Carbocisteine  (Synonyms: Carbocysteine)

Carbocisteine is an orally active mucolytic agent. Carbocisteine attenuates the phosphorylation of NF-κB p65 and ERK1/2. Carbocisteine modulates Nrf2/HO-1 and NFκB interplay. Carbocisteine inhibits Apoptosis. Carbocisteine is used in chronic obstructive pulmonary disease (COPD) research^{[1][2][3][4][5][6][7][8][9][10][11][12][13]}.

Carbocisteine (10-1000 μM, 24 h) attenuates hydrogen peroxide-induced inflammatory injury in A549 cells via NF-κB and ERK1/2 MAPK pathways^[4].
Carbocisteine (L-Carbocisteine, 10 μM, from 3 days before infection) shows inhibitory effects on type A seasonal influenza virus infection in human airway epithelial cells^[5].
Carbocisteine (L-carbocisteine, 10 μM, 72 h) inhibits oxidant-induced apoptosis in cultured human airway epithelial cells^[12].
Carbocisteine (10-1000 μM, 24 h) attenuates TNF-α-induced inflammation in human alveolar epithelial cells in vitro through suppressing NF-κB and ERK1/2 MAPK signaling pathways^[13].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Carbocisteine (100 mg/kg, oral gavage, twice daily from 1 day before CS exposure until the end of the experiment) reduces virus-induced pulmonary inflammation in mice exposed to cigarette smoke^[2].
. Carbocisteine (100 mg/kg, p.o.) promotes phagocytosis of apoptotic cells by alveolar macrophages in BALB/c mice^[3].
. Carbocisteine (125-250 mg/kg/d, gavage, once a week for 3 weeks) protects against emphysema induced by cigarette smoke extract in rats^[6].
Carbocisteine (500 mg/kg/day, p.o., in two divided doses, 2 days) inhibits oxidative stress, inflammatory response, and apoptosis in acetic acid-induced UC by modulating the Nrf2/HO-1 and NFκB interplay in rats^[7].
Carbocisteine (112.5-225 mg/kg/d, gavage, 12 weeks) inhibits the expression of Muc5b in COPD mouse model^[8].
Carbocisteine (300 mg/kg, i.g., once every day for the last 6 weeks) ameliorates steroid resistance in rat COPD model^[9].
Carbocisteine (250 mg/kg ×2/day, p.o., 25 days) inhibits the changes in these enzyme (fucosidase, sialidase, fucosyltransferase and sialyltransferase) activities and the expressions of Muc5ac mRNA and protein in the lungin SO₂-exposed rats^[10].
Carbocysteine (300 mg/kg, p.o., every day both from week 6 to week 12 of smoke exposure) restores steroid sensitivity by targeting histone deacetylase 2 in a thiol/GSH-dependent manner in rats^[11].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

179.19

C₅H₉NO₄S

638-23-3

Solid

White to off-white

N[C@@H](CSCC(O)=O)C(O)=O

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

• [1]. Paola Rogliani, et al. Efficacy and safety profile of mucolytic/antioxidant agents in chronic obstructive pulmonary disease: a comparative analysis across erdosteine, carbocysteine, and N-acetylcysteine. Respir Res. 2019 May 27;20(1):104.  [Content Brief]

  [2]. Yageta Y, et al. Carbocisteine reduces virus-induced pulmonary inflammation in mice exposed to cigarette smoke. Am J Respir Cell Mol Biol. 2014 May;50(5):963-73.  [Content Brief]

  [3]. Inoue M, et al. Carbocisteine promotes phagocytosis of apoptotic cells by alveolar macrophages. Eur J Pharmacol. 2012 Feb 29;677(1-3):173-9.  [Content Brief]

  [4]. Wang W, et al. Carbocisteine attenuates hydrogen peroxide-induced inflammatory injury in A549 cells via NF-κB and ERK1/2 MAPK pathways. Int Immunopharmacol. 2015 Feb;24(2):306-313.  [Content Brief]

  [5]. Yamaya M, et al. Inhibitory effects of carbocisteine on type A seasonal influenza virus infection in human airway epithelial cells. Am J Physiol Lung Cell Mol Physiol. 2010 Aug;299(2):L160-8.  [Content Brief]

  [6]. Hanaoka M, et al. Carbocisteine protects against emphysema induced by cigarette smoke extract in rats. Chest. 2011 May;139(5):1101-1108.  [Content Brief]

  [7]. Abdelhamid AM, et al. Carbocisteine as a Modulator of Nrf2/HO-1 and NFκB Interplay in Rats: New Inspiration for the Revival of an Old Drug for Treating Ulcerative Colitis. Front Pharmacol. 2022 Jun 8;13:887233.  [Content Brief]

  [8]. Song Y, et al. Carbocisteine inhibits the expression of Muc5b in COPD mouse model. Drug Des Devel Ther. 2019 Sep 16;13:3259-3268.  [Content Brief]

  [9]. Song Y, et al. A mucoactive drug carbocisteine ameliorates steroid resistance in rat COPD model. Pulm Pharmacol Ther. 2016 Aug;39:38-47.  [Content Brief]

  [10]. Ishibashi Y, et al. Effects of carbocisteine on altered activities of glycosidase and glycosyltransferase and expression of Muc5ac in SO2-exposed rats. Eur J Pharmacol. 2004 Mar 8;487(1-3):7-15.  [Content Brief]

  [11]. Song Y, et al. Carbocysteine restores steroid sensitivity by targeting histone deacetylase 2 in a thiol/GSH-dependent manner. Pharmacol Res. 2015 Jan;91:88-98.  [Content Brief]

  [12]. Yoshida M, et al. Carbocisteine inhibits oxidant-induced apoptosis in cultured human airway epithelial cells. Respirology. 2009 Sep;14(7):1027-34.  [Content Brief]

  [13]. Wang W, et al. Carbocisteine attenuates TNF-α-induced inflammation in human alveolar epithelial cells in vitro through suppressing NF-κB and ERK1/2 MAPK signaling pathways. Acta Pharmacol Sin. 2016 May;37(5):629-36.  [Content Brief]