased cell survival in Calhm1+/+ slices but had no significant effect in Calhm1−/− slices.
Cells. 2020 Mar 9;9(3):664.
hippocampal slices
10 μM and 30 μM
OGD for 15 min, reoxygenation for 2 h
To evaluate the neuroprotective effect of CGP37157 in the OGD/Reox model. Results showed that CGP37157 reduced cell death in Calhm1+/+ slices but had no significant effect in Calhm1−/− slices.
Cells. 2020 Mar 9;9(3):664.
rat cortical neurons
10μM
1 h
To analyze how intracellular Ca2+ levels are modulated by CGP37157 during NMDA insults, it was found that CGP37157 strongly prevented depolarization-induced [Ca2+]i increase by blocking voltage-gated Ca2+ channels (VGCCs), while it did not induce depletion of ER Ca2+ stores. Moreover, mitochondrial Ca2+ overload was reduced as a consequence of diminished Ca2+ entry through VGCCs, leading to attenuation of excitotoxic mitochondrial damage.
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