LDN-27219
目录号 : GC13015
An inhibitor of TG2
Cas No.:312946-37-5
Sample solution is provided at 25 µL, 10mM.
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LDN-27219 is a reversible and slow-binding inhibitor of tissue transglutaminase (TGases) with IC50 value of 250nM for TGase 2 [1, 2].
LDN-27219 is discovered as a moderately potent inhibitor of TGase. It shows inhibitory activity against hTGase with IC50 value of 0.6μM. LDN-27219 is also a selective inhibitor. It has no effect on Factor XIIIa or caspase 3 at concentration up to 50μM. Besides that, LDN-27219 is found to be mutually exclusive inhibitors with GTP which is an allosteric inhibitor of TGase. It binds at sites other than the GTP site or the active site of the enzyme. The mechanism of LDN-27219 is also not similar with GTP. It has a modest effect on the binding of calcium. Moreover, it is found that LDN-27219 is a competitive inhibitor of the hTGase-catalyzed hydrolysis of Z-Pro-Gln-Ala-Trp [1].
References:
[1] Case A, Stein R L. Kinetic analysis of the interaction of tissue transglutaminase with a nonpeptidic slow-binding inhibitor. Biochemistry, 2007, 46(4): 1106-1115.
[2] Duval E, Case A, Stein R L, et al. Structure–activity relationship study of novel tissue transglutaminase inhibitors. Bioorganic & medicinal chemistry letters, 2005, 15(7): 1885-1889.
| Cas No. | 312946-37-5 | SDF | |
| 化学名 | (Z)-2-((4-oxo-3,5-diphenyl-3,4-dihydrothieno[2,3-d]pyrimidin-2-yl)thio)acetohydrazonic acid | ||
| Canonical SMILES | N/N=C(O)/CSC1=NC2=C(C(N1C3=CC=CC=C3)=O)C(C4=CC=CC=C4)=CS2 | ||
| 分子式 | C20H16N4O2S2 | 分子量 | 408.5 |
| 溶解度 | DMSO: 100 mM | 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 | 2.448 mL | 12.2399 mL | 24.4798 mL |
| 5 mM | 0.4896 mL | 2.448 mL | 4.896 mL |
| 10 mM | 0.2448 mL | 1.224 mL | 2.448 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