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Chemical Structure| 1008510-37-9 Chemical Structure| 1008510-37-9

Structure of Razuprotafib
CAS No.: 1008510-37-9

Chemical Structure| 1008510-37-9

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Razuprotafib is a potent VE-PTP (HPTPß) catalytic activity inhibitor (IC50 = 17 pM) that activates the TIE2 pathway, promoting ANG1-induced TIE2 activation and stimulating downstream signaling molecules like AKT, eNOS, and ERK phosphorylation. It also inhibits HPTPη (IC50 = 36 pM) and HPTPγ (IC50 = 100 pM), showing good selectivity and inhibiting the structure-related phosphatase PTP1B (IC50 = 780 nM).

Synonyms: AKB-9778

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Product Details of Razuprotafib

CAS No. :1008510-37-9
Formula : C26H26N4O6S3
M.W : 586.70
SMILES Code : O=S(NC(C=C1)=CC=C1C[C@@H](C2=CSC(C3=CC=CS3)=N2)NC([C@@H](NC(OC)=O)CC4=CC=CC=C4)=O)(O)=O
Synonyms :
AKB-9778
MDL No. :MFCD32861535

Safety of Razuprotafib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of Razuprotafib

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
EA.hy926-KO cells 10 µM 72 hours Reduced monocyte adhesion Front Immunol. 2021 Nov 30;12:789142
PANC-1, MDA-MB-231, HeLa 10 µM 24 to 48 hours To evaluate the effect of Razuprotafib on VEGF secretion by cancer cells under hypoxic conditions, results showed that OD_PSL@AKB significantly reduced VEGF secretion. Biomater Res. 2025 Feb 11;29:0144
HUVECs 10 µM 24 to 48 hours To evaluate the effect of Razuprotafib on the stability of vascular endothelial cells, results showed that PSL@AKB restored VE-cadherin expression and reduced vascular permeability. Biomater Res. 2025 Feb 11;29:0144
EA.hy926-KO cells 10 µM 48 hours Increased L-fucose content, improved glycocalyx structure Front Immunol. 2021 Nov 30;12:789142

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Extracorporeal circulation model Intravenous injection 20 mg/kg Single dose, duration of 75 minutes To evaluate the effect of Razuprotafib on ECC-induced microcirculatory perfusion disturbances and renal edema. Results showed that Razuprotafib did not improve microcirculatory perfusion disturbances or renal edema but reduced pulmonary interstitial inflammation and improved respiratory function. Int J Mol Sci. 2025 Mar 25;26(7):3000

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02387788 Retinal Vein Occlusion PHASE2 COMPLETED 2025-04-17 Wilmer Eye Institute, Baltimor... More >>e, Maryland, 21287, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.70mL

0.34mL

0.17mL

8.52mL

1.70mL

0.85mL

17.04mL

3.41mL

1.70mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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