Zileuton

Zileuton (CAS 111406-87-2)

Zileuton | CAS 111406-87-2 is rated 5.0 out of 5 by 1.
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Application: A 5-LO (5-lipoxygenase) inhibitor
CAS Number: 111406-87-2
Purity: >99%
Molecular Weight: 236.29
Molecular Formula: C11H12N2O2S
* Refer to Certificate of Analysis for lot specific data (including water content).
Submit a review for this product and receive 15 CruzCredits

Zileuton is an orally active 5-LO (5-lipoxygenase) inhibitor that inhibits LTB4 synthesis (IC50 values are 0.56, 2.3 and 2.6 μM in dog, rat and human blood respectively). Zileuton inhibits antigen-induced contraction of tracheal strips in vitro (IC50 = 6 μM) and shows antiasthmatic activity in vivo. Zileuton also weakly inhibits CYP1A2 (Ki = 66 - 98 μM).


References

McMillan et al (1992) Pre-clinical pharmacology of ICI D2138, a potent orally-active non-redox inhibitor of 5-lipoxygenase. Br.J.Pharmacol. 107 1042. Malo et al (1994) The 5-lipoxygenase inhibitory activity of zileuton in in vitro and in vivo models of antigen-induced airway anaphylaxis. Pulm.Pharmacol. 7 73. Lu et al (2003) Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor. Drug Metab.Dispos. 31 1352.

Appearance :
Crystalline powder
Physical State :
Solid
Solubility :
Soluble in DMSO (47 mg/ml at 25° C), methanol, ethanol (47 mg/ml at 25° C), DMF (~30 mg/ml), and 1:1 DMSO:PBS(pH 7.2) (~0.5 mg/ml).
Storage :
Store at room temperature
Melting Point :
152-153° C
Boiling Point :
~449.4° C at 760 mmHg (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.70 (Predicted)
IC50 :
5-LO: IC50 = 0.5 µM (RBL-1 cells); LTB4 synthesis: IC50 = 0.56 µM (dog); LTB4 synthesis: IC50 = 2.3 µM (rat); LTB4 synthesis: IC50 = 2.6 µM (human); Antigen-induced contraction of tracheal strips: IC50 = 6 µM
Ki Data :
CYP1A2: Ki= 66-98 µM
pK Values :
pKa: 9.97 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
1
RTECS :
YR9057000
PubChem CID :
60490
Merck Index :
14: 10124
MDL Number :
MFCD00866097
SMILES :
CC(C1=CC2=CC=CC=C2S1)N(C(=O)N)O

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Certificate of Analysis

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Zileuton  Product Citations

See how others have used Zileuton. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 29074417  Wang, Y.|Sherchan, P.|Huang, L.|Akyol, O.|McBride, DW.|Zhang, JH.| et al. 2018. Exp. Neurol. 300: 30-40.

PMID: # 24583243  2014. Anal. Biochem. 453: 4-6.

Citations 1 to 2 of 2 total

Please, I Need to dilute Zileuton (CAS 111406-87-2) in Carboxymethylcellulose 0,5% to give to my rats by gavage in a dosage of 30 mg/kg. Do you have any suggestion how can I dilute it? Thanks in advance.

Asked by: Marcell
Unfortunately we are not able to provide that information. Our compounds are not pharmaceutical grade and not manufactured under GMP guidelines. Please consult your principal investigator and your animal care and use committee (ACUC) regarding the use of our compounds.
Answered by: Technical Support
Date published: 2019-01-26
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Rated 5 out of 5 by from Kuvibidila et al Kuvibidila et al. (PubMed ID 26412995) found that Zileuton likely reduced IL-2 secretion via inhibition of 5-lipoxygenase in patients with sickle cell disease. -SCBT Publication Review
Date published: 2015-03-25
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