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。
Cas No.:3061-91-4
Sample solution is provided at 25 µL, 10mM.
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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]。
| Cell experiment [1]: | |
Cell lines | RAW 264.7 cells |
Preparation Method | RAW 264.7 cells were cultured in DMEM medium containing 10% fetal bovine serum (FBS) and 10% heat-inactivated fetal bovine serum and 100U/ml penicillin–streptomycin at 37℃ and 5% CO2. Cells were incubated in 100μM of H-Val-Tyr-OH for 1h and then stimulated with 1μg/ml of LPS for 4h. Subsequently, western blot analysis was carried out. |
Reaction Conditions | 100μM; 5h |
Applications | H-Val-Tyr-OH treatment reduced the phosphorylation level of IκBα in LPS-stimulated RAW 264.7 cells. |
| Animal experiment [2]: | |
Animal models | Male Tsukuba Hypertensive Mouse (THM) |
Preparation Method | Male THMs (11 weeks of age), which were housed in an air-ventilated cabinet under specific pathogen-free conditions at 23±1°C and 55±5% humidity under controlled lighting from 08:00 to 20:00. Mice had free access to food (NMF) and autoclaved water. A single oral dose of 0.1mg/g H-Val-Tyr-OH, dissolved in 1ml saline solution, was administered to THM by intubation with a nutritional catheter. Control mice were given the same volume of saline solution alone. Systolic blood pressure (SBP) and heart rate (HR) were measured 0, 1, 3, 6, 9, 12 and 24h after administration. |
Dosage form | 0.1mg/g for once; p.o. |
Applications | H-Val-Tyr-OH treatment resulted in a prolonged reduction of blood pressure for up to 9h in THM, without affecting HR. |
References: | |
| Cas No. | 3061-91-4 | SDF | |
| 别名 | Valyl-tyrosine | ||
| 分子式 | C14H20N2O4 | 分子量 | 280.32 |
| 溶解度 | DMSO : 100 mg/mL (356.74 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5674 mL | 17.8368 mL | 35.6735 mL |
| 5 mM | 713.5 μL | 3.5674 mL | 7.1347 mL |
| 10 mM | 356.7 μL | 1.7837 mL | 3.5674 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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