| Bioactivity | CLP290 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. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose levels in STZ rats[1][2]. | ||||||||||||
| Target | KCC2 | ||||||||||||
| In Vivo | CLP290 (oral gavage; 100 mg/kg; twice a day; 7 day) enhances KCC2 activity and restores Cl- transport in superficial dorsal horn (SDH) neurons of morphine-treated rats, and prevents morphine-induced hyperalgesia (MIH) in rat[1]. Animal Model: | ||||||||||||
| Name | CLP290 | ||||||||||||
| CAS | 1181083-81-7 | ||||||||||||
| Formula | C19H21FN4O3S | ||||||||||||
| Molar Mass | 404.46 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Ferrini F, et al. Enhancing KCC2 function counteracts morphine-induced hyperalgesia. Sci Rep. 2017 Jun 20;7(1):3870. [2]. Gagnon M, et al. Chloride extrusion enhancers as novel therapeutics for neurological diseases. Nat Med. 2013 Nov;19(11):1524-8. [3]. Kim YB, et al. Excitatory GABAergic Action and Increased Vasopressin Synthesis in Hypothalamic Magnocellular Neurosecretory Cells Underlie the High Plasma Level of Vasopressin in Diabetic Rats. Diabetes. 2018 Mar;67(3):486-495. |