[CAS NO. 186097-54-1] Cilobradine hydrochloride
PRODUCTS SPECIFICATIONS [186097-54-1]
DESCRIPTION [186097-54-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 519.07 |
| Molecular Formula | C28H39ClN2O5 |
| SMILES | O=C1N(C[C@@H]2CN(CCC3=CC=C(OC)C(OC)=C3)CCC2)CCC4=CC(OC)=C(OC)C=C4C1.[H]Cl |
Summary
Cilobradine is an HCN Channel blocker; an open channel blocker of neuronal Ih and related cardiac If channels. Target: HCN Channel blocker Cilobradine is a HCN channel blocker that is about 3 times more potent than ZD7288. At a concentration of 10 μM, Cilobradine inhibits WT mHCN2 channel current by 86 ± 2% (n = 5). In contrast, I432A and A425G channel currents were only reduced by 14 ± 1% (n = 4) and 19 ± 2% (n = 8), respectively, by this concentration of Cilobradine. The double mutant (I432A/A425G) channel was even less sensitive to 10 μM Cilobradine (8 ± 2% inhibition; n = 4).
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02264002 | Boehringer Ingelheim |
Healthy
|
February 2003 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 125 mg/mL ( 240.82 mM )
H 2 O : 100 mg/mL ( 192.65 mM ; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9265 mL | 9.6326 mL | 19.2652 mL |
| 5 mM | 0.3853 mL | 1.9265 mL | 3.8530 mL |
| 10 mM | 0.1927 mL | 0.9633 mL | 1.9265 mL |