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MedChemExpressModel Chlorzoxazone - 95-25-0

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Chlorzoxazone is a SK-type potassium channel activator. Chlorzoxazone modulates FOXO3 phosphorylation and Aβ. Chlorzoxazone enhances immunosuppression, attenuates vasoconstriction, attenuates cognitive deficits, and improves experimental autoimmune encephalomyelitis[1][sup>[2][3][sup>[4][sup>[5][sup>[6][7][8][9][10].
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Chlorzoxazone

MCE China:Chlorzoxazone

Brand:MedChemExpress (MCE)

Cat. No.HY-B1462

CAS:95-25-0

Purity:99.84%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Chlorzoxazone is a SK-type potassium channel activator. Chlorzoxazone modulates FOXO3 phosphorylation and Aβ. Chlorzoxazone enhances immunosuppression, attenuates vasoconstriction, attenuates cognitive deficits, and improves experimental autoimmune encephalomyelitis.

In Vitro:Chlorzoxazone (200-1000 μM, 0-24 h) decreases viability and induces [Ca2+]i rises in a concentration‑dependent manner in OC2 cells[2]. Chlorzoxazone (2-20 μM, 4 days) augments immunosuppressive capacity of mesenchymal stem cells via modulation of FOXO3 phosphorylation[3]. Chlorzoxazone (1-30 μM, 30 min) inhibits IL-6 secretion of dendritic cells[4]. Chlorzoxazone (30 μM) suppresses voltage-dependent L-type Ca2+ current in pituitary GH3 cells[5]. Chlorzoxazone (2.5-80 μM, 24 h) attenuates inflammatory response and amyloidogenesis in the isolated astrocytes and microglial cells with Aβ[6]. Chlorzoxazone (300 μM) abolishs 4-aminopyridine (HY-B0604)-induced vasoconstriction in rat thoracic aorta[7]. Chlorzoxazone (600 μM) or 1-EBIO increases Na+ absorption across cystic fibrosis airway epithelial cells[8].

In Vivo:Chlorzoxazone (30-100 mg/kg, p.o., daily, from day 3 following immunization until the end of the experiment) alleviates experimental autoimmune encephalomyelitis in mice[4]. Chlorzoxazone (25-100 mg/kg, p.o., daily, 4 weeks) attenuates cognitive deficits and neuron death in AD mice[6]. Chlorzoxazone (20 mg/kg, i.v.; 50 mg/kg, p.o.) is metabolized to OH-CZX via CYP2E1 in rat models of diabetes induced by Alloxan (HY-W017227) or Streptozotocin (HY-13753)[9]. Chlorzoxazone (10-50 mg/kg, i.p., 20-30 min before onset of access to alcohol) reduces excessive alcohol intake in IAA rats[10].

IC50 & Target:CYP2

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References:

[1]. Yamamura Y, et al. Comprehensive kinetic analysis and influence of reaction components for chlorzoxazone 6-hydroxylation in human liver microsomes with CYP antibodies. Xenobiotica. 2015 Apr;45(4):353-360.  [Content Brief]

[2]. Lu T, et al. Action of chlorzoxazone on Ca2+movement and viability in human oral cancer cells. Chin J Physiol. 2019 May-Jun;62(3):123-130.  [Content Brief]

[3]. Deng L, et al. Chlorzoxazone, a small molecule drug, augments immunosuppressive capacity of mesenchymal stem cells via modulation of FOXO3 phosphorylation. Cell Death Dis. 2020 Mar 2;11(3):158.  [Content Brief]

[4]. Lv J, et al. Chlorzoxazone Alleviates Experimental Autoimmune Encephalomyelitis via Inhibiting IL-6 Secretion of Dendritic Cells. J Immunol. 2022 Apr 1;208(7):1545-1553.  [Content Brief]

[5]. Liu YC, et al. Stimulatory effects of chlorzoxazone, a centrally acting muscle relaxant, on large conductance calcium-activated potassium channels in pituitary GH3 cells. Brain Res. 2003 Jan 3;959(1):86-97.  [Content Brief]

[6]. Bai Y, et al. Chlorzoxazone exhibits neuroprotection against Alzheimer's disease by attenuating neuroinflammation and neurodegeneration in vitro and in vivo. Int Immunopharmacol. 2020 Nov;88:106790.  [Content Brief]

[7]. Dong DL, et al. Chlorzoxazone inhibits contraction of rat thoracic aorta. Eur J Pharmacol. 2006 Sep 18;545(2-3):161-6.  [Content Brief]

[8]. Gao L, et al. Chlorzoxazone or 1-EBIO increases Na(+) absorption across cystic fibrosis airway epithelial cells. Am J Physiol Lung Cell Mol Physiol. 2001 Nov;281(5):L1123-9.  [Content Brief]

[9]. Baek HW, et al. Pharmacokinetics of chlorzoxazone in rats with diabetes: Induction of CYP2E1 on 6-hydroxychlorzoxazone formation. J Pharm Sci. 2006 Nov;95(11):2452-62.  [Content Brief]

[10]. Hopf FW, et al. Chlorzoxazone, an SK-type potassium channel activator used in humans, reduces excessive alcohol intake in rats. Biol Psychiatry. 2011 Apr 1;69(7):618-24.  [Content Brief]

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