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Tranilast

Tranilast

产品编号 T2690   CAS 53902-12-8
别名: 曲尼司特, MK 341, SB 252218

Tranilast (SB 252218) 是一种抗过敏药物,可抑制炎症细胞释放脂质介质和细胞因子,抑制前列腺素 D2 (PGD2)产生,IC50为 0.1 mM。它拮抗血管紧张素 II 并抑制其在血管平滑肌细胞中的生物学作用,具有抗炎和免疫调节作用。

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
Tranilast Chemical Structure
Tranilast, CAS 53902-12-8
规格 价格/CNY 货期 数量
5 mg ¥ 197 现货
10 mg ¥ 278 现货
25 mg ¥ 428 现货
50 mg ¥ 591 现货
100 mg ¥ 747 现货
200 mg ¥ 1,080 现货
500 mg ¥ 1,850 现货
1 mL * 10 mM (in DMSO) ¥ 213 现货
其他形式的 Tranilast:
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: Tranilast (T2690)
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选择批次  
纯度: 100%
纯度: 99.57%
纯度: 99.56%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Tranilast (SB 252218), an antiallergic drug, suppresses lipid mediator and cytokine release from inflammatory cells, therefore utilized in the treatment of allergic disorders.
靶点活性 PGD2:0.1 mM (IC50)
体外活性 在糖尿病大鼠的心脏中,Tranilast减少磷酸化Smad2, 能够降低心脏纤维化.
体内活性 在瘢痕瘤和增生性瘢痕组织中, Tranilast(3-300 mM)通过抑制抑制转化生长因子(TGF)-β1,从而抑制成纤维细胞的胶原合成,但它不抑制正常的皮肤成纤维细胞。
激酶实验 His-tagged human Mps1Cat encoding amino acids 510-857 is generated. For kinase assays, 500 ng is added to buffer (25 mM Tris-HCl, pH 7.4, 100 mM NaCl, 50 μg/mL BSA, 0.1 mM EGTA, 0.1% β-mercaptoethanol, 10 mM MgCl2, and 0.5 μg/mL myelin basic protein), AZ3146, and 100 μM γ-[32P]ATP (2 μCi/assay). Reactions are incubated at 30°C for 20 min, spotted onto P81 paper, washed in 0.5% phosphoric acid, and immersed in acetone. Phosphate incorporation is determined by scintillation counting. For immunoprecipitation kinase assays, HeLa cells are treated with nocodazole for 14 h, mitotic cells isolated, washed in PBS, and lysed for 30 min in 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 0.5% NP-40, 5 mM EDTA, 5 mM EGTA, 40 mM β-glycerophosphate, 0.2 mM PMSF, 1 mM DTT, 1 mM sodium orthovanadate, 20 mM sodium fluoride, 1 μM okadaic acid, and complete EDTA-free protease inhibitor cocktail. Full-length Mps1 is immunoprecipitated. Purified complexes are washed with lysis buffer containing 100 mM NaCl and assayed as described for the recombinant protein. To quantify 32P incorporation, reactions are stopped with SDS sample buffer and separated by SDS-PAGE followed by phosphorimaging. The plate is analyzed using a phosphorimager using AIDA software. To assess the specificity of AZ3146, a single-point screen is carried using kinase profiling service. 50 kinases are selected and assayed with 1 μM AZ3146[1].
别名 曲尼司特, MK 341, SB 252218
分子量 327.33
分子式 C18H17NO5
CAS No. 53902-12-8

存储

keep away from direct sunlight,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 32.7 mg/mL (100 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.055 mL 15.2751 mL 30.5502 mL 76.3755 mL
5 mM 0.611 mL 3.055 mL 6.11 mL 15.2751 mL
10 mM 0.3055 mL 1.5275 mL 3.055 mL 7.6376 mL
20 mM 0.1528 mL 0.7638 mL 1.5275 mL 3.8188 mL
50 mM 0.0611 mL 0.3055 mL 0.611 mL 1.5275 mL
100 mM 0.0306 mL 0.1528 mL 0.3055 mL 0.7638 mL

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TargetMol Library Books参考文献

1. Suzawa H, et al. Jpn J Pharmacol, 1992, 60(2), 91-96. 2. Suzawa H, et al. Jpn J Pharmacol, 1992, 60(2), 85-90. 3. Miyazawa K, et al. Atherosclerosis, 1995, 118(2), 213-221. 4. Martin J, et al. Cardiovasc Res, 2005, 65(3), 694-701. 5. Shiota N, et al. Circulation, 1999, 99(8), 1084-1090. 6. Huang R, Li S, Tian C, et al. Thermal stress involved in TRPV2 promotes tumorigenesis through the pathway of PI3K/Akt/mTOR in esophageal squamous cell carcinoma[J]. 2020 7. Huang R, Wang F, Yang Y, et al. Recurrent activations of transient receptor potential vanilloid‐1 and vanilloid‐4 promote cellular proliferation and migration in esophageal squamous cell carcinoma cells[J]. FEBS open bio. 2019 Jan 18;9(2):206-225. 8. Liu J, Zhao Z, Wen J, et al. TNF-α differently regulates TRPV2 and TRPV4 channels in human dental pulp cells[J]. International endodontic journal. 2019. 9. Weiqiang H, Longshan Z, Mi Y, et al. Cancer-Associated Fibroblasts Promote the Survival of Irradiated Nasopharyngeal Carcinoma Cells via the NF-κB Pathway[J]. Journal of Experimental & Clinical Cancer Research. 2020

TargetMol Library Books文献引用

1. Huang W, Zhang L, Yang M, et al. Cancer-associated fibroblasts promote the survival of irradiated nasopharyngeal carcinoma cells via the NF-κB pathway. Journal of Experimental & Clinical Cancer Research. 2021, 40(1): 1-14 2. Huang W, Zhang L, Yang M, et al. Cancer-associated fibroblasts promote the survival of irradiated nasopharyngeal carcinoma cells via the NF-κB pathway. Journal of Experimental & Clinical Cancer Research. 2021, 40(1): 1-14 3. Huang R, Li S, Tian C, et al. Thermal stress involved in TRPV2 promotes tumorigenesis through the pathway of PI3K/Akt/mTOR in esophageal squamous cell carcinoma. british journal of cancer. 2022 Nov;127(8):1424-1439. 4. Huang R, Li S, Tian C, et al. Thermal stress involved in TRPV2 promotes tumorigenesis through the pathways of HSP70/27 and PI3K/Akt/mTOR in esophageal squamous cell carcinoma. British Journal of Cancer. 2022: 1-16. 5. Liu J, Zhao Z, Wen J, et al. TNF-α differently regulates TRPV2 and TRPV4 channels in human dental pulp cells. International endodontic journal. 2019 6. Huang R, Wang F, Yang Y, et al. Recurrent activations of transient receptor potential vanilloid‐1 and vanilloid‐4 promote cellular proliferation and migration in esophageal squamous cell carcinoma cells. FEBS Open Bio. 2019 Jan 18;9(2):206-225 7. Amissah O B, Chen W, de Dieu Habimana J, et al.NY-ESO-1-specific T cell receptor-engineered T cells and Tranilast, a TRPV2 antagonist bivalent treatment enhances the killing of esophageal cancer: a dual-targeted cancer therapeutic route.Cancer Cell International.2024, 24(1): 1-18.
Angiotensin II (3-8), human Azilsartan Enalapril PD 123319 Benazeprilat N-Acetyl-Ser-Asp-Lys-Pro MLN-4760 Lisinopril dihydrate

相关化合物库

该产品包含在如下化合物库中:
药物功能重定位化合物库 抑制剂库 GPCR靶点分子库 抗癌临床化合物库 中药单体化合物库 抗癌上市药物库 膜蛋白靶向化合物库 抗癌药物库 已知活性化合物库 免疫/炎症分子化合物库

TargetMol Calculator剂量换算

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TargetMol Calculator 体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Tranilast 53902-12-8 Endocrinology/Hormones GPCR/G Protein Immunology/Inflammation RAAS Prostaglandin Receptor Inhibitor endothelial chemotaxis tube MK341 anti-atopic prostaglandin SB252218 vascular Angiogenesis SB-252218 Angiotensin Receptor MK-341 proliferation inhibit microvascular 曲尼司特 MK 341 SB 252218 factor growth inhibitor

 

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