Eact是一种高特异性、强效的TMEM16A激活剂，能在钙离子浓度升高时激活TMEM16A。
Cas No.:461000-66-8
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
Eact is a highly specific and potent activator of TMEM16A, which activates TMEM16A when the calcium ion concentration increases [1]. At no Ca²⁺ conditions, Eact significantly enhances the Cl- current, and increases the amplitude and frequency of isolated guinea pig ileum contraction [2]. Eact has been widely used to regulate the contraction of coronary artery smooth muscle and to control membrane potential[3].
In vivo, Eact treatment at a single dose (20μl; 4.67mM) via injecting into the paw of a mouse can induce a strong and persistent hyperalgesia to heat for 60 minutes[4]. Thirty minutes before the epilepsy test, a single dose of Eact (10mg/kg) was administered through the gastric intubation, which significantly reduced the severity of acoustically evoked seizures and decreased the frequency of wild running seizures (WRS) in rats[5].
References:
[1] Kunzelmann K, Ousingsawat J, Cabrita I, et al. TMEM16A in cystic fibrosis: activating or inhibiting?[J]. Frontiers in pharmacology, 2019, 10: 3.
[2] Hao A, Guo S, Shi S, et al. Emerging modulators of TMEM16A and their therapeutic potential[J]. The Journal of Membrane Biology, 2021, 254(4): 353-365.
[3] Dick G, Tune J. Smooth Muscle Contraction Is Regulated by Chloride Channels: Functional Evidence for TMEM16A in Porcine Coronary Arteries[J]. The FASEB Journal, 2021, 35.
[4] Liu S, Feng J, Luo J, et al. Eact, a small molecule activator of TMEM16A, activates TRPV1 and elicits pain‐and itch‐related behaviours[J]. British journal of pharmacology, 2016, 173(7): 1208-1218.
[5] Thomas M, Simms M, N’Gouemo P. Activation of calcium-activated chloride channels suppresses inherited seizure susceptibility in genetically epilepsy-prone rats[J]. Biomedicines, 2022, 10(2): 449.
Eact是一种高特异性、强效的TMEM16A激活剂，能在钙离子浓度升高时激活TMEM16A[1]。在无Ca2+条件下，Eact可显著增强Cl⁻电流，并增加离体豚鼠回肠收缩的幅度和频率[2]。Eact已被广泛用于调节冠状动脉平滑肌的收缩和膜电位控制[3]。
在体外，将单剂量（20µl；4.67mM）Eact注射到小鼠爪中，可诱导出持续60分钟的强效热痛觉过敏[4]。在癫痫试验前30分钟，通过灌胃单次给予10mg/kg剂量的Eact，可显著降低大鼠因声诱导的癫痫发作严重程度，并减少狂奔性癫痫发作的频率[5]。
| Animal experiment [1]: | |
Animal models | Genetically epilepsy-prone (GEPR-3s) rats |
Preparation Method | GEPR-3s rats (eight-week-old) were housed in a temperature/humidity-controlled room on a 12h/12h light/dark cycle with free access to food and water. Eact (10mg/kg) and T16Ainh-A01 (10mg/kg) were dissolved in dimethyl sulfonic acid (1%) and sterile water using sonication (80kHz; 100% power); the solutions were filtered and administered 30min before seizure testing. The vehicle, Eact, and T16Ainh-A01 were given p.o. by gastric intubation. To induce seizures, an acoustic stimulus that consisted of pure tones at a 100-105 decibels sound pressure level was presented until either seizure was elicited, or 60s passed with no seizure activity. |
Dosage form | 10mg/kg for once; p.o. |
Applications | Eact treatment significantly reduced the severity of sound-induced epileptic seizures and decreased the frequency of wild running seizures (WRS) in rats. |
References: | |
| Cas No. | 461000-66-8 | SDF | |
| 别名 | 3,4,5-三甲氧基-N-(2-甲氧基乙基)-N-(4-苯基-2-噻唑基)苯甲酰胺 | ||
| 化学名 | 3,4,5-trimethoxy-N-(2-methoxyethyl)-N-(4-phenylthiazol-2-yl)benzamide | ||
| Canonical SMILES | COCCN(C1=NC(C2=CC=CC=C2)=CS1)C(C3=CC(OC)=C(OC)C(OC)=C3)=O | ||
| 分子式 | C22H24N2O5S | 分子量 | 428.5 |
| 溶解度 | <42.85mg/ml in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3337 mL | 11.6686 mL | 23.3372 mL |
| 5 mM | 466.7 μL | 2.3337 mL | 4.6674 mL |
| 10 mM | 233.4 μL | 1.1669 mL | 2.3337 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet