产品说明书
CLP-290
 |
同义名 : | - |
| CAS号 : | 1181083-81-7 | |
| 货号 : | A692338 | |
| 分子式 : | C19H21FN4O3S | |
| 纯度 : | 95% | |
| 分子量 : | 404.459 | |
| MDL号 : | MFCD28166314 | |
| 存储条件： |
粉末 Keep in dark place,Sealed in dry,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 35 mg/mL(86.54 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The K+-Cl- cotransporter2 (KCC2) is responsible for maintaining low Cl- concentration in neurons of the central nervous system (CNS), which is essential for postsynaptic inhibition through GABAA and glycine receptors. Loss of activity of this transporter has emerged as a key mechanism underlying several neurological and psychiatric disorders, including epilepsy, motor spasticity, stress, anxiety, schizophrenia, morphine-induced hyperalgesia (MIH) and chronic pain[1]. CLP290, a CLP257 prodrug, is an orally available activator of the neuron-specific K+-Cl- cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications[1]. In vivo co-treatment with morphine and oral CLP290 prevented membrane KCC2 downregulation in superficial dorsal horn (SDH) neurons. Concurrently, co-treatment with CLP290 significantly mitigated MIH and acute administration of CLP257 in established MIH restored normal nociceptive behavior[2]. Treatment with CLP290 significantly lowered blood arginine-vasopressin (AVP) and glucose levels in STZ rats[3]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.47mL 0.49mL 0.25mL |
12.36mL 2.47mL 1.24mL |
24.72mL 4.94mL 2.47mL |
| 参考文献 |
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