p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine) 是一种高效、选择性的,可逆、竞争性的色氨酸羟化酶 (TPH) 抑制剂,其 Ki 值为 32.6 μM。
生物活性
p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a K i of 32.6 μM.
性状
Solid
IC50 & Target[1][2]
Ki: 32.6 μM (TPH)
体外研究(In Vitro)
p-Ethynylphenylalanine selectively and reversibly inhibits the biosynthesis of serotonin.p-Ethynylphenylalanine has a low affinity for various recombinant 5-HT receptors (5-HT1, 5-HT2, 5-HT4, 5-HT5, 5-HT6, and 5-HT7). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
p-Ethynylphenylalanine (30 mg/kg; i.p.) decreases in 5-HT and 5-HIAA levels in the rat midbrain but not in tissue.
p-Ethynylphenylalanine does not inhibit the aromatic amino acid decarboxylase. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Stokes AH, et al. p-ethynylphenylalanine: a potent inhibitor of tryptophan hydroxylase. J Neurochem. 2000 May;74(5):2067-73.
溶解度数据
In Vitro: 1M HCl : 240 mg/mL (1268.43 mM; ultrasonic and adjust pH to 1 with HCl)1M NaOH : 240 mg/mL (1268.43 mM; ultrasonic and adjust pH to 11 with NaOH)DMSO : 2.22 mg/mL (11.73 mM; Need ultrasonic)