Ulixacaltamide
Based on 1 publication(s) in Google Scholar
Ulixacaltamide (Z944) is an orally available T-type calcium channel antagonist that can slow the progression of epilepsy. Ulixacaltamide effectively reduces tremor in a normal alkaline tremor animal model. Ulixacaltamide reverses thermal hyperalgesia and mediates pain relief.
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- Pureza: 99.26%
- No. CAS: 1199236-64-0
- Fòrmula: C19H27ClFN3O2
- Peso molecular:383.89
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) Ulixacaltamide
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Actividad biológica
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T-type calcium channel |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
37 nM
Compound: 2
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Inhibition of T-type calcium channel Cav3.1 (unknown origin) expressed in HEK293 cells assessed as calcium influx by Fluo-4-AM dye-based FLIPR assay
Inhibition of T-type calcium channel Cav3.1 (unknown origin) expressed in HEK293 cells assessed as calcium influx by Fluo-4-AM dye-based FLIPR assay
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[PMID: 27579577] |
| HEK293 | IC50 |
73 nM
Compound: 2
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Inhibition of recombinant T-type calcium channel Cav3.2 (unknown origin) expressed in HEK293 cells assessed as inhibition of CaCl2-induced calcium influx preincubated for 3 mins prior CaCl2 addition by Fluo-4-AM dye-based FLIPR assay
Inhibition of recombinant T-type calcium channel Cav3.2 (unknown origin) expressed in HEK293 cells assessed as inhibition of CaCl2-induced calcium influx preincubated for 3 mins prior CaCl2 addition by Fluo-4-AM dye-based FLIPR assay
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[PMID: 27579577] |
| HEK293 | IC50 |
86 nM
Compound: 2
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Inhibition of T-type calcium channel Cav3.3 (unknown origin) expressed in HEK293 cells assessed as calcium influx by Fluo-4-AM dye-based FLIPR assay
Inhibition of T-type calcium channel Cav3.3 (unknown origin) expressed in HEK293 cells assessed as calcium influx by Fluo-4-AM dye-based FLIPR assay
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[PMID: 27579577] |
Ulixacaltamide (1 μM) inhibits the whole-cell current amplitude of transiently expressed human Cav3.2 calcium channels by approximately 50% (IC50=0.60 μM)[4]. Ulixacaltamide (10 μM) abolishs completely the transient current component generated by depolarization to 30 mV after activation of T-type calcium channels, reducing the whole-cell calcium current of tsA-201 cells by approximately 70%[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat model of harmaline-induced tremor[3].
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Dosage:0.1-3 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Reduced tremor frequency by 50% at a dose of 1 mg/kg and by 72% at a dose of 3 mg/kg.
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Animal Model:Rat model of harmaline-induced tremor[3].
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Dosage:3-300 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Did not induce gross motor impairment including sedation or ataxia in rats at a dose of 100 mg/kg. At a dose of 300 mg/kg, 7 of 10 rats showed mild dyskinesia and 1 showed moderate dyskinesia.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1199236-64-0
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Appearance Solid
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Peso molecular 383.89
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Fòrmula C19H27ClFN3O2
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Color White to off-white
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SMILES
O=C(C1=CC(F)=CC(Cl)=C1)NCC2CCN(CC2)CC(NC(C)(C)C)=O
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Synonyms
Z944; PRAX-944
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 50 mg/mL (130.25 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Marks WN, et al. The T-type calcium channel antagonist Z944 rescues impairments in crossmodal and visual recognition memory in Genetic Absence Epilepsy Rats from Strasbourg. Neurobiol Dis. 2016 Oct;94:106-15. [Content Brief]
[2]. Casillas-Espinosa P M, et al. Z944, a novel selective T-type calcium channel antagonist delays the progression of seizures in the amygdala kindling model[J]. PLoS One, 2015, 10(8): e0130012. [Content Brief]
[3]. Scott L, et al. Translational pharmacology of PRAX‐944, a novel T‐type calcium channel blocker in development for the treatment of essential tremor[J]. Movement Disorders, 2022, 37(6): 1193-1201. [Content Brief]
[4]. Antunes F T T, et al. Effect of ABT-639 on Cav3. 2 channel activity and its analgesic actions in mouse models of inflammatory and neuropathic pain[J]. European Journal of Pharmacology, 2024, 967: 176416. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6049 mL | 13.0246 mL | 26.0491 mL | 65.1228 mL |
| 5 mM | 0.5210 mL | 2.6049 mL | 5.2098 mL | 13.0246 mL | |
| 10 mM | 0.2605 mL | 1.3025 mL | 2.6049 mL | 6.5123 mL | |
| 15 mM | 0.1737 mL | 0.8683 mL | 1.7366 mL | 4.3415 mL | |
| 20 mM | 0.1302 mL | 0.6512 mL | 1.3025 mL | 3.2561 mL | |
| 25 mM | 0.1042 mL | 0.5210 mL | 1.0420 mL | 2.6049 mL | |
| 30 mM | 0.0868 mL | 0.4342 mL | 0.8683 mL | 2.1708 mL | |
| 40 mM | 0.0651 mL | 0.3256 mL | 0.6512 mL | 1.6281 mL | |
| 50 mM | 0.0521 mL | 0.2605 mL | 0.5210 mL | 1.3025 mL | |
| 60 mM | 0.0434 mL | 0.2171 mL | 0.4342 mL | 1.0854 mL | |
| 80 mM | 0.0326 mL | 0.1628 mL | 0.3256 mL | 0.8140 mL | |
| 100 mM | 0.0260 mL | 0.1302 mL | 0.2605 mL | 0.6512 mL |
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