Iopanoic-acid-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIopanoic 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(shù)據(jù)體外實驗 DMSO : 113.3 mg/mL (198.45 mM; Need ultrasonic and warming)M

2、ass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.7515 mL 8.7576 mL 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(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，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Iopanoic acid個 5-Deiodinase 抑制劑，也 種碘造影劑。IC50 & Target 5-Deiodinase 1體外研究The thyrotro

3、pin-releasing-hormone (TRH)-induced thyrotropin (TSH) release from the pituitary fragments isinhibited by 3,5,3-triiodothyronin (T3) (10-7 M), by triiodothyroacetic acid (10-7 to 10-7 M), and by highconcentrations of iodide (10-4 or 10-5 M). Iopanoic acid has no significant effect at the concentrati

4、ons tested1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE2.體內(nèi)研究 Iopanoic acid (IOP) administration to pregnant rats during days 18 and 19 postconception does not modifylitter size (controls: 11.80.5 fetusesldam, Iopanoic acid-treated: 11.60.6 fetusesldam) or body weight at day20 (controls: 3.270.1

5、2 g, Iopanoic acid-treated: 3.420.20 g). Iopanoic acid treatment produces a significantblockage 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

6、brainand liver nuclei of Iopanoic acid-treated fetuses when compare with control fetuses at day 20 (p3 content andplasma T3 concentration. Iopanoic acid inhibition of IBAT 5D activity in fetuses at term is as effective as atday 20 1.PROTOCOLCell Assay 2 Rat pituitary fragments are superfused by Medi

7、um-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) 10-7M, triiodothyroacetic acid (TRIAC) (stock solution 10-4 M in 20% methanol, final concentrations 10-8 to 10-6M), Iopanoic acid (

8、stock solution 10-3 M in 0.2 M NaOH, final concentrations 10-7 to 10-5 M), or potassiumiodide 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. They are for reference only.Animal Wis

9、tar rats initially weighing 180 to 200 g are used. The administration of Iopanoic acid (IOP) is started atAdministration 1 day 18 of gestation. Pregnant rats are injected subcutaneously with 10 mg of Iopanoic acid every 12 h, fromday 18 of gestation to 12 h before they are killed on the morning of d

10、ay 20 or 22 of gestation. Control animalsreceive the vehicle solution with identical timing. Iopanoic acid effectiveness in decreasing interscapularbrown adipose tissue (IBAT) nuclear 3,5,3-triiodothyronin (T3) is assessed by Iopanoic acid (IOP)administration to adult male rats (220 to 250 g body we

11、ight) following the same dose and time schedule as inpregnant dams during two days. Caesarean sections are performed at 18 (only untreated animals), 20 and22 days of gestation. Fetuses are killed by decapitation, and IBAT, brain, and liver are removed. Tissuesamples are immediately frozen in liquid

12、nitrogen with the exception of brown fat from several 22 day-oldfetuses, which is directly homogenized in 0.25 M sucrose for mitochondria isolation 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Tuca A, et al. Inhibition of iodothyronine

13、 5-deiodinase by iopanoic acid does not block nuclear T3 accumulation during rat fetaldevelopment. Pediatr Res. 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 thyrotropin release from superfused rat pituitary fragments. Acta Endocrinol (Copenh). 1991 Oct;125(4):427-34.Mc