WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H561786
CAS#: 942195-55-3
Description: Tegoprazan is a potassium-competitive acid blocker that controls gastric acid secretion and motility. Tegoprazan works by inhibiting the H+/K+ transporter (ATP4A), also known as the gastric proton pump, in the stomach lining. This reduces the secretion of gastric acid. According to a study, tegoprazan has stronger and more reversible gastric acid suppression than traditional PPIs. Another study says that tegoprazan is associated with lower hepatotoxicity than other PPIs. .
Hodoodo Cat#: H561786
Name: Tegoprazan
CAS#: 942195-55-3
Chemical Formula: C20H19F2N3O3
Exact Mass: 387.14
Molecular Weight: 387.380
Elemental Analysis: C, 62.01; H, 4.94; F, 9.81; N, 10.85; O, 12.39
Synonym: Tegoprazan; CJ-12420; CJ 12420; CJ12420; RQ-00000004; RQ00000004; RQ 00000004;
IUPAC/Chemical Name: (S)-4-((5,7-Difluorochroman-4-yl)oxy)-N,N,2-trimethyl-1H-benzo[d]imidazole-6-carboxamide
InChi Key: CLIQCDHNPDMGSL-HNNXBMFYSA-N
InChi Code: InChI=1S/C20H19F2N3O3/c1-10-23-14-6-11(20(26)25(2)3)7-17(19(14)24-10)28-15-4-5-27-16-9-12(21)8-13(22)18(15)16/h6-9,15H,4-5H2,1-3H3,(H,23,24)/t15-/m0/s1
SMILES Code: O=C(C1=CC(O[C@H]2CCOC3=C2C(F)=CC(F)=C3)=C4C(NC(C)=N4)=C1)N(C)C
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: Tegoprazan (CJ-12420) is a fast-acting, oral , potassium-competitive acid blocker (P-CAB). It's used to treat acid-related gastrointestinal diseases , such as peptic ulcers and gastroesophageal reflux disease (GERD).
Biological target: | |
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In vivo activity: |
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
Soluble in DMSO | 0.0 | 100.00 |
The following data is based on the product molecular weight 387.38 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.
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: | |
In vitro protocol: | |
In vivo protocol: |
1: Jeon HK, Kim GH, Cheon YI, Shin SC, Lee BJ. Efficacy of Tegoprazan in Patients with Laryngopharyngeal Reflux Disease: A Preliminary Feasibility Study. J Clin Med. 2023 Sep 22;12(19):6116. doi: 10.3390/jcm12196116. PMID: 37834761; PMCID: PMC10573336.
2: Han GH, Kim SJ, Ko WK, Hong JB, Sheen SH, Cho MJ, Sohn S. Anti-Inflammatory Effects of Tegoprazan in Lipopolysaccharide-Stimulated Bone-Marrow-Derived Macrophages. Int J Mol Sci. 2023 Sep 26;24(19):14589. doi: 10.3390/ijms241914589. PMID: 37834036; PMCID: PMC10572893.
3: Choi HH. Is Tegoprazan-Based Triple Therapy Effective in Regions with High Rates of Clarithromycin Resistance? Gut Liver. 2023 Sep 15;17(5):668-669. doi: 10.5009/gnl230338. PMID: 37712188; PMCID: PMC10502489.
4: Park CH, Park JH, Jung YS. Comparative Efficacy of Tegoprazan vs Esomeprazole/Sodium Bicarbonate for the Treatment of Helicobacter pylori Infection. Clin Transl Gastroenterol. 2023 Nov 1;14(11):e00632. doi: 10.14309/ctg.0000000000000632. PMID: 37561041; PMCID: PMC10684139.
5: Oh M, Lee H, Kim S, Kim B, Song GS, Shin JG, Ghim JL. Evaluation of pharmacokinetic drug-drug interaction between tegoprazan and clarithromycin in healthy subjects. Transl Clin Pharmacol. 2023 Jun;31(2):114-123. doi: 10.12793/tcp.2023.31.e11. Epub 2023 Jun 27. PMID: 37440779; PMCID: PMC10333645.
6: Lee JA, Goak IS, Lee J, Kim B, Moon SJ, Kwak YG, Kim MG. Evaluation of the comparative pharmacokinetic properties of a new orally disintegrating tablet of tegoprazan in healthy Korean subjects. Int J Clin Pharmacol Ther. 2023 Sep;61(9):410-420. doi: 10.5414/CP204378. PMID: 37382330.
7: Kwon YH, Jeon SW, Nam SY, Lee DW, Park JH, Bae HJ. Ten-day tegoprazan-based concomitant therapy as a first-line treatment for Helicobacter pylori eradication. Korean J Intern Med. 2023 Jul;38(4):493-503. doi: 10.3904/kjim.2022.345. Epub 2023 Jun 28. PMID: 37369525; PMCID: PMC10338248.
8: Kim M, Kim B, Lee JH, Kim D, Song GS, Williams SD, Son WC. Carcinogenicity assessment of tegoprazan in Sprague-Dawley (Crl:CD) rats and ICR (Crl:CD1) mice. Regul Toxicol Pharmacol. 2023 Aug;142:105424. doi: 10.1016/j.yrtph.2023.105424. Epub 2023 Jun 7. PMID: 37295487.
9: Park S, Yang E, Kim B, Kwon J, Jang IJ, Lee SH. Pharmacokinetic and pharmacodynamic exploration of various combinations of tegoprazan immediate and delayed-release formulations. Br J Clin Pharmacol. 2023 Sep;89(9):2877-2887. doi: 10.1111/bcp.15784. Epub 2023 Jun 1. PMID: 37170677.
10: Anik AH, Proma FA, Saha P, Sarker S. Tegoprazan as a New Remedy for Gastrointestinal Diseases in Comparison with its Therapeutic Predecessors: A Mini-Review. Curr Drug Res Rev. 2023 Apr 28. doi: 10.2174/2589977515666230428140741. Epub ahead of print. PMID: 37132138.
11: Kim JS, Ko W, Chung JW, Kim TH. Efficacy of tegoprazan-based bismuth quadruple therapy compared with bismuth quadruple therapy for Helicobacter pylori infection: A randomized, double-blind, active-controlled study. Helicobacter. 2023 Jun;28(3):e12977. doi: 10.1111/hel.12977. Epub 2023 Apr 21. PMID: 37083222.
12: Wei Z, Jeong HC, Kim MG, Shin KH. Prediction of the Drug-Drug Interaction Potential between Tegoprazan and Amoxicillin/Clarithromycin Using the Physiologically Based Pharmacokinetic and Pharmacodynamic Model. Pharmaceuticals (Basel). 2023 Feb 26;16(3):360. doi: 10.3390/ph16030360. PMID: 36986460; PMCID: PMC10054914.
13: Guo K, He X, Zhao H, Ma C. Characterisation of degradation products of tegoprazan by LC-MS and GC-MS. J Pharm Biomed Anal. 2023 May 10;228:115323. doi: 10.1016/j.jpba.2023.115323. Epub 2023 Mar 4. PMID: 36921447.
14: Yang E, Ji SC, Jang IJ, Lee S. Evaluation of CYP2C19-Mediated Pharmacokinetic Drug Interaction of Tegoprazan, Compared with Vonoprazan or Esomeprazole. Clin Pharmacokinet. 2023 Apr;62(4):599-608. doi: 10.1007/s40262-023-01228-4. Epub 2023 Mar 10. PMID: 36897544; PMCID: PMC10085907.
15: Kim MG, Im YJ, Lee JH, Kim EY, Yeom SW, Kim JS. Comparison of hepatotoxicity of tegoprazan, a novel potassium-competitive acid blocker, with proton pump inhibitors using real-world data: A nationwide cohort study. Front Med (Lausanne). 2023 Jan 11;9:1076356. doi: 10.3389/fmed.2022.1076356. PMID: 36714137; PMCID: PMC9876560.
16: Ngo LT, Lee J, Yun HY, Chae JW. Development of a Physiologically Based Pharmacokinetic Model for Tegoprazan: Application for the Prediction of Drug- Drug Interactions with CYP3A4 Perpetrators. Pharmaceutics. 2023 Jan 4;15(1):182. doi: 10.3390/pharmaceutics15010182. PMID: 36678810; PMCID: PMC9862396.
17: Kim JS, Seo SI, Kang SH, Lee SK, Kim AR, Park HW, Kim BT, Song GS. Effects of Tegoprazan Versus Esomeprazole on Nighttime Heartburn and Sleep Quality in Gastroesophageal Reflux Disease: A Multicenter Double-blind Randomized Controlled Trial. J Neurogastroenterol Motil. 2023 Jan 30;29(1):58-64. doi: 10.5056/jnm22104. Epub 2022 Dec 30. PMID: 36581325; PMCID: PMC9837551.
18: Jung YS, Kim S, Kim HY, Noh SJ, Park JH, Sohn CI, Park CH. Efficacy and Tolerability of 14-Day Tegoprazan- versus Rabeprazole-Based Triple Therapy for Eradication of Helicobacter pylori: A Real-World Evidence Study. Gut Liver. 2023 Sep 15;17(5):711-721. doi: 10.5009/gnl220218. Epub 2022 Dec 13. PMID: 36510776; PMCID: PMC10502490.
19: Park CH, Song MJ, Jung BW, Park JH, Jung YS. Comparative Efficacy of 14-Day Tegoprazan-Based Triple vs. 10-Day Tegoprazan-Based Concomitant Therapy for Helicobacter pylori Eradication. J Pers Med. 2022 Nov 17;12(11):1918. doi: 10.3390/jpm12111918. PMID: 36422094; PMCID: PMC9695183.
20: Han S, Choi HY, Kim YH, Choi S, Kim S, Nam JY, Kim B, Song GS, Lim HS, Bae KS. Comparison of Pharmacodynamics between Tegoprazan and Dexlansoprazole Regarding Nocturnal Acid Breakthrough: A Randomized Crossover Study. Gut Liver. 2023 Jan 15;17(1):92-99. doi: 10.5009/gnl220050. Epub 2022 Nov 1. PMID: 36317518; PMCID: PMC9840922.