There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
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
GW280264X is an inhibitor of ADAM10/17 with IC50s of 11.5 nM and 8.0 nM, respectively[1].At a concentration of 3 µM, acting for 48 hours, GW280264X inhibited GS-7 cell proliferation[2].
GW280264X 细胞实验
Cell Line
Concentration
Treated Time
Description
References
BV2 cells
10 μM
12 hours
Evaluate the synergistic effect of GW280264X and desmosterol on the erythrophagocytosis ability of BV2 cells, showing that GW280264X and desmosterol at 10 μM significantly enhanced the phagocytic ability of BV2 cells.
Theranostics. 2024 Jan 1;14(1):283-303
GS-9 cells
3 μM
48 hours
To evaluate the effect of ADAM10 and ADAM17 inhibitors on ULBP2 cell surface expression, results showed significant upregulation of ULBP2
Neuro Oncol. 2014 Mar;16(3):382-91
GS-7 cells
3 μM
48 hours
To evaluate the effect of ADAM10 and ADAM17 inhibitors on ULBP2 cell surface expression, results showed significant upregulation of ULBP2
Neuro Oncol. 2014 Mar;16(3):382-91
OVCAR-8
3 μM
48 hours
ADAM17 inhibition significantly reduced cell viability and enhanced cisplatin-induced apoptosis
Cancers (Basel). 2021 Apr 23;13(9):2039
SKOV-3
3 μM
48 hours
ADAM17 inhibition significantly reduced cell viability and enhanced cisplatin-induced apoptosis
Cancers (Basel). 2021 Apr 23;13(9):2039
HEY
3 μM
48 hours
ADAM17 inhibition significantly reduced cell viability and enhanced cisplatin-induced apoptosis
Cancers (Basel). 2021 Apr 23;13(9):2039
Igrov-1
3 μM
48 hours
ADAM17 inhibition significantly reduced cell viability and enhanced cisplatin-induced apoptosis
Cancers (Basel). 2021 Apr 23;13(9):2039
A2780
3 μM
48 hours
ADAM17 inhibition significantly reduced cell viability and enhanced cisplatin-induced apoptosis
Cancers (Basel). 2021 Apr 23;13(9):2039
human microvascular endothelial cells (HMVEC-L)
10 μM
24 hours
Inhibition of LPS-induced endothelial permeability increase and IL-8-induced neutrophil transendothelial migration
EMBO Mol Med. 2012 May;4(5):412-23
Adam10/17 −/− mEFs
0.5 μM to 10 μM
2 hours
GW280264X effectively inhibited ADAM9 activity at concentrations as low as 0.5 μM and increasing inhibition was observed at concentrations between 1 and 10 μM.
Biochem J. 2017 Apr 13;474(9):1467-1479
human hepatic stellate cells (HSC)
3 μM
GW280264X partially inhibited the release of soluble CX3CL1 from IFN-γ stimulated HSC, suggesting the involvement of other proteases.
J Cell Mol Med. 2009 Aug;13(8A):1526-35
Human umbilical vein endothelial cells (HUVECs)
10 μM
30 minutes
GW280264X inhibits ADAM10 and ADAM17, significantly increasing cell-surface EMCN protein levels to 231% of the vehicle control, indicating a critical role of ADAM10 in maintaining EMCN cell-surface levels.
J Biol Chem. 2020 May 8;295(19):6641-6651
GW280264X 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
LPS-induced acute lung injury model
Intranasal
40 mg/kg
Single dose, observed at 4 and 24 hours
GW280264X significantly reduced LPS-induced vascular permeability increase, edema formation, release of TNF-α and IL-6, and pulmonary leukocyte recruitment
EMBO Mol Med. 2012 May;4(5):412-23
C57BL/6 mice
Acute ischemic stroke model
Intranasal administration
0.25, 0.5, 1.0, or 1.5 μg/μL
Immediately after surgery, continuous observation
GW280264x inhibits the metalloprotease activity of ADAM17, preventing CX3CL1 from being sheared into its soluble form, thereby promoting microglial polarization from M1 to M2 phenotype
Neural Regen Res. 2023 May;18(5):1033-1039
GW280264X 动物研究
Animal study
Administered intraperitoneally at a dose of 100 µg/kg once daily for one week starting 4 hours after surgery, GW280264X significantly improved functional recovery after spinal cord injury in an animal model[3].
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