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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.
| 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.
| Molecular Weight | 586.70 |
| Formula | C26H26N4O6S3 |
| CAS Number | 1008510-37-9 |
| Purity | >99% |
| Solubility | DMSO ≥ 60 mg/mL |
| Storage | at -20°C |
| Related Phosphatase Products |
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| ABBV-CLS-484
Abbv-cls-484 is a potent inhibitor of PTPN1 or PTPN2 with subnanomolar activity. |
| PTP1B-IN-1
Ptp1b-in-1 is a small molecule inhibitor of PTP1B with an IC50 value of 1.6mm, and is often used as a parent nucleus derived from analogues. |
| RMC-4630
Rmc-4630 (SHP2-IN-7) is a SHP2 inhibitor derived from patent WO2018013597. |
| Rbin-1
Rbin-1 (ribozinoindole-1) is a potent and reversible inhibitor of Midasin (Mdn1), an enzyme belonging to the AAA+ (ATPases associated with diverse cellular activities) protein family (GI50 value 136 nM in wild-type cells). |
| Voclosporin (ISATX247)
Voclosporin (ISATX247) is a novel calcineurin (PP2B) (CN) inhibitor. |
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