Benzamidine (hydrochloride)是一种可逆的、竞争性胰蛋白酶样丝氨酸蛋白酶抑制剂。
Cas No.:1670-14-0
Sample solution is provided at 25 µL, 10mM.
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Benzamidine (hydrochloride) is a reversible, competitive trypsin-like serine protease inhibitor. Benzamidine inhibits the activities of tryptase (Ki=20μM), trypsin (Ki=21μM), uPA (Ki=97μM, factor Xa (Ki=110μM), thrombin (Ki=320μM), and tPA (Ki=750μM). Benzamidine can be used in studies related to the coagulation and fibrinolytic systems, physiological enzymology, and relevant pharmacology[1-4].
In vitro, human fetal lung fibroblasts were pretreated with Benzamidine (1–100μM) for 60 minutes, followed by stimulation with human mast cell tryptase (17.6mU/ml) for 48 hours. Benzamidine inhibited tryptase-induced fibroblast proliferation[5]. HEK293 cells incubated with KIF (10μM) and SWA (50μM) were treated with Benzamidine (5mM) for 48 hours. Benzamidine promoted cellular corin expression and inhibited corin autocleavage[6].
In vivo, Benzamidine (100μM; 200μl) was administered by intragastric gavage to MC903-induced atopic dermatitis (AD) model mice for 14 consecutive days. Benzamidine significantly alleviated the inflammatory phenotype and inflammatory infiltration in the mice[7].
References:
[1] Katz BA, Mackman R, Luong C, et al. Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator. Chem Biol. 2000 Apr;7(4):299-312.
[2] Cairns JA, Walls AF. Mast cell tryptase stimulates the synthesis of type I collagen in human lung fibroblasts. J Clin Invest. 1997 Mar 15;99(6):1313-21.
[3] Ristow SS, Starkey JR, Hass GM. In vitro effects of protease inhibitors on murine natural killer cell activity. Immunology. 1983 Jan;48(1):1-8.
[4] Wang X, Jin X, Xie Z, et al. Benzamidine Conjugation Converts Expelled Potential Active Agents into Antifungals against Drug-Resistant Fungi. J Med Chem. 2023 Oct 12;66(19):13684-13704.
[5] Akers IA, Parsons M, Hill MR, et al. Mast cell tryptase stimulates human lung fibroblast proliferation via protease-activated receptor-2. Am J Physiol Lung Cell Mol Physiol. 2000 Jan;278(1):L193-201.
[6] Wang H, Liu YS, Peng Y, et al. Golgi α-mannosidases regulate cell surface N-glycan type and ectodomain shedding of the transmembrane protease corin. J Biol Chem. 2023 Oct;299(10):105211.
[7] Jia T, Che D, Zheng Y, et al. Mast Cells Initiate Type 2 Inflammation through Tryptase Released by MRGPRX2/MRGPRB2 Activation in Atopic Dermatitis. J Invest Dermatol. 2024 Jan;144(1):53-62.e2.
Benzamidine (hydrochloride)是一种可逆的、竞争性胰蛋白酶样丝氨酸蛋白酶抑制剂。Benzamidine可抑制Tryptase（Ki=20μM）、Trypsin（Ki=21μM）、uPA（Ki=97μM）、Factor Xa（Ki=110μM）、Thrombin（Ki=320μM）和tPA（Ki=750μM）的活性。Benzamidine可用于凝血与纤溶系统、生理酶学及相关药理学研究[1-4]。
在体外，Benzamidine（1-100μM）预处理人胎儿肺成纤维细胞60分钟，随后以人肥大细胞类胰蛋白酶（17.6mU/ml）刺激48小时。Benzamidine抑制类胰蛋白酶诱导的成纤维细胞增殖[5]。Benzamidine（5mM）处理KIF（10μM）和SWA（50μM）孵育的HEK293细胞48小时。Benzamidine促进了细胞的corin表达，并抑制corin自切割[6]。
在体内，Benzamidine（100μM；200μl）灌胃给药于MC903诱导的AD模型小鼠，连续14天。Benzamidine显著减轻了小鼠的炎症表型和炎症浸润[7]。
| Cell experiment [1]: | |
Cell lines | Human fetal lung fibroblasts (HFL1), adult lung parenchymal fibroblasts, adult airway fibroblasts, and adult dermal fibroblasts |
Preparation Method | Fibroblasts were maintained in Dulbecco's modified Eagle's medium (DMEM) containing penicillin (100U/ml), streptomycin (100μg/ml), and newborn calf serum (NCS) at 37°C in a humidified atmosphere of air containing 10% CO₂. Cells were seeded onto 96-well microtiter plates at 10⁴ cells/well and grown to confluence. The medium was replaced with serum-free medium containing BSA (1mg/ml) and holo-transferrin (1μg/ml) for 24 hours. Cells were then treated with tryptase (17mU/ml) that had been preincubated with Benzamidine (1-100μM) for 60 minutes at 37°C. |
Reaction Conditions | 1-100μM; preincubation with tryptase for 60 minutes; cell treatment for 48 hours |
Applications | Benzamidine caused concentration-dependent inhibition of tryptase-induced fibroblast proliferation. Benzamidine inhibited the response to tryptase. Benzamidine inhibited tryptase-induced cleavage of the synthetic peptide substrate tosyl-Gly-Pro-Arg pNA. |
| Animal experiment [2]: | |
Animal models | WT mice with MC903-induced AD model |
Preparation Method | Benzamidine was applied by intragastric administration on WT mice with AD for 14 consecutive days. |
Dosage form | 100μM in 200μl; intragastric administration; 14 consecutive days |
Applications | Benzamidine application resulted in a milder inflammatory phenotype and less inflammatory infiltration than in WT mice treated with MC903 alone. |
References: | |
| Cas No. | 1670-14-0 | SDF | |
| 别名 | 苄脒盐酸盐 | ||
| Canonical SMILES | NC(C1=CC=CC=C1)=N.Cl | ||
| 分子式 | C7H8N2•HCl | 分子量 | 156.6 |
| 溶解度 | DMF: 25 mg/ml,DMSO: 25 mg/ml,Ethanol: 10 mg/ml,PBS (pH 7.2): 3 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 6.3857 mL | 31.9285 mL | 63.857 mL |
| 5 mM | 1.2771 mL | 6.3857 mL | 12.7714 mL |
| 10 mM | 638.6 μL | 3.1928 mL | 6.3857 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % 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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
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