CLP290 is a novel, orally available KCC2 modulator, highly selective for KCC2 over related Cl- transporters. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose levels in STZ rats.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO ≥ 25 mg/mL|
Excitatory GABAergic Action and Increased Vasopressin Synthesis in Hypothalamic Magnocellular Neurosecretory Cells Underlie the High Plasma Level of Vasopressin in Diabetic Rats.
Kim YB, et al. Diabetes. 2018 Mar;67(3):486-495. PMID: 29212780.
Enhancing KCC2 function counteracts morphine-induced hyperalgesia.
Ferrini F, et al. Sci Rep. 2017 Jun 20;7(1):3870. PMID: 28634406.
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