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Razuprotafib (AKB-9778) sodium is a potent and selective inhibitor of VE-PTP (HPTPη) catalytic activity, with an IC50 of 17 pM. It promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib sodium also inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Additionally, apart from HPTPη (IC50 of 36 pM) and HPTPγ (100 pM), it has good selectivity for VE-PTP.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | Razuprotafib (AKB-9778) sodium is a potent and selective inhibitor of VE-PTP (HPTPη) catalytic activity, with an IC50 of 17 pM. It promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib sodium also inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Additionally, apart from HPTPη (IC50 of 36 pM) and HPTPγ (100 pM), it has good selectivity for VE-PTP. |
| In vitro | Razuprotafib (AKB-9778) sodium promotes the phosphorylation of TIE2 and activates downstream signaling pathways in HUVEC, enhancing angiopoietin-induced TIE2 phosphorylation. |
| In vivo | Razuprotafib sodium (20 mg/kg; subcutaneous injection) enhances TIE2 phosphorylation in retinal endothelial cells. At doses of 10-20 mg/kg, administered subcutaneously twice daily for 7 days, Razuprotafib sodium inhibits subretinal neovascularization (NV). |
| Synonyms | AKB-9778 sodium |
| Molecular Weight | 610.69 |
| Formula | C26H27N4NaO6S3 |
| Cas No. | 1809275-69-1 |
| Smiles | [C@@H](CC1=CC=C(NS(=O)(=O)O)C=C1)(NC([C@H](CC2=CC=CC=C2)NC(OC)=O)=O)C=3N=C(SC3)C4=CC=CS4.[Na] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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