Eact |
Catalog No.GC18142
One-Click Copy Product Info
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Eact는 TMEM16A의 고특이적이고 강력한 활성화제로 칼슘 이온 농도가 증가할 때 TMEM16A를 활성화한다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 461000-66-8
Sample solution is provided at 25 µL, 10mM.
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Eact는 TMEM16A의 고특이적이고 강력한 활성화제로 칼슘 이온 농도가 증가할 때 TMEM16A를 활성화한다. Ca²⁺가 없는 조건에서 Eact는 Cl⁻ 전류를 현저하게 증가시키고 격리된 기니피그 회장 수축의 진폭과 빈도를 증가시킨다[2]. Eact는 관상동맥 평활근의 수축을 조절하고 막 전위를 제어하기 위해 일반적으로 사용되고 있다[3].
체내 실험에서 쥐 발바닥에 주사하는 단일 용량 (20μl; 4.67mM)의 Eact 처리는 60분 동안 강력하고 지속적인 열에 대한 과통각을 유도할 수 있다[4]. 뇌전증 검사 30분 전에 위관 삽입을 통해 단일 용량의 Eact (10mg/kg)를 투여하였고 쥐에서 소리에 의해 유발된 발작의 중증도를 현저하게 감소시키고 야생 주행 발작 (WRS)의 빈도를 감소시켰다[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.
| 동물 실험 [1]: | |
동물 모형 | 유전적으로 간질이 잘 발생하는(GEPR-3) 쥐 |
제조 방법 | GEPR-3s 쥐(8주령)를 온도/습도 조절된 방에서 12시간/12시간 명암 주기로 사육하였고 사료와 물을 자유롭게 섭취할 수 있도록 하였습니다. Eact (10mg/kg)와 T16Ainh-A01 (10mg/kg)을 디메틸설폰산(1%)과 무균수에 초음파 처리(80kHz; 100% 출력)해서 용해시킨 후; 용액을 여과하고 발작 검사 30분 전에 투여하였습니다. 용매, Eact 및 T16Ainh-A01을 위관 삽입을 통해 경구(p.o.) 투여하였습니다. 발작을 유도하기 위해100-105데시벨 소음압 수준의 순음으로 구성된 청각 자극을 발작이 유발되거나 60초 동안 발작 활동이 없을 때까지 제시하였습니다. |
제형 | 10mg/kg 한번; p.o. |
응용 분야 | Eact 처리는 소리에 의해 유발된 뇌전증 발작의 심각성을 현저하게 감소시키고 쥐의 야생 주행 발작(WRS) 빈도를 감소시켰습니다. |
References: | |
| Cas No. | 461000-66-8 | SDF | |
| Chemical Name | 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 | ||
| Formula | C22H24N2O5S | M.Wt | 428.5 |
| Solubility | <42.85mg/ml in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)