Valproic acid sodium salt (Sodium valproate)是一种HDAC抑制剂,IC50为0.4 mM,也抑制GABA-转氨酶或琥珀酸半醛脱氢酶。
Valproic Acid Sodium Salt is a branched chain fatty acid which is reported to inhance central GABAergic neurotransmission and inhibit Sodium Channel Protein (Na+ channels). This compound is also reported to cause inositol depletion, activate the ERK pathway, inhibit GSK-3α and GSK-3β. This compound is also an inhibitor of the CYP2C9 enzyme. Valproic Acid Sodium Salt has been reported to be a potent inhibitor of HDAC (histone deacetylase) in vitro (IC50 = 400 μM for HDAC1), thereby relieving HDAC-dependent transcriptional repression and causes the hyperacetylation of histones in cultured cells. In animal studies, Valproic Acid has been observed to reduce tumor growth and metastasis formation.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Phiel CJ, et al. J Biol Chem, 2001, 276(39), 36734-36741.
[2] Tunnicliff, G., et al., 1999. Actions of sodium valproate on the central nervous system. Journal of physiology and pharmacology : an official journal of the Polish Physiological Society. 50(3): 347-65.
[3] Göttlicher, M., et al., 2001. Valproic acid defines a novel class of HDAC inhibitors inducing differentiation of transformed cells. The EMBO journal. 20(24): 6969-78.
[4] Gökçe, Selim., et al., 2010. Valproic acid-associated vanishing bile duct syndrome. Journal of child neurology. 25(7): 909-11.
分子式 C8H15NaO2 |
分子量 166.19 |
CAS号 1069-66-5 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 50 mM |
Water 50 mg/mL |
Ethanol 30 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00431522 | Bipolar Disorder | Drug: Valproic acid, sodium salt | Sanofi | Phase 4 | 2004-12-01 | 2009-05-28 |
NCT00228046 | Attention Deficit Disorder With Hyperactivity|Conduct Disorder|Oppositional Defiant Disorder | Drug: Divalproex Sodium|Drug: Methylphenidate|Drug: Dextroamphetamine|Drug: Mixed Amphetamine Salts|Behavioral: Family Counseling|Behavioral: Behavior Management Training with Parents | Stony Brook University|National Institute of Mental Health (NIMH) | Phase 4 | 2004-01-01 | 2013-10-29 |
NCT01960075 | Benzodiazepine Refractory Status Epilepticus | Drug: Fosphenytoin|Drug: Levetiracetam|Drug: Valproic acid | University of Virginia|University of Michigan|Medical University of South Carolina|Children's Research Institute|University of Minnesota - Clinical and Translational Science Institute|National Institute of Neurological Disorders and Stroke (NINDS) | Phase 3 | 2015-10-01 | 2016-11-03 |
NCT01674010 | Bipolar 1 Disorder | Drug: ELND005|Drug: Lamotrigine|Drug: Valproic acid|Drug: Placebo | Transition Therapeutics Ireland Limited|Elan Pharmaceuticals | Phase 2 | 2012-08-01 | 2016-05-17 |
NCT00088452 | Childhood Absence Epilepsy|Petit Mal Epilepsy|Epilepsy|Seizures | Drug: ethosuximide|Drug: lamotrigine|Drug: valproic acid | Children's Hospital Medical Center, Cincinnati|National Institute of Neurological Disorders and Stroke (NINDS) | Phase 3 | 2004-07-01 | 2017-02-03 |
NCT00021866 | Epilepsy|Seizure|Cognition Disorders | Behavioral: Differential Abilities Scale|Behavioral: Neuropsychological Testing | Emory University|National Institute of Neurological Disorders and Stroke (NINDS) | 2000-09-01 | 2013-11-08 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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