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Razuprotafib

Cat. No. M11432
Razuprotafib Structure
Synonym:

AKB-9778

Size Price Availability Quantity
5mg USD 580  USD580 In stock
10mg USD 980  USD980 In stock
25mg USD 1800  USD1800 In stock
50mg USD 3000  USD3000 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

Razuprotafib (AKB-9778) is an effective selective inhibitor of ve-PTP (HPTPß) catalytic activity (IC50=17 pM), which promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signal molecules in TIE2 pathway. Including AKT, eNOS, and ERK. Razuprotafib inhibited structure-related phosphatase PTP1B with an IC50 of 780 nM. Besides HPTPη (IC50=36 pM) and HPTPγ (100 pM), Razuprotafib showed good selectivity to VE-PTP.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 586.70
Formula C26H26N4O6S3
CAS Number 1008510-37-9
Purity >99%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
References

[1] Mitchell Brigell, et al. Transl Vis Sci Technol. Tie2 Activation via VE-PTP Inhibition With Razuprotafib as an Adjunct to Latanoprost in Patients With Open Angle Glaucoma or Ocular Hypertension

[2] Solvey Pollmann, et al. Front Immunol. Endothelial Dysfunction in Fabry Disease Is Related to Glycocalyx Degradation

[3] Patrick Camilleri, et al. Xenobiotica. Oxidative metabolism of razuprotafib (AKB-9778), a sulfamic acid phosphatase inhibitor, in human microsomes and recombinant human CYP2C8 enzyme

[4] Brandi Lynn Soldo, et al. Xenobiotica. The in vivo disposition of subcutaneous injected 14 C-razuprotafib ( 14 C-AKB-9778), a sulphamic acid phosphatase inhibitor, in nonclinical species and human

[5] Quan Dong Nguyen, et al. Int J Retina Vitreous. The Tie2 signaling pathway in retinal vascular diseases: a novel therapeutic target in the eye

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Keywords: Razuprotafib, AKB-9778 supplier, Phosphatase, inhibitors

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