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MedKoo Cat#: 463871 | Name: Methimazole-d3
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Methimazole-d3 is intended for use as an internal standard for the quantification of methimazole by GC- or LC-MS. Methimazole is an inhibitor of thyroid hormone synthesis. It is a substrate for thyroid peroxidase that traps oxidized iodide, preventing its use by thyroglobulin for thyroid hormone synthesis. Methimazole (0.4 mg/kg) inhibits the absorption of radiolabeled iodide by the thyroid gland in rats by 80.9%. It reduces the incidence of lymphocytic thyroiditis in the insulin-dependent type 1 diabetic BB/W rat.4 Methimazole has been used to induce hypothyroidism in mice.5,6 Formulations containing methimazole have been used in the treatment of hyperthyroidism.

Chemical Structure

Methimazole-d3
Methimazole-d3
CAS#1160932-07-9

Theoretical Analysis

MedKoo Cat#: 463871

Name: Methimazole-d3

CAS#: 1160932-07-9

Chemical Formula: C4H3D3N2S

Exact Mass: 117.0440

Molecular Weight: 117.18

Elemental Analysis: C, 41.00; H, 7.74; N, 23.91; S, 27.36

Price and Availability

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1mg USD 450.00 2 Weeks
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Synonym
Methimazole-d3; Methimazole d3;
IUPAC/Chemical Name
1-(methyl-d3)-1,3-dihydro-2H-imidazole-2-thione
InChi Key
PMRYVIKBURPHAH-FIBGUPNXSA-N
InChi Code
InChI=1S/C4H6N2S/c1-6-3-2-5-4(6)7/h2-3H,1H3,(H,5,7)/i1D3
SMILES Code
S=C1NC=CN1C([2H])([2H])[2H]
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Methimazole-d3 is intended for use as an internal standard for the quantification of methimazole by GC- or LC-MS. Methimazole is an inhibitor of thyroid hormone synthesis.
In vitro activity:
This study attempted to investigate the cytotoxic mechanism(s) of methimazole toward isolated rat hepatocytes. Methimazole-induced cytotoxicity was accompanied by collapse in MMP, increase in ROS formation, and LPO. Further, methimazole caused reduction in GSH reservoirs, and the cytotoxic effect of the drug was much more severe in GSH-depleted cells. Reference: Drug Chem Toxicol. 2013 Oct;36(4):403-11. https://pubmed.ncbi.nlm.nih.gov/23256569/
In vivo activity:
The aim of the study was to determine effects of long-term oral methimazole treatment in male Wistar rats on biochemical bone metabolism markers, as well as morphological, geometric, densitometric and mechanical properties of femur and tibia. Methimazole treatment significantly decreased serum OC concentration by 21% (P=0.02) and increased CTX-I concentration by 17% (P=0.06). Methimazole decreased morphological, geometric and densitometric parameters of femur and tibia in rats. Reference: Biomed Pharmacother. 2017 Oct;94:124-128. https://pubmed.ncbi.nlm.nih.gov/28759749/

Preparing Stock Solutions

The following data is based on the product molecular weight 117.18 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Heidari R, Babaei H, Eghbal M. Mechanisms of methimazole cytotoxicity in isolated rat hepatocytes. Drug Chem Toxicol. 2013 Oct;36(4):403-11. doi: 10.3109/01480545.2012.749272. Epub 2012 Dec 21. PMID: 23256569. 2. Crescioli C, Cosmi L, Borgogni E, Santarlasci V, Gelmini S, Sottili M, Sarchielli E, Mazzinghi B, Francalanci M, Pezzatini A, Perigli G, Vannelli GB, Annunziato F, Serio M. Methimazole inhibits CXC chemokine ligand 10 secretion in human thyrocytes. J Endocrinol. 2007 Oct;195(1):145-55. doi: 10.1677/JOE-07-0240. PMID: 17911406. 3. Tatara MR, Gołyński M, Radzki RP, Bieńko M, Krupski W. Effects of long-term oral administration of methimazole on femur and tibia properties in male Wistar rats. Biomed Pharmacother. 2017 Oct;94:124-128. doi: 10.1016/j.biopha.2017.07.107. Epub 2017 Jul 28. PMID: 28759749. 4. Nace CG, Genter MB, Sayre LM, Crofton KM. Effect of methimazole, an FMO substrate and competitive inhibitor, on the neurotoxicity of 3,3'-iminodipropionitrile in male rats. Fundam Appl Toxicol. 1997 Jun;37(2):131-40. doi: 10.1006/faat.1997.2307. PMID: 9242586.
In vitro protocol:
1. Heidari R, Babaei H, Eghbal M. Mechanisms of methimazole cytotoxicity in isolated rat hepatocytes. Drug Chem Toxicol. 2013 Oct;36(4):403-11. doi: 10.3109/01480545.2012.749272. Epub 2012 Dec 21. PMID: 23256569. 2. Crescioli C, Cosmi L, Borgogni E, Santarlasci V, Gelmini S, Sottili M, Sarchielli E, Mazzinghi B, Francalanci M, Pezzatini A, Perigli G, Vannelli GB, Annunziato F, Serio M. Methimazole inhibits CXC chemokine ligand 10 secretion in human thyrocytes. J Endocrinol. 2007 Oct;195(1):145-55. doi: 10.1677/JOE-07-0240. PMID: 17911406.
In vivo protocol:
1. Tatara MR, Gołyński M, Radzki RP, Bieńko M, Krupski W. Effects of long-term oral administration of methimazole on femur and tibia properties in male Wistar rats. Biomed Pharmacother. 2017 Oct;94:124-128. doi: 10.1016/j.biopha.2017.07.107. Epub 2017 Jul 28. PMID: 28759749. 2. Nace CG, Genter MB, Sayre LM, Crofton KM. Effect of methimazole, an FMO substrate and competitive inhibitor, on the neurotoxicity of 3,3'-iminodipropionitrile in male rats. Fundam Appl Toxicol. 1997 Jun;37(2):131-40. doi: 10.1006/faat.1997.2307. PMID: 9242586.
1: Haddaden M, Hanna A, Odish F, Husami S, Imam Z, Tahhan M. Cholestatic Hepatitis in Graves' Disease: A Diagnostic Challenge. ACG Case Rep J. 2021 Jan 14;8(1):e00526. doi: 10.14309/crj.0000000000000526. PMID: 33490298; PMCID: PMC7810504. 2: Chen J, Wang W, Guo Z, Huang S, Lei H, Zang P, Lu B, Shao J, Gu P. Associations between gut microbiota and thyroidal function status in Chinese patients with Graves' disease. J Endocrinol Invest. 2021 Jan 22. doi: 10.1007/s40618-021-01507-6. Epub ahead of print. PMID: 33481211. 3: Kwak JJ, Altoos R, Jensen A, Altoos B, McDermott MT. Increased Risk of Radioiodine Treatment Failure Associated with Graves Disease Refractory to Methimazole. Endocr Pract. 2020 Nov;26(11):1312-1319. doi: 10.4158/EP-2020-0164. PMID: 33471662. 4: Mizokami T, Hamada K, Maruta T, Higashi K, Tajiri J. Long-Term Outcomes of Radioiodine Therapy for Juvenile Graves Disease with Emphasis on Subsequently Detected Thyroid Nodules: A Single Institution Experience from Japan. Endocr Pract. 2020 Jul;26(7):729-737. doi: 10.4158/EP-2019-0468. Epub 2020 Nov 24. PMID: 33471641. 5: Azizi F, Abdi H, Amouzegar A. Control of Graves' hyperthyroidism with very long-term methimazole treatment: a clinical trial. BMC Endocr Disord. 2021 Jan 14;21(1):16. doi: 10.1186/s12902-020-00670-w. PMID: 33446181; PMCID: PMC7807686. 6: Kayaş L, Çamtosun E, Akıncı A, Bircan R. TSHRV656F Activating Variant of the Thyroid Stimulating Hormone Receptor Gene in Neonatal Onset Hyperthyroidism: A Case Review. J Clin Res Pediatr Endocrinol. 2021 Jan 14. doi: 10.4274/jcrpe.galenos.2020.2020.0229. Epub ahead of print. PMID: 33443352. 7: Brown J, Cham MD, Huang GS. Storm and STEMI: a case report of unexpected cardiac complications of thyrotoxicosis. Eur Heart J Case Rep. 2020 Nov 12;4(6):1-5. doi: 10.1093/ehjcr/ytaa414. PMID: 33442653; PMCID: PMC7793194. 8: Molinaro G, De Vecchis R, Badolati E, Giannattasio R. Thyrotoxic dilated cardiomyopathy: personal experience and case collection from the literature. Endocrinol Diabetes Metab Case Rep. 2020 Dec 24;2020:EDM200068. doi: 10.1530/EDM-20-0068. Epub ahead of print. PMID: 33434150. 9: de Souza Cardoso J, Baldissarelli J, Reichert KP, Teixeira F, Pereira Soares MS, Chitolina Schetinger MR, Morsch VM, Farias Martins Filho AO, Duarte Junior HR, Ribeiro Coriolano FH, Spanevello RM, Stefanello FM, Tavares RG. Neuroprotection elicited by resveratrol in a rat model of hypothyroidism: possible involvement of cholinergic signaling and redox status. Mol Cell Endocrinol. 2021 Jan 6:111157. doi: 10.1016/j.mce.2021.111157. Epub ahead of print. PMID: 33421531. 10: Shin JH, Seo GH, Oh SH, Chung WY, Kim HY, Kim YM, Bae MH, Park KH, Kwak MJ. An A627V-activating mutation in the thyroid-stimulating hormone receptor gene in familial nonautoimmune hyperthyroidism. Ann Pediatr Endocrinol Metab. 2020 Dec;25(4):282-286. doi: 10.6065/apem.2040076.038. Epub 2020 Dec 31. PMID: 33401884; PMCID: PMC7788338. 11: Sun J, Zhao F, Lin B, Feng J, Wu X, Liu Y, Zhao L, Zhu B, Wei Y. Gut Microbiota Participates in Antithyroid Drug Induced Liver Injury Through the Lipopolysaccharide Related Signaling Pathway. Front Pharmacol. 2020 Dec 17;11:598170. doi: 10.3389/fphar.2020.598170. PMID: 33390986; PMCID: PMC7774100. 12: Giuliani C, Bucci I, Napolitano G. Phenylmethimazole is a candidate drug for the treatment of severe forms of coronavirus disease 2019 (COVID-19) as well as other virus-induced "cytokines storm". Med Hypotheses. 2021 Jan;146:110473. doi: 10.1016/j.mehy.2020.110473. Epub 2020 Dec 24. PMID: 33385879; PMCID: PMC7759336. 13: van Moorsel D, Tummers-de Lind van Wijngaarden RF. An uncommon side effect of thiamazole treatment in Graves' disease. Neth J Med. 2020 Dec;78(6):389-391. PMID: 33380538. 14: Thewjitcharoen Y, Karndumri K, Chatchomchuan W, Porramatikul S, Krittiyawong S, Wanothayaroj E, Butadej S, Nakasatien S, Rajatanavin R, Himathongkam T. Serum T3 Level and Duration of Minimum Maintenance Dose Therapy Predict Relapse n Methimazole-Treated Graves Disease. J Endocr Soc. 2020 Nov 5;5(1):bvaa170. doi: 10.1210/jendso/bvaa170. PMID: 33305160; PMCID: PMC7716657. 15: Picot C, Grenet G, Cucherat M, Cottin J. Pattern of malformations after methimazole or propylthiouracil exposure in early pregnancy: a meta-analytic approach. Reprod Toxicol. 2020 Oct;97:6. doi: 10.1016/j.reprotox.2020.04.012. PMID: 33353711. 16: Lee SY, Pearce EN. Testing, Monitoring, and Treatment of Thyroid Dysfunction in Pregnancy. J Clin Endocrinol Metab. 2020 Dec 22:dgaa945. doi: 10.1210/clinem/dgaa945. Epub ahead of print. PMID: 33349844. 17: Beernaert L, Vanderhulst J. Antithyroid Drug-Induced Lupus Erythematosus and Immunoglobulin A Deficiency. Am J Case Rep. 2020 Dec 22;21:e927929. doi: 10.12659/AJCR.927929. PMID: 33349625; PMCID: PMC7767573. 18: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006–. Carbimazole. 2020 Dec 21. PMID: 30000818. 19: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006–. Propylthiouracil. 2020 Dec 21. PMID: 30000143. 20: Drugs and Lactation Database (LactMed) [Internet]. Bethesda (MD): National Library of Medicine (US); 2006–. Methimazole. 2020 Dec 21. PMID: 30000083.