Description
IC50: 0.73, 0.31, and 0.99 μM for COX-1, COX-2, and 5-LO, respectively ZLJ-6 is a dual inhibitor of COX and 5-lipoxygenase (5-LO). Cyclooxygenase (COX) is an enzyme that is responsible for formation of prostanoids, such as thromboxane and prostaglandins such as prostacyclin. 5-lipoxygenase (5-LO) is the major source of leukotrienes. In vitro: ZLJ-6 was identified as a potent inhibitor of cyclooxygenase in human whole blood. It also inhibited the production of thromboxane B(2) and prostaglandin E(2) in calcium ionophore A23187-induced human and rat whole blood, and rat peritoneal leukocytes. ZLJ-6 suppressed the activity of 5-lipoxygenase in the rat basophilic leukemia (RBL-1) cell lysate and in intact cells and reduced the generation of leukotriene B(4) (LTB(4)) in A23187-stimulated human or rat whole blood, and rat peritoneal leukocytes . In vivo: Orally administered ZLJ-6 demonstrated potent anti-inflammatory activity in the carrageenin-induced paw oedema model in rats and showed analgesic activity in the acetic acid-induced abdominal construction model in mice. No gastrointestinal ulcers were found with the anti-inflammatory dose (30 mg/kg) in normal rats . Clinical trial: So far, no clinical study has been conducted.
Product information
CAS Number: 1051931-39-5
Molecular Weight: 374.43
Formula: C14H18N2O6S2
Chemical Name: (3Z)-5-amino-3-[(4-methanesulfonylphenyl)methylidene]-4-methyl-3,4-dihydro-2H-pyrrol-2-one; methanesulfonic acid
Smiles: CS(=O)(=O)C1=CC=C(C=C1)/C=C1/C(C)C(N)=NC/1=O.CS(O)(=O)=O
InChiKey: HMVSXWPJALXXEV-AJULUCINSA-N
InChi: InChI=1S/C13H14N2O3S.CH4O3S/c1-8-11(13(16)15-12(8)14)7-9-3-5-10(6-4-9)19(2,17)18;1-5(2,3)4/h3-8H,1-2H3,(H2,14,15,16);1H3,(H,2,3,4)/b11-7-;
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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