曲尼司特作用機制 - Medchemexpress - MCE中國

1、Product Data SheetTranilastCat. No.: HY-B0195CAS No.: 53902-12-8分式: CHNO分量: 327.33作靶點: Angiotensin Receptor; Prostaglandin Receptor作通路: GPCR/G Protein儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 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制備儲備液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請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -2

3、0C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 0.5% CMC-Na/saline water2.Solubility: 2 mg/mL (6.11 mM); Preci

4、pitated solution; Need ultrasonic請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.64 mM); Clear solution此案可獲得 2.5 mg/mL (7.64 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。Page 1 of 2 www.

5、MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.64 mM); Suspended solution; Need ultrasonic此案可獲得 2.5 mg/mL (7.64 mM) 的均勻懸濁液，懸濁液可于服和腹腔注射。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。4. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/m

6、L (7.64 mM); Clear solution此案可獲得 2.5 mg/mL (7.64 mM，飽和度未知) 的澄 溶液，此案不適于實驗周 期在半個以上的實驗。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 900 L 油中，混合均勻。5. 請依序添加每種溶劑： 30 % SBE-CDSolubility: 5 mg/mL (15.28 mM); Suspended solution; Need ultrasonicBIOLOGICAL ACTIVITY物活性 Tranilast (MK-341) 種抗變態(tài)反應(yīng)劑。抑制前列腺素 D2 產(chǎn) (PG

7、D2，IC50=0.1 mM)。具有抗炎和免疫調(diào)節(jié)作1 。Tranilast sodium 拮抗管緊張素 II (angiotensin II) 并抑制其在管平滑肌細胞中的物學(xué)作2。IC & Target PGD2 Angiotensin II0.1 mM (IC50)體外研究 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、.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻 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.