2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. Ulixacaltamide

Ulixacaltamide  (Synonyms: Z944; PRAX-944)

Cat. No.: HY-120546 Purity: 98.73%
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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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Ulixacaltamide Chemical Structure

Ulixacaltamide Chemical Structure

CAS No. : 1199236-64-0

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Based on 1 publication(s) in Google Scholar

Other Forms of Ulixacaltamide:

Ulixacaltamide Related Antibodies

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View All Calcium Channel Isoform Specific Products:

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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Description

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[1][2][3][4].

IC50 & Target

T-type calcium channel

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
37 nM
Compound: 2
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
[PMID: 27579577]
HEK293 IC50
73 nM
Compound: 2
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
[PMID: 27579577]
HEK293 IC50
86 nM
Compound: 2
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
[PMID: 27579577]
In Vitro

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.

Ulixacaltamide Related Antibodies
In Vivo

Ulixacaltamide (5, 10, 30 and 100 mg/kg; i.p.; single dose) delaies the development of fully induced epilepsy in mice at a dose of 30 mg/kg, requiring more stimulations to induce type III, IV or V seizures[2].
Ulixacaltamide (0.1-3 mg/kg; p.o.) dose-dependently reduces the frequency of harmaline-induced tremors in rats[3].
Ulixacaltamide (10 mg/kg; i.p.; single dose) effectively reverses the thermal hypersensitivity response induced by Complete Freund's adjuvant (CFA) (HY-153808) in male C57BL mice, with the analgesic effect reaching a peak at 90 minutes after injection[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Rat model of harmaline-induced tremor[3].
Dosage: 0.1-3 mg/kg
Administration: Oral gavage (p.o.)
Result: Reduced tremor frequency by 50% at a dose of 1 mg/kg and by 72% at a dose of 3 mg/kg.
Animal Model: Rat model of harmaline-induced tremor[3].
Dosage: 3-300 mg/kg
Administration: Oral gavage (p.o.)
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.
Molecular Weight

383.89

Formula

C19H27ClFN3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC(F)=CC(Cl)=C1)NCC2CCN(CC2)CC(NC(C)(C)C)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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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Ulixacaltamide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ulixacaltamide1199236-64-0Z944 PRAX-944Z 944Z-944PRAX944PRAX 944PRAX-944Calcium ChannelCa2+ channelsCa channelsInhibitorinhibitorinhibit

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