TRAM 39
目录号 : GC15323
Potent KCa3.1 blocker
Cas No.:197525-99-8
Sample solution is provided at 25 µL, 10mM.
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TRAM-39, 2-(2-chlorophenyl)-2, 2-diphenyl acetonitrile, is a potent, synthetic, selective inhibitor of intermediate-conductance Ca2+-activated K+channels. TRAM-39 selectively block K-Ca3 but do not inhibit other Ca2+-activated K+channels.[1,3]
Intermediate conductance Ca2-activated K channels are the product of the IKCa1 genes and are important in regulating the membrane potential of colonic epithelial cells, and lymphocytes. The IKCa1 gene is also important in volume regulation of red blood cells. IKCa1 modulates the paneth cell alpha-defensin secretion and involve in the mucosal defense of the intestinal epithelium against ingested bacterial pathogens.[1,2]
TRAM-39 inhibits the Kca3,so as to Inhibit paneth cell secretion stimulated by bacteria or bacterial lipopolysaccharide. Endothelium-derived hyperpolarizing factor (EDHF ) responses are brought about by the activation of endothelial SKCa and IKCa.[1,3]
A combination of TRAM-39 and apamin abolished endothelium-derived hyperpolarizing factor (EDHF) mediated relaxation of the rat isolated mediated relaxation. The combination of TRAM-39 and apamin evoked a small, transient depolarization of endothelial cells.[2]
References:
[1] Ayabe T1, Wulff H, Darmoul D, etal. , Modulation of mouse Paneth cell alpha-defensin secretion by mIKCa1, a Ca2+-activated, intermediate conductance potassium channel. J Biol Chem. 2002 Feb 1;277(5):3793-800.
[2]Hinton JM, Langton PD. Inhibition of EDHF by two new combinations of K+-channel inhibitors in rat isolated mesenteric arteries. Br J Pharmacol. 2003 Mar; 138(6):1031-5.
[3]Burnham MP, Johnson IT, Weston AH. Impaired small-conductance Ca2+-activated K+ channel-dependent EDHF responses in Type II diabetic ZDF rats. Br J Pharmacol. 2006 Jun;148(4):434-41.
| Cas No. | 197525-99-8 | SDF | |
| 化学名 | 2-(2-chlorophenyl)-2,2-diphenylacetonitrile | ||
| Canonical SMILES | ClC(C=CC=C1)=C1C(C2=CC=CC=C2)(C#N)C3=CC=CC=C3 | ||
| 分子式 | C20H14ClN | 分子量 | 303.78 |
| 溶解度 | <15.44mg/ml in DMSO | 储存条件 | Store at RT |
| 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2919 mL | 16.4593 mL | 32.9186 mL |
| 5 mM | 0.6584 mL | 3.2919 mL | 6.5837 mL |
| 10 mM | 0.3292 mL | 1.6459 mL | 3.2919 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%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet