TC-T 6000
目录号 : GC50098
TC-T 6000是一种有效的、选择性的人平衡核苷转运蛋白4（ENT4）抑制剂，IC50为74.4nM。
Cas No.:949467-71-4
Sample solution is provided at 25 µL, 10mM.
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TC-T 6000, a Dipyridamole analog, is a potent and selective human ENT4 (Balanced nucleoside transporter 4) inhibitor with an IC50 of 74.4nM. Making it about 38 times more potent than Dipyridamole [1].
TC-T 6000(10μM; 24h) shows no cytotoxicity against PK15/hENT4 cells.
References:
[1]. Wang C, Lin W, et,al. Dipyridamole analogs as pharmacological inhibitors of equilibrative nucleoside transporters. Identification of novel potent and selective inhibitors of the adenosine transporter function of human equilibrative nucleoside transporter 4 (hENT4). Biochem Pharmacol. 2013 Dec 1;86(11):1531-40. doi: 10.1016/j.bcp.2013.08.063. Epub 2013 Sep 7. PMID: 24021350; PMCID: PMC3866046.
TC-T 6000是一种有效的、选择性的人平衡核苷转运蛋白4（ENT4）抑制剂，IC50为74.4nM。TC-T 6000比双嘧达莫有效约38倍[1]。
TC-T 6000(10μM;24h)对PK15/hENT4细胞无细胞毒性。
| Cell experiment [1]: | |
Cell lines | PK15/hENT cells (PK15 cells stably expressing hENT4) |
Preparation Method | Cells were seeded at 5×103 cells were seeded in 96-well plates, treated with 10μM test TC-T 6000 and incubated at 37 ℃ in phenol-free MEM for 24h. |
Reaction Conditions | 10μM; 24h |
Applications | TC-T 6000 shows no cytotoxicity against PK15/hENT4 cells. |
| Transporter inhibition assays [1]: | |
Preparation Method | Transport activity of cells transiently transfected with hENT4 was examined with [3H] Adenosine. K15/hENT4 cells were incubated with transport buffer containing TC-T 6000 at pH 6.0 for 15min before addition of 0.2μM [3H] Adenosine, and then further incubation for 2min. Uptake was terminated by rapidly aspirating the incubation mixture and washing cells three times with ice-cold PBS. The cells were solubilized overnight in 400μl of 5% Triton X-100 and 200μl of cell lysate was counted using a scintillation counter. Protein concentration in the cell lysate was determined using the BCA protein assay kit. The concentrations of test compounds that caused 50% inhibition of [3H] Adenosine uptake (IC50) were calculated using a nonlinear fitting method in the Prism 4 program. |
Reaction Conditions | 10μM; 15min |
Applications | TC-T 6000 is a potent and selective human ENT4 (Balanced nucleoside transporter 4) inhibitor with an IC50 of 74.4nM. |
References: | |
| Cas No. | 949467-71-4 | SDF | |
| Canonical SMILES | CC(C)CN(CC(C)C)C2=NC(NCCO)=NC1=C(N(CC(C)C)CC(C)C)N=C(NCCO)N=C12 | ||
| 分子式 | C26H48N8O2 | 分子量 | 504.71 |
| 溶解度 | Soluble 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。 |
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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 | 1.9813 mL | 9.9067 mL | 19.8134 mL |
| 5 mM | 0.3963 mL | 1.9813 mL | 3.9627 mL |
| 10 mM | 0.1981 mL | 0.9907 mL | 1.9813 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet