1. Metabolic Enzyme/Protease
  2. Phosphatase
  3. Razuprotafib

Razuprotafib (Synonyms: AKB-9778)

Cat. No.: HY-109041 Purity: 99.18%
Handling Instructions

Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM).

For research use only. We do not sell to patients.

Razuprotafib Chemical Structure

Razuprotafib Chemical Structure

CAS No. : 1008510-37-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 839 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2450 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3850 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM)[1].

In Vitro

Razuprotafib (AKB-9778) promotes TIE2 phosphorylation and activation of downstream signaling in HUVECs and enhances angiopoietin-induced TIE2 phosphorylation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Razuprotafib (20 mg/kg; s.c.) promotes phosphorylation of TIE2 in retinal endothelial cells in vivo[1]. Razuprotafib (10-20 mg/kg; s.c.; twice daily for 7 days) suppresses subretinal neovascularization (NV)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

586.70

Formula

C₂₆H₂₆N₄O₆S₃

CAS No.

1008510-37-9

SMILES

O=C([[email protected]@H](NC(OC)=O)CC1=CC=CC=C1)N[[email protected]](C2=CSC(C3=CC=CS3)=N2)CC4=CC=C(NS(=O)(O)=O)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (170.44 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7044 mL 8.5222 mL 17.0445 mL
5 mM 0.3409 mL 1.7044 mL 3.4089 mL
10 mM 0.1704 mL 0.8522 mL 1.7044 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.26 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.26 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.26 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

RazuprotafibAKB-9778AKB9778AKB 9778PhosphataseacutekidneyinjuryTie-2diabeticnephropathyInhibitorinhibitorinhibit

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Razuprotafib
Cat. No.:
HY-109041
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