WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H540120
CAS#: 84611-23-4
Description: Erdosteine is a thiol derivative and antioxidant used to treat bronchitis and COPD. It inhibits H2O2-induced oxidative stress and DNA damage, scavenges free radicals, and decreases levels of leukotrienes.
Hodoodo Cat#: H540120
Name: Erdosteine
CAS#: 84611-23-4
Chemical Formula: C8H11NO4S2
Exact Mass: 249.01
Molecular Weight: 249.290
Elemental Analysis: C, 38.54; H, 4.45; N, 5.62; O, 25.67; S, 25.72
Synonym: Erdosteine; PV 144; PV144; PV-144; RV 144; RV144; RV-144
IUPAC/Chemical Name: 2-((2-oxo-2-((2-oxotetrahydrothiophen-3-yl)amino)ethyl)thio)acetic acid
InChi Key: QGFORSXNKQLDNO-UHFFFAOYSA-N
InChi Code: InChI=1S/C8H11NO4S2/c10-6(3-14-4-7(11)12)9-5-1-2-15-8(5)13/h5H,1-4H2,(H,9,10)(H,11,12)
SMILES Code: O=C(O)CSCC(NC(CCS1)C1=O)=O
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:
| Biological target: | Erdosteine inhibits lipopolysaccharide (LPS)-induced NF-κB activation. |
| In vitro activity: | Cell viability, pro-inflammatory cytokines and the degradation of ECM biomarkers were tested to determine the effects of ER (erdosteine) at 10, 20, and 40 μM doses on IL-1β-induced rat chondrocytes for 24 h in vitro. In vivo, intra-articular injections of 50 μl of 100 mg/ml ER twice a week for 8 weeks. The results showed ER significantly suppressed the expressions of IL-1β-induced the production of inflammatory factors in a dose-dependent pattern (4.30-fold decrease in COX-2, p < 0.05; 4.77-fold decrease in iNOS, p < 0.05 at 40 μM in protein levels). Reference: Eur J Pharmacol. 2020 Apr 15;873:172925. https://pubmed.ncbi.nlm.nih.gov/31958453/ |
| In vivo activity: | Erdosteine at 80 mg/kg reversed the deleterious effects of ISO and normalized myocardium. Erdosteine showed anti-inflammatory, antiapoptotic, and antioxidant activities through inhibition of MAPK and Nrf-2/HO-1 pathways. To conclude, erdosteine was found protective in ISO-induced myocardial necrosis through MAPK and Nrf-2/HO-1 pathway. Reference: J Biochem Mol Toxicol. 2020 Dec;34(12):e22590. https://pubmed.ncbi.nlm.nih.gov/33210414/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.3 | 173.81 | |
| DMSO:PBS (pH 7.2) (1:5) | 0.2 | 0.64 | |
| DMF | 25.0 | 100.28 | |
| Ethanol | 10.0 | 40.11 | |
| Water | 6.7 | 26.76 |
The following data is based on the product molecular weight 249.29 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: | 1. Xi Y, Huang X, Tan G, Chu X, Zhang R, Ma X, Ni B, You H. Protective effects of Erdosteine on interleukin-1β-stimulated inflammation via inhibiting the activation of MAPK, NF-κB, and Wnt/β-catenin signaling pathways in rat osteoarthritis. Eur J Pharmacol. 2020 Apr 15;873:172925. doi: 10.1016/j.ejphar.2020.172925. Epub 2020 Jan 17. PMID: 31958453. 2. Kim SJ, Park C, Lee JN, Lim H, Hong GY, Moon SK, Lim DJ, Choe SK, Park R. Erdosteine protects HEI-OC1 auditory cells from cisplatin toxicity through suppression of inflammatory cytokines and induction of Nrf2 target proteins. Toxicol Appl Pharmacol. 2015 Oct 15;288(2):192-202. doi: 10.1016/j.taap.2015.07.014. Epub 2015 Jul 18. PMID: 26193055. 3. Mutneja E, Verma VK, Malik S, Sahu AK, Ray R, Bhatia J, Arya DS. Erdosteine salvages cardiac necrosis: Novel effect through modulation of MAPK and Nrf-2/HO-1 pathway. J Biochem Mol Toxicol. 2020 Dec;34(12):e22590. doi: 10.1002/jbt.22590. Epub 2020 Jul 30. PMID: 33210414. 4. Dobrakowski M, Machoń-Grecka A, Nowak P, Szczęsny P, Maciejczyk M, Kasperczyk A, Pryzwan T, Kasperczyk S. The influence of erdosteine administration on lead-induced oxidative stress in rat muscle. Drug Chem Toxicol. 2019 Sep 10:1-5. doi: 10.1080/01480545.2019.1659810. Epub ahead of print. PMID: 31502475. |
| In vitro protocol: | 1. Xi Y, Huang X, Tan G, Chu X, Zhang R, Ma X, Ni B, You H. Protective effects of Erdosteine on interleukin-1β-stimulated inflammation via inhibiting the activation of MAPK, NF-κB, and Wnt/β-catenin signaling pathways in rat osteoarthritis. Eur J Pharmacol. 2020 Apr 15;873:172925. doi: 10.1016/j.ejphar.2020.172925. Epub 2020 Jan 17. PMID: 31958453. 2. Kim SJ, Park C, Lee JN, Lim H, Hong GY, Moon SK, Lim DJ, Choe SK, Park R. Erdosteine protects HEI-OC1 auditory cells from cisplatin toxicity through suppression of inflammatory cytokines and induction of Nrf2 target proteins. Toxicol Appl Pharmacol. 2015 Oct 15;288(2):192-202. doi: 10.1016/j.taap.2015.07.014. Epub 2015 Jul 18. PMID: 26193055. |
| In vivo protocol: | 1. Mutneja E, Verma VK, Malik S, Sahu AK, Ray R, Bhatia J, Arya DS. Erdosteine salvages cardiac necrosis: Novel effect through modulation of MAPK and Nrf-2/HO-1 pathway. J Biochem Mol Toxicol. 2020 Dec;34(12):e22590. doi: 10.1002/jbt.22590. Epub 2020 Jul 30. PMID: 33210414. 2. Dobrakowski M, Machoń-Grecka A, Nowak P, Szczęsny P, Maciejczyk M, Kasperczyk A, Pryzwan T, Kasperczyk S. The influence of erdosteine administration on lead-induced oxidative stress in rat muscle. Drug Chem Toxicol. 2019 Sep 10:1-5. doi: 10.1080/01480545.2019.1659810. Epub ahead of print. PMID: 31502475. |
1: Kim SJ, Park C, Lee JN, Lim H, Hong GY, Moon SK, Lim DJ, Choe SK, Park R. Erdosteine protects HEI-OC1 auditory cells from cisplatin toxicity through suppression of inflammatory cytokines and induction of Nrf2 target proteins. Toxicol Appl Pharmacol. 2015 Oct 15;288(2):192-202. doi: 10.1016/j.taap.2015.07.014. Epub 2015 Jul 18. PubMed PMID: 26193055.
2: Dal Negro RW, Visconti M, Turco P. Efficacy of erdosteine 900 versus 600 mg/day in reducing oxidative stress in patients with COPD exacerbations: Results of a double blind, placebo-controlled trial. Pulm Pharmacol Ther. 2015 Aug;33:47-51. doi: 10.1016/j.pupt.2015.06.004. Epub 2015 Jun 23. PubMed PMID: 26116425.
3: Dokuyucu R, Karateke A, Gokce H, Kurt RK, Ozcan O, Ozturk S, Tas ZA, Karateke F, Duru M. Antioxidant effect of erdosteine and lipoic acid in ovarian ischemia-reperfusion injury. Eur J Obstet Gynecol Reprod Biol. 2014 Dec;183:23-7. doi: 10.1016/j.ejogrb.2014.10.018. Epub 2014 Oct 24. PubMed PMID: 25461347.
4: Park JS, Park MY, Cho YJ, Lee JH, Yoo CG, Lee CT, Lee SM. Anti-inflammatory Effect of Erdosteine in Lipopolysaccharide-Stimulated RAW 264.7 Cells. Inflammation. 2016 Aug;39(4):1573-81. doi: 10.1007/s10753-016-0393-4. PubMed PMID: 27317418.
5: Nacar A, Karaboğa I, Okuyan HM, Sefil NK, Nacar E, Motor S, Akküçük S, Ozkan OV. Investigation of the protective effect of erdosteine against cyclosporine-induced injury in rat liver with histological and biochemical methods. Turk J Med Sci. 2015;45(6):1390-5. PubMed PMID: 26775399.
6: Guven A, Ickin M, Uzun O, Bakar C, Balbay EG, Balbay O. Erdosteine protects rat testis tissue from hypoxic injury by reducing apoptotic cell death. Andrologia. 2014 Feb;46(1):50-8. doi: 10.1111/and.12041. Epub 2012 Nov 16. PubMed PMID: 23157213.
7: Saritas A, Kandis H, Baltaci D, Yildirim U, Kaya H, Karakus A, Colakoglu S, Memisogullari R, Kara IH. N-Acetyl cysteine and erdosteine treatment in acetaminophen-induced liver damage. Toxicol Ind Health. 2014 Aug;30(7):670-8. doi: 10.1177/0748233712463780. Epub 2012 Oct 15. PubMed PMID: 23070635.
8: Moustafa NM, Badawey AM, Lamie NT, El-Aleem Ael-A. Stability-indicating methods for the determination of erdosteine in the presence of its acid degradation products. J AOAC Int. 2014 Jan-Feb;97(1):86-93. PubMed PMID: 24672863.
9: Jin J, Chen XY, Zhang YF, Ma ZY, Zhong DF. [Simultaneous determination of erdosteine and its active metabolite in human plasma by liquid chromatography-tandem mass spectrometry with pre-column derivatization]. Yao Xue Xue Bao. 2013 Mar;48(3):395-400. Chinese. PubMed PMID: 23724654.
10: Moretti M, Fagnani S. Erdosteine reduces inflammation and time to first exacerbation postdischarge in hospitalized patients with AECOPD. Int J Chron Obstruct Pulmon Dis. 2015 Oct 28;10:2319-25. doi: 10.2147/COPD.S87091. eCollection 2015. PubMed PMID: 26604731; PubMed Central PMCID: PMC4630194.
11: Sirmali R, Armağan A, Öktem F, Uz E, Kirbas A, Dönmezs S, Yilmaz HR, Silay MS, Sirmali M. Protective effects of erdosteine, vitamin E, and vitamin C on renal injury induced by the ischemia-reperfusion of the hind limbs in rats. Turk J Med Sci. 2015;45(1):33-7. PubMed PMID: 25790527.
12: Hoza J, Salzman R, Starek I, Schalek P, Kellnerova R. Efficacy and safety of erdosteine in the treatment of chronic rhinosinusitis with nasal polyposis - a pilot study. Rhinology. 2013 Dec;51(4):323-7. doi: 10.4193/Rhin13.039. PubMed PMID: 24260764.
13: Saliba I, El Fata F. Is intratympanic injection of erdosteine protective against cisplatin-induced ototoxicity? Neurotox Res. 2012 Apr;21(3):302-8. doi: 10.1007/s12640-011-9282-7. Epub 2011 Oct 12. PubMed PMID: 21989624.
14: Elkady AA, Ibrahim IM. Protective effects of erdosteine against nephrotoxicity caused by gamma radiation in male albino rats. Hum Exp Toxicol. 2016 Jan;35(1):21-8. doi: 10.1177/0960327115574919. Epub 2015 Feb 24. PubMed PMID: 25716170.
15: Demiralay R, Gürsan N, Erdem H. The effects of erdosteine and N-acetylcysteine on apoptotic and antiapoptotic markers in pulmonary epithelial cells in sepsis. Eurasian J Med. 2013 Oct;45(3):167-75. doi: 10.5152/eajm.2013.35. PubMed PMID: 25610275; PubMed Central PMCID: PMC4261429.
16: Waissbluth S, Dupuis I, Daniel SJ. Protective effect of erdosteine against cisplatin-induced ototoxicity in a guinea pig model. Otolaryngol Head Neck Surg. 2012 Apr;146(4):627-32. doi: 10.1177/0194599811426261. Epub 2011 Nov 3. PubMed PMID: 22051542.
17: Dal Negro RW, Visconti M, Tognella S, Micheletto C. Erdosteine affects eicosanoid production in COPD. Int J Clin Pharmacol Ther. 2011 Jan;49(1):41-5. PubMed PMID: 21176724.
18: Tutanc M, Arica V, Yılmaz N, Nacar A, Zararsiz I, Basarslan F, Tutanc OD, Nacar E. Effects of erdosteine on cyclosporin-A-induced nephrotoxicity. Hum Exp Toxicol. 2012 Jun;31(6):565-73. doi: 10.1177/0960327111417907. Epub 2011 Aug 3. PubMed PMID: 21813577.
19: Ma L, Zhang LD, Wang WN, Yao TW. [HPLC determination of the related substances in erdosteine]. Yao Xue Xue Bao. 2012 Aug;47(8):1039-42. Chinese. PubMed PMID: 23162901.
20: Guzel A, Kayhan S, Tutuncu S, Guzel A, Duran L, Alacam H, Gunaydin M, Torun AC, Yilmaz MZ, Selcuk MY, Murat N. Attenuation of bleomycin induced lung fibrosis by erdosteine and inhibition of the inducible nitric oxide synthase. Bratisl Lek Listy. 2015;116(3):196-202. PubMed PMID: 25869570.
