| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg | |||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
Z944 targets T-type calcium channels (Cav3.x), specifically the Cav3.1, Cav3.2, and Cav3.3 isoforms. It is a state-dependent antagonist. By blocking these channels, it reduces calcium influx into neurons, modulating neuronal excitability and neurotransmitter release. Z944 is a selective T-type calcium channel blocker. It disrupts prepulse inhibition in both epileptic and non-epileptic rats.
|
|---|---|
| ln Vitro |
In vitro, Z944 is a potent T-type calcium channel antagonist with IC₅₀ values of 50 to 160 nM for hCav3.1, hCav3.2, and hCav3.3. It exhibits 50- to 600-fold selectivity for Cav3.x channels over related ion channels. Its ability to inhibit T-type calcium currents has been characterized in patch-clamp electrophysiology studies using cells expressing the different Cav3 isoforms.
|
| ln Vivo |
In vivo, Z944 delays the progression of seizures in the amygdala kindling model. It disrupts prepulse inhibition in both epileptic and non-epileptic rats. Z944 rescues impairments in crossmodal and visual recognition memory. It is an orally available T-type calcium channel antagonist that can slow the progression of epilepsy. It effectively reduces tremor in a normal alkaline tremor animal model.
|
| Enzyme Assay |
The activity of Z944 can be assessed using electrophysiological techniques, specifically patch-clamp electrophysiology. Cells expressing human Cav3.1, Cav3.2, or Cav3.3 channels are treated with varying concentrations of Z944. The T-type calcium currents are recorded, and the IC₅₀ for channel blockade is determined from dose-response curves. Selectivity over other ion channels is assessed using similar assays.
|
| Cell Assay |
To evaluate the cellular effects of Z944, neurons or cells expressing T-type calcium channels are treated with the compound. The inhibition of calcium influx and its effects on neuronal excitability are measured using calcium imaging or electrophysiological recordings. The compound's effects on cell viability and neurotransmitter release can also be assessed.
|
| Animal Protocol |
In vivo studies with Z944 typically involve administration to animal models via oral routes. In models of epilepsy (e.g., amygdala kindling model), the compound's effects on seizure progression are assessed. In models of tremor, its effects on tremor severity are evaluated. Its effects on cognitive function are assessed using behavioral tests such as prepulse inhibition and recognition memory tasks.
|
| ADME/Pharmacokinetics |
Z944 has a molecular formula of C₁₉H₂₇ClFN₃O₂ and a molecular weight of 383.89 g/mol. Its CAS number is 1199236-64-0. It is an orally bioavailable compound. The purity is typically ≥98%. It should be stored according to the manufacturer's instructions.
|
| Toxicity/Toxicokinetics |
Specific toxicology data for Z944 are not extensively detailed in the available literature. However, its use in animal models at effective doses suggests a degree of tolerability. As with all research compounds, standard safety precautions should be taken when handling Z944. It is intended for research use only and is not for human consumption.
|
| References | |
| Additional Infomation |
Ulisakamide belongs to the piperidine, benzamide, monochlorobenzene, monofluorobenzene, and secondary carboxamide classes. It is a T-type calcium channel blocker and a non-narcotic analgesic.
Z944 (Ulixacaltamide) is a potent, selective, and orally available T-type calcium channel antagonist. It has IC₅₀ values of 50-160 nM for Cav3.1, Cav3.2, and Cav3.3 channels. Z944 delays the progression of seizures in epilepsy models and reduces tremor. It is a research tool for studying T-type calcium channels, epilepsy, and pain. |
| Molecular Formula |
C19H27N3O2FCL
|
|---|---|
| Molecular Weight |
383.88798
|
| Exact Mass |
383.178
|
| CAS # |
1199236-64-0
|
| Related CAS # |
Ulixacaltamide-d9 hydrochloride;1346604-21-4
|
| PubChem CID |
44540045
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.188
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
26
|
| Complexity |
490
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JOCLITFYIMJMNK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H27ClFN3O2/c1-19(2,3)23-17(25)12-24-6-4-13(5-7-24)11-22-18(26)14-8-15(20)10-16(21)9-14/h8-10,13H,4-7,11-12H2,1-3H3,(H,22,26)(H,23,25)
|
| Chemical Name |
N-[[1-[2-(tert-butylamino)-2-oxoethyl]piperidin-4-yl]methyl]-3-chloro-5-fluorobenzamide
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~130.25 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6049 mL | 13.0246 mL | 26.0491 mL | |
| 5 mM | 0.5210 mL | 2.6049 mL | 5.2098 mL | |
| 10 mM | 0.2605 mL | 1.3025 mL | 2.6049 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
