曲尼司特作用机制 - Medchemexpress - MCE中国

1、Product Data SheetTranilastCat. No.: HY-B0195CAS No.: 53902-12-8分式: CHNO分量: 327.33作靶点: Angiotensin Receptor; Prostaglandin Receptor作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (152.75 mM; Need ultrasonic)H2O : 10 mg/mL (30.55 mM;

2、ultrasonic and adjust pH to 12 with NaOH)H2O : 0.1 mg/mL (insoluble)SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 3.0550 mL 15.2751 mL 30.5502 mL5 mM 0.6110 mL 3.0550 mL 6.1100 mL10 mM 0.3055 mL 1.5275 mL 3.0550 mL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；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -2

3、0C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 0.5% CMC-Na/saline water2.Solubility: 2 mg/mL (6.11 mM); Preci

4、pitated solution; Need ultrasonic请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.64 mM); Clear solution此案可获得 2.5 mg/mL (7.64 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。Page 1 of 2 www.

5、MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.64 mM); Suspended solution; Need ultrasonic此案可获得 2.5 mg/mL (7.64 mM) 的均匀悬浊液，悬浊液可于服和腹腔注射。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 20% 的 SBE-CD 理盐溶液中，混合均匀。4. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/m

6、L (7.64 mM); Clear solution此案可获得 2.5 mg/mL (7.64 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。5. 请依序添加每种溶剂： 30 % SBE-CDSolubility: 5 mg/mL (15.28 mM); Suspended solution; Need ultrasonicBIOLOGICAL ACTIVITY物活性 Tranilast (MK-341) 种抗变态反应剂。抑制前列腺素 D2 产 (PG

7、D2，IC50=0.1 mM)。具有抗炎和免疫调节作1 。Tranilast sodium 拮抗管紧张素 II (angiotensin II) 并抑制其在管平滑肌细胞中的物学作2。IC & Target PGD2 Angiotensin II0.1 mM (IC50)体外研究 Tranilast exhibits significant immunomodulatory activity inhibiting Endotoxin-induced prostaglandin E2 (PGE2; IC50=1-20 M), thromboxane B2 (IC50=10-50 M), (TGF-

8、1; IC50=100-200 M), and IL-8 (IC50=100 M) formation.A23187-induced monocyte leukotriene C4 or PGE2 formation is inhibited by Tranilast at IC50s of 10-40 M and 2-20 M, respectively3.Tranilast (10-200 M) exhibits the anti-proliferative effect in a dose-dependent manner in both MCF-7 and MDA-MB-231 cel

9、l lines. Tranilast also (10-200M) enhances the anti-tumor effects of Tamoxifen (1-20 M) on human breastcancer cells in vitro4.Tranilast (12.5, 25, 50, 100 g/mL; 72 hours) inhibits proliferation of HDMECs5.Cell Proliferation Assay4Cell Line: MCF-7 and MDA-MB-231 cellsConcentration: 10, 20, 50, 100, a

10、nd 200 MIncubation Time: 48 hoursResult: Anti-proliferative effect in a dose-dependent manner in both cell lines.Cell Viability Assay5Cell Line: Human dermal microvascular endothelial cells (HDMECs)Concentration: 12.5, 25, 50, 100 g/mLIncubation Time: 72 hoursResult: IC50 value was 44.3 g/mL (136 M)

11、.体内研究Tranilast (300 mg/kg; administered orally twice a day for 3 days) dose-dependently suppresses angiogenesis in mice5.Page 2 of 3 www.MedChemEAnimal Model: Nine-week-old male C57BL/6 mice5Dosage: 300 mg/kgAdministration: Administered orally twice a day for 3 daysResult: Suppressed the VEGF-induce

12、d angiogenesis in matrigel; 58% of significantsuppression was observed at a dose of 300 mg/kg.The ED50 value and 95% confidence limits were 165 mg/kg and 162169 mg/kg,respectively.户使本产品发表的科研献 Pharmacol Res. 2017 Nov;125(Pt B):150-160.See more customer validations on HYPERLINK www.MedChemE www.MedChe

13、mEREFERENCES1. K Ikai , et al. Inhibitory Effect of Tranilast on Prostaglandin D Synthetase. Biochem Pharmacol. 1989 Aug 15;38(16):2673-6.2. Sara Darakhshan, et al. Tranilast Enhances the Anti-Tumor Effects of Tamoxifen on Human Breast Cancer Cells in Vitro. J Biomed Sci. 2013 Oct21;20(1):76.3. E A

14、Capper, et al. Modulation of Human Monocyte Activities by Tranilast, SB 252218, a Compound Demonstrating Efficacy in Restenosis. J Pharmacol ExpTher. 2000 Dec;295(3):1061-9.4. M Isaji , et al. Tranilast Inhibits the Proliferation, Chemotaxis and Tube Formation of Human Microvascular Endothelial Cells in Vitro and Angiogenesis inVivo. Br J Pharmacol. 1997 Nov;122(6):1061-6.5. K Miyazawa , et al. Tranilast Antagonizes Angiotensin II and Inhibits Its Biological Effects in Vascular Smooth Muscle Cells. Atherosclerosis. 1996 Apr5;121(2):167-73.