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Propylthiouracil Peroxidases inhibitor

Cat.No.S1988

Propylthiouracil (NSC 6498, NSC 70461) is a thyroperoxidase and 5'-deiodinase inhibitor, used to treat hyperthyroidism.
Propylthiouracil Peroxidases inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 170.23

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Quality Control

Batch: S198801 DMSO]80 mg/mL]false]Ethanol]19 mg/mL]false]Water]Insoluble]false Purity: 99.46%
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99.46

Solubility

In vitro
Batch:

DMSO : 80 mg/mL (469.95 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 19 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 170.23 Formula

C7H10N2OS

Storage (From the date of receipt)
CAS No. 51-52-5 Download SDF Storage of Stock Solutions

Synonyms NSC 6498, NSC 70461 Smiles CCCC1=CC(=O)NC(=S)N1

Mechanism of Action

Targets/IC50/Ki
thyroperoxidase
5'-deiodinase
In vivo
Propylthiouracil-induced hypothyroidism reduces oxidative damage in the lung, hepatic, renal and ileal tissues probably due to hypometabolism in rats, which is associated with decreased production of reactive oxygen metabolites and enhancement of antioxidant mechanisms. This compound-induced congenital hypothyroidism upregulates vimentin phosphorylation and depletes antioxidant defenses in immature rat testis. It results in lesser concentrations of thyroxine (T4) and triiodothyronine (T3), greater concentrations of follicle stimulating hormone (FSH) and luteinizing hormone (LH) peptides, and increase in steroidogenic gene expression after 12 hours and 48 hours in zebrafish. This compound-induced hypothyroidism is associated with increased tolerance of the isolated rat heart toischaemia-reperfusion. It dramatically reduces thyroid hormones on PND21 and produced deficits in body weight that persisted to adulthood in developing rats. This compound inhibits both the synthesis of thyroid hormones in the thyroid gland and the conversion of T4 to its active form, T3. This treatment significantly increases circulating TSH at both P3 and P7. This exposure of adult rats, at a dose inducing modest reductions in circulating T4 concentrations and no significant effect on brain BDNF, significantly alteres the thyroid hormones and hippocampal BDNF levels in the offspring at 3 and 7 d after birth.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/12967335/
  • [5] https://pubmed.ncbi.nlm.nih.gov/14519490/
  • [6] https://pubmed.ncbi.nlm.nih.gov/22253429/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02390180 Completed
Taste Qualities|Primary Tastes
Purdue University
October 2014 --
NCT01097915 Completed
Dysgeusia
University of Cagliari
October 2009 --
NCT00570466 Completed
Type 2 Diabetes
National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Baylor College of Medicine
January 2008 Not Applicable

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