Lumiracoxib(CGS 35189 COX 189)

Molecular Weight (MW)	293.72
Formula	C15H13ClFNO2
CAS No.	220991-20-8
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 59 mg/mL (200.9 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)	Chemical Name: 2-(2-((2-chloro-6-fluorophenyl)amino)-5-methylphenyl)acetic acid InChi Key: KHPKQFYUPIUARC-UHFFFAOYSA-N InChi Code: InChI=1S/C15H13ClFNO2/c1-9-5-6-13(10(7-9)8-14(19)20)18-15-11(16)3-2-4-12(15)17/h2-7,18H,8H2,1H3,(H,19,20) SMILES Code: O=C(O)CC1=CC(C)=CC=C1NC2=C(F)C=CC=C2Cl
Synonyms	Lumiracoxib; COX-189; CGS-35189; CGS 35189; COX189; CGS35189; COX 189; trade name: Prexige.

Molecular Weight (MW)

293.72

Formula

C15H13ClFNO2

CAS No.

220991-20-8

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: 59 mg/mL (200.9 mM)

Water: <1 mg/mL

Ethanol: <1 mg/mL

Solubility (In vivo)

Chemical Name: 2-(2-((2-chloro-6-fluorophenyl)amino)-5-methylphenyl)acetic acid

InChi Key: KHPKQFYUPIUARC-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H13ClFNO2/c1-9-5-6-13(10(7-9)8-14(19)20)18-15-11(16)3-2-4-12(15)17/h2-7,18H,8H2,1H3,(H,19,20)

SMILES Code: O=C(O)CC1=CC(C)=CC=C1NC2=C(F)C=CC=C2Cl

Synonyms

Lumiracoxib; COX-189; CGS-35189; CGS 35189; COX189; CGS35189; COX 189; trade name: Prexige.

In Vitro	In vitro activity: Lumiracoxib has an IC50 of 0.14 μm in COX-2-expressing dermal fibroblasts, but caused no inhibition of COX-1 at concentrations up to 30 μm (HEK 293 cells transfected with human COX-1). In a human whole blood assay, IC50 values for Lumiracoxib are 0.13 μM for COX-2 and 67 μM for COX-1 (COX-1/COX-2 selectivity ratio 515).
In Vivo	Lumiracoxib is a highly selective COX-2 inhibitor with anti-inflammatory, analgesic and antipyretic activities comparable with diclofenac, the reference NSAID, but with much improved gastrointestinal safety. Lumiracoxib is rapidly absorbed following oral administration in rats with peak plasma levels being reached between 0.5 and 1 h. Efficacy of Lumiracoxib in rat models of hyperalgesia, oedema, pyresis and arthritis is dose-dependent and similar to diclofenac. However, consistent with its low COX-1 inhibitory activity, Lumiracoxib at a dose of 100 mg/kg orally causes no ulcers and is significantly less ulcerogenic than diclofenac.
Animal model	Female Lewis rats
Formulation & Dosage	Dissolved in phosphate-buffered saline; 0.2–2 mg/kg; Oral gavage
References	Br J Pharmacol. 2005 Feb;144(4):538-50.

In Vitro

In vitro activity: Lumiracoxib has an IC50 of 0.14 μm in COX-2-expressing dermal fibroblasts, but caused no inhibition of COX-1 at concentrations up to 30 μm (HEK 293 cells transfected with human COX-1). In a human whole blood assay, IC50 values for Lumiracoxib are 0.13 μM for COX-2 and 67 μM for COX-1 (COX-1/COX-2 selectivity ratio 515).

In Vivo

Lumiracoxib is a highly selective COX-2 inhibitor with anti-inflammatory, analgesic and antipyretic activities comparable with diclofenac, the reference NSAID, but with much improved gastrointestinal safety. Lumiracoxib is rapidly absorbed following oral administration in rats with peak plasma levels being reached between 0.5 and 1 h. Efficacy of Lumiracoxib in rat models of hyperalgesia, oedema, pyresis and arthritis is dose-dependent and similar to diclofenac. However, consistent with its low COX-1 inhibitory activity, Lumiracoxib at a dose of 100 mg/kg orally causes no ulcers and is significantly less ulcerogenic than diclofenac.

Animal model

Female Lewis rats

Formulation & Dosage

Dissolved in phosphate-buffered saline; 0.2–2 mg/kg; Oral gavage

References

Br J Pharmacol. 2005 Feb;144(4):538-50.

CAS NO:	220991-20-8
规格:	≥98%

包装	价格(元)
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议
1g	电议
2g	电议