| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized powder. |
| Product Type | |
| Purity | |
| Reconstitution | |
| Shipping | |
| Solubility | 35 mM in water, 100 mM in DMSO. Centrifuge all product preparations before use (10 000 x g for 1 min). |
| Source | Synthetic |
| Storage | |
| Target |
Product details
- Chemical name: (1S,2S)-2-[2[[3-(2-Benzimidazolyl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-isopropyl-2-naphthyl methoxyacetate dihydrochloride hydrate.
- Also known as: Ro 40-5967 hydrate
- CAS number: 116666-63-8
- Molecular formula: C29H40Cl2FN3O3.
- Purity: >98%
- Concentration: 0.01-50 µM.
- Form: Lyophilized powder.
- Solubility: 35 mM in water, 100 mM in DMSO. Centrifuge all product preparations before use (10 000 x g for 1 min).
- Reconstitution: Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in sterile water at a concentration of at least 0.1 mg/mL. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. It is recommended to prepare fresh solutions in working buffers just before use. Repeat freeze-thawing may result in loss of activity.
- Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
- Target: CaV3, Orai1-3, KV10.1 channels
- Source: Synthetic
- Activity: Mibefradil blocks T-type Ca2+ channels with an IC50 of ~1 µM. Orai1-3 and most potent on Orai32. It also modulates the gating properties of KV10.1 channel3.
- Alternative names: Ro 40-5967 hydrate
Scientific background
Mibefradil dihydrochloride hydrate, a potent T-type calcium antagonist, belongs to a new class of Ca2+ antagonists, the tetralol derivatives. It selectively blocks T-type Ca2+ channels in contrast to other Ca2+ antagonists which block only L-type channels1. Mibefradil also modulates the gating properties of KV10.1 channel6. It also blocks Orai1-3 channels with the following IC50: 52.6, 14.1, and 3.8 μM respectively, in whole-cell and excised-membrane patch clamp7.Mibefradil dihydrochloride hydrate has moderate selectivity for T-type Ca2+ channels displaying IC50 values of 2.7 μM and 18.6 μM for T-type and L-type channels respectively2. Mibefradil relaxes coronary arteries without suppressing myocardial contractility and causes a dose-related decrease in heart rate. Mibefradil demonstrated end organ protection such as preventing neointima formation after vascular injury and myocardial hypertrophy3. In addition, it has been shown that it inhibits human cancer cell proliferation in vitro with several cell lines including glioblastoma (GB), by inhibiting passage beyond the G1/S interphase4,5.
Lead time: 1-2 Business Days
Country of origin: Israel/IL
Applications key
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Bioassay tested: Yes
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- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
- QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
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