[CAS NO. 1008510-37-9] Razuprotafib
PRODUCTS SPECIFICATIONS [1008510-37-9]
DESCRIPTION [1008510-37-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 586.70 |
| Molecular Formula | C26H26N4O6S3 |
| SMILES | O=C([C@@H](NC(OC)=O)CC1=CC=CC=C1)N[C@H](C2=CSC(C3=CC=CS3)=N2)CC4=CC=C(NS(=O)(O)=O)C=C4 |
1 Publications Citing Use of MCE
Summary
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC 50 of 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 IC 50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC 50 =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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03197870 | Aerpio Therapeutics |
Nonproliferative Diabetic Retinopathy
|
June 9, 2017 | Phase 2 |
| NCT02858271 | Aerpio Therapeutics |
Healthy
|
July 2016 | Phase 1 |
| NCT02050828 | Aerpio Therapeutics |
Diabetic Macular Edema (DME)
|
January 2014 | Phase 2 |
| NCT01702441 | Aerpio Therapeutics |
Diabetic Macular Edema (DME)
|
September 2012 | Phase 1|Phase 2 |
| NCT04511650 | Aerpio Therapeutics|Medical Technology Enterprise Consortium (MTEC) |
COVID-19|Acute Respiratory Distress Syndrome
|
October 21, 2020 | Phase 2 |
| NCT04284514 | Aerpio Therapeutics |
Ocular Hypertension|Primary Open Angle Glaucoma
|
May 2, 2019 | Phase 1 |
| NCT02387788 | Aerpio Therapeutics |
Retinal Vein Occlusion
|
January 2015 | Phase 2 |
| NCT04405245 | Aerpio Therapeutics |
Ocular Hypertension|Primary Open Angle Glaucoma
|
June 6, 2020 | Phase 2 |
Appearance
Solid
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
DMSO : 100 mg/mL ( 170.44 mM ; Need ultrasonic)
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 |