H-Val-Tyr-OH is a dipeptide that inhibits the angiotensin converting enzyme (ACE) with an IC50 value of 26μM [1]. H-Val-Tyr-OH specifically inhibits angiotensin I (Ang I)-evoked contraction through ACE inhibition, without affecting angiotensin II receptor[2]. H-Val-Tyr-OH has been widely used as an internal standard to develop infrared spectroscopy and nuclear magnetic resonance methods for the identification of related compounds[3].
In vitro, H-Val-Tyr-OH treatment (100μM) for 5h reduced the phosphorylation level of IκBα in lipopolysaccharide (LPS)-stimulated RAW 264.7 cells, and inhibited the activation of the NF-κB signaling pathway[4].
In vivo, H-Val-Tyr-OH treatment via oral administration at a single dose of 0.1mg/g resulted in a prolonged reduction of blood pressure for up to 9h in hypertensive mice [5].
References:
[1] Matsufuji H, Matsui T, Ohshige S, et al. Antihypertensive effects of angiotensin fragments in SHR[J]. Bioscience, biotechnology, and biochemistry, 1995, 59(8): 1398-1401.
[2] Vercruysse L, Morel N, Van Camp J, et al. Antihypertensive mechanism of the dipeptide Val-Tyr in rat aorta[J]. Peptides, 2008, 29(2): 261-267.
[3] Koleva B B, Kolev T M, Spiteller M. Spectroscopic and structural elucidation of l-tyrosine-containing dipeptides valyl-tyrosine and tyrosyl-alanine: Solid-state IR-LD spectroscopy, quantum chemical calculations and vibrational analysis[J]. Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy, 2007, 68(5): 1187-1196.
[4] Yasir M, Park J, Han E T, et al. Investigating Natural Product Inhibitors of IKKα: Insights from Integrative In Silico and Experimental Validation[J]. Molecules, 2025, 30(9): 2025.
[5] Matsui T, Hayashi A, Tamaya K, et al. Depressor effect induced by dipeptide, Val‐Tyr, in hypertensive transgenic mice is due, in part, to the suppression of human circulating renin–angiotensin system[J]. Clinical and experimental pharmacology and physiology, 2003, 30(4): 262-265.
H-Val-Tyr-OH是一种二肽，能够抑制血管紧张素转化酶（ACE），IC50值为26μM[1]。H-Val-Tyr-OH通过抑制ACE，特异性阻断血管紧张素I（Ang I）诱发的收缩反应，而不影响血管紧张素II受体[2]。H-Val-Tyr-OH已被广泛用作内参，用于开发红外光谱和核磁共振方法以鉴定相关化合物[3]。
在体外，使用100μM的H-Val-Tyr-OH处理脂多糖（LPS）刺激的RAW 264.7细胞5小时，降低了IκBα的磷酸化水平，并抑制了NF-κB信号通路的激活[4]。
在体内，高血压小鼠单次口服0.1mg/g剂量的H-Val-Tyr-OH，使血压持续降低长达9小时[5]。