1、Product Data SheetIopanoic acidCat. No.: HY-B1664CAS No.: 96-83-3分式: CHINO分量: 570.93作靶點: Others作通路: Others儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 100 mg/mL (175.15 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 1.7515 mL 8.7576 mL

2、17.5153 mL5 mM 0.3503 mL 1.7515 mL 3.5031 mL10 mM 0.1752 mL 0.8758 mL 1.7515 mL請根據產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，避免反復凍融造成的產品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內使，-20C 儲存時，請在 1 個內使。體內實驗請根據您的實驗動物和給藥式選擇適當的溶解案。以下溶解案都請先按照 In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄 的儲備液可以根據儲存條

3、件，適當保存；體內實驗的作液，建議您現現配，當天使； 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沉淀、析出現象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.38 mM); Clear solution此案可獲得 2.5 mg/mL (4.38 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5

4、0 L Tween-80，混合均勻；然后繼續加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (4.38 mM); Clear solution此案可獲得 2.5 mg/mL (4.38 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合3. 請依序添加每種溶劑： 10% DMSO 90% c

5、orn oilSolubility: 2.5 mg/mL (4.38 mM); Clear solution此案可獲得 2.5 mg/mL (4.38 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。BIOLOGICAL ACTIVITY物活性 Iopanoic acid個 5-Deiodinase 抑制劑，也 種碘造影劑。IC & Target 5-Deiodinase1體外研究 The thyrotropin-releasing-hormone (TR

6、H)-induced thyrotropin (TSH) release from the pituitary fragments is inhibitedby 3,5,3-triiodothyronin (T3) (10-7 M), by triiodothyroacetic acid (10-7 to 10-7 M), and by high concentrations ofiodide (10-4 or 10-5 M). Iopanoic acid has no significant effect at the concentrations tested2.體內研究 Iopanoic

7、 acid (IOP) administration to pregnant rats during days 18 and 19 postconception does not modify litter size(controls: 11.80.5 fetusesldam, Iopanoic acid-treated: 11.60.6 fetusesldam) or body weight at day 20 (controls:3.270.12 g, Iopanoic acid-treated: 3.420.20 g). Iopanoic acid treatment produces

8、a significant blockage of 5-Deiodinase (5D) activity in interscapular brown adipose tissue (IBAT) and brain; in contrast, liver 5D is not modified.3,5,3-triiodothyronin (T3) content is similar in IBAT and slightly increased in brain and liver nuclei of Iopanoic acid-treated fetuses when compare with

9、 control fetuses at day 20 (p0.05). However, when administered to adult rats,Iopanoic acid produces a significant reduction in IBAT nuclear T3 content and plasma T3 concentration. Iopanoic acidinhibition of IBAT 5D activity in fetuses at term is as effective as at day 201.PROTOCOLCell Assay 2 Rat pi

10、tuitary fragments are superfused by Medium-199. After a 90 min equilibration period, the superfusion iscontinued for 135 min with or without inclusion into the superfusion medium of 3,5,3-triiodothyronin (T3) 10-7 M,triiodothyroacetic acid (TRIAC) (stock solution 10-4 M in 20% methanol, final concen

11、trations 10-8 to 10-6 M), Iopanoicacid (stock solution 10-3 M in 0.2 M NaOH, final concentrations 10-7 to 10-5 M), or potassium iodide 10-7 to 10-4 M.The superfusion is followed by a 6-min pulse of thyrotropin-releasing-hormone (TRH)2.MCE has not independently confirmed the accuracy of these methods

12、. They are for reference only.Animal Wistar rats initially weighing 180 to 200 g are used. The administration of Iopanoic acid (IOP) is started at day 18 ofAdministration 1 gestation. Pregnant rats are injected subcutaneously with 10 mg of Iopanoic acid every 12 h, from day 18 ofgestation to 12 h be

13、fore they are killed on the morning of day 20 or 22 of gestation. Control animals receive thevehicle solution with identical timing. Iopanoic acid effectiveness in decreasing interscapular brown adipose tissue(IBAT) nuclear 3,5,3-triiodothyronin (T3) is assessed by Iopanoic acid (IOP) administration

14、 to adult male rats (220 to250 g body weight) following the same dose and time schedule as in pregnant dams during two days. Caesareansections are performed at 18 (only untreated animals), 20 and 22 days of gestation. Fetuses are killed by decapitation,and IBAT, brain, and liver are removed. Tissue

15、samples are immediately frozen in liquid nitrogen with the exception ofbrown fat from several 22 day-old fetuses, which is directly homogenized in 0.25 M sucrose for mitochondriaisolation1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3 www.

16、MedChemEREFERENCES1. Tuca A, et al. Inhibition of iodothyronine 5-deiodinase by iopanoic acid does not block nuclear T3 accumulation during rat fetal development. PediatrRes. 1994 Jan;35(1):91-5.2. Szabolcs I, et al. Effects of triiodothyronine, triiodothyroacetic acid, iopanoic acid and iodide on the thyrotropin-releasing hormone-induced thyrotropinrelease from superfused rat pituitary fragments. Acta Endocrinol (Copenh