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

Ulixacaltamide  (Synonyms: Z944; PRAX-944)

目录号: HY-120546 纯度: 98.73%
COA 产品使用指南

Ulixacaltamide (Z944) 是一种口服有效的 T 型钙通道 (calcium channel) 拮抗剂,可缓解癫痫发病进展。Ulixacaltamide 在正碱性震颤动物模型中,有效地减轻震颤。Ulixacaltamide 能逆转热痛觉过敏,并介导疼痛的缓解。

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Ulixacaltamide Chemical Structure

Ulixacaltamide Chemical Structure

CAS No. : 1199236-64-0

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Customer Review

Other Forms of Ulixacaltamide:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

细胞效力
(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]
体外研究
(In Vitro)

Ulixacaltamide (1 μM) 抑制了大约 50% 瞬时表达的人 Cav3.2 钙通道全细胞电流幅度 (IC50=0.60 μM) [4]
Ulixacaltamide (10 μM) 完全消除了 T 型钙通道被激活后去极化至 30 mV 所产生的瞬态电流成分,使整个 tsA-201 细胞钙电流降低了约 70%[4]

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

体内研究
(In Vivo)

Ulixacaltamide (5, 10, 30 和 100 mg/kg; i.p.; 单剂量注射) 在30 mg/kg 的剂量下延缓了完全诱发小鼠的癫痫发展进程,需要更多的刺激次数来诱发 III 类、IV 类或 V 类癫痫发作[2]
Ulixacaltamide (0.1-3 mg/kg; p.o.) 剂量依赖性地降低了 Harmaline 引起的大鼠震颤频率[3]
Ulixacaltamide (10 mg/kg; i.p.; 单剂量注射) 对 Complete Freund's adjuvant (CFA) (HY-153808) 诱导的热过敏反应在雄性 C57BL 小鼠体内有效逆转,在注射后 90 分钟达到峰值并产生镇痛作用[4]

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.
分子量

383.89

Formula

C19H27ClFN3O2

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

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

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (130.25 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 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
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 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
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.

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产品名称:
Ulixacaltamide
目录号:
HY-120546
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