KT195
(Synonyms: ML-295) 目录号 : GC13367
An ABHD6 inhibitor
Cas No.:1402612-58-1
Sample solution is provided at 25 µL, 10mM.
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IC50: 10 nM
KT195 is an α/β-hydrolase domain-containing protein 6 (ABHD6) inhibitor.
AMPA receptors are major postsynaptic receptors mediating fast excitatory neurotransmission and synaptic plasticity. The proper functioning of AMPA receptors is critical for brain function, and AMPA receptor dysfunction can result in multiple neurologic disorders. AMPA receptors are macromolecular complexes associated with various auxiliary proteins, including α/β-hydrolase domain-containing 6 (ABHD6).
In vitro: KT195 acted as a potent and selective inhibitor of ABHD6 with negligible activity against DAGLβ. KT195 also had a comparable selectivity profile to its analogs of KT109 and KT172 against other serine hydrolases. KT195 also showed negligible activity against DAGLβ while completely inactivating ABHD6. KT195 blocked ABHD6 activity with no activity against other serine hydrolases [1].
In vivo: Mice were treated with KT195, KT172 and KT109 at various doses for 4 h, sacrificed, and thioglycollate-elicited peritoneal macrophages were collected and analyzed. Results showed that both KT172 and KT109 could completely inactivate DAGLβ at doses as low as 0.5 mg/kg. Whereas, KT195 showed no activity against DAGLβ at any tested dose. Moreover, time-course studies revealed that both KT109 and KT172 produced complete inhibition of macrophage DAGLβ, and this inhibition was maintained for 6 h, but however, KT195 showed no evidence of DAGLβ inhibition [1].
Clinical trial: Up to now, KT195 is still in the preclinical development stage.
Reference:
[1] K. L. Hsu, K. Tsuboi, A. Adibekian, et al. DAGLβ inhibition perturbs a lipid network involved in macrophage inflammatory responses. Nature Chemical Biology. 8(12), 999-1007 (2012).
| Cas No. | 1402612-58-1 | SDF | |
| 别名 | ML-295 | ||
| 化学名 | [4-(4'-methoxy[1,1'-biphenyl]-4-yl)-1H-1,2,3-triazol-1-yl](2-phenyl-1-piperidinyl)-methanone | ||
| Canonical SMILES | O=C(N1N=NC(C2=CC=C(C3=CC=C(OC)C=C3)C=C2)=C1)N4C(C5=CC=CC=C5)CCCC4 | ||
| 分子式 | C27H26N4O2 | 分子量 | 438.5 |
| 溶解度 | ≤10mg/ml in DMSO;5mg/ml in dimethyl formamide | 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 | 2.2805 mL | 11.4025 mL | 22.805 mL |
| 5 mM | 0.4561 mL | 2.2805 mL | 4.561 mL |
| 10 mM | 0.2281 mL | 1.1403 mL | 2.2805 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