[CAS NO. 2117405-13-5] SEN177
PRODUCTS SPECIFICATIONS [2117405-13-5]
DESCRIPTION [2117405-13-5]
Overview
| MDL | MFCD30343871 |
|---|---|
| Molecular Weight | 338.38 |
| Molecular Formula | C18H19FN6 |
| SMILES | CN1C(C2CCN(C3=NC=CC=C3C4=CC=C(F)N=C4)CC2)=NN=C1 |
Summary
SEN177 is a potent glutaminyl cyclase (QPCT) inhibitor with an IC 50 of 0.013μM for glutaminyl-peptide cyclotransferase-like (QPCTL). SEN177 has a K i of 20 nM for human glutaminyl cyclase (hQC). SEN177 greatly reduces the early stages of mutant HTT oligomerisation and reduces the percentage of neurons with Q80 aggregates. SEN177 has the potential for Huntington’s disease research [1] .
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 33.33 mg/mL ( 98.50 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9553 mL | 14.7763 mL | 29.5526 mL |
| 5 mM | 0.5911 mL | 2.9553 mL | 5.9105 mL |
| 10 mM | 0.2955 mL | 1.4776 mL | 2.9553 mL |
References
- [1] Meike E W Logtenberg, et al. Glutaminyl cyclase is an enzymatic modifier of the CD47- SIRPα axis and a target for cancer immunotherapy. Nat Med
- [2] Cecilia Pozzi, et al. The structure of the human glutaminyl cyclase-SEN177 complex indicates routes for developing new potent inhibitors as possible agents for the treatment of neurological disorders. J Biol Inorg Chem. 2018 Dec;23(8):1219-1226.
- [3] Maria Jimenez-Sanchez, et al. siRNA screen identifies QPCT as a druggable target for Huntington's disease. Nat Chem Biol. 2015 May;11(5):347-354.