Valdecoxib|cas 181695-72-7|DC Chemicals

Cas No.:	181695-72-7
Synonyms:	Bextra;SC 65872
SMILES:	CC1=C(C2=CC=C(S(N)(=O)=O)C=C2)C(C3=CC=CC=C3)=NO1
Formula:	C₁₆H₁₄N₂O₃S
M.Wt:	314.3589
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Valdecoxib (SC 65872) is a COX-2 selective inhibitor with an IC50 value of 5 nM. Valdecoxib is a non-steroidal anti-inflammatory drug (NSAID) used in the treatment of osteoarthritis, rheumatoid arthritis, and painful menstruation and menstrual symptoms. in vitro: The overall saturation binding affinity for COX-2 of valdecoxib is 2.6 nM (compared with 1.6 nM for celecoxib, 51 nM for rofecoxib, and 260 nM for etoricoxib), with a slow off-rate (t(1/2) approximately 98 min). Valdecoxib inhibits COX-1 in a competitive fashion only at very high concentrations (IC(50) = 150 microM). Collectively, these data provide a mechanistic basis for the potency and in vitro selectivity of valdecoxib for COX-2. Valdecoxib showed similar activity in the human whole-blood COX assay (COX-2 IC(50) = 0.24 microM; COX-1 IC(50) = 21.9 microM). The affinity of [(3)H]celecoxib for COX-2 (K(D) = 2.3 nM) was similar to the affinity of [(3)H]valdecoxib (K(D) = 3.2 nM). The binding to COX-2 seems to be both rapid and slowly reversible with association rates of 5.8 x 10(6)/M/min and 4.5 x 10(6)/M/min and dissociation rates of 14 x 10(-3)/min (t(1/2) = 50 min) and 7.0 x 10(-3)/min (t(1/2) = 98 min) for [(3)H]celecoxib and [(3)H]valdecoxib, respectively. in vivo: In rats, valdecoxib demonstrated marked potency in acute and chronic models of inflammation (air pouch ED(50) = 0.06 mg/kg; paw edema ED(50) = 5.9 mg/kg; adjuvant arthritis ED(50) = 0.03 mg/kg). In these same animals, COX-1 was spared at doses greater than 200 mg/kg . Valdecoxib was extensively metabolized after a single 5 mg/kg oral administration of [(14)C]valdecoxib and elimination of unchanged drug was minor (less than 1%) in male and female mice.

MSDS

COA

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2018-0101

Cat. No.	Product name	Field of application
DC45337	4,4'-Dihydroxy-2,6-dimethoxydihydrochalcone	4,4'-Dihydroxy-2,6-dimethoxydihydrochalcone exhibits COX-1 and COX-2 inhibitory activity.
DC47700	Enflicoxib	Enflicoxib (E 6087) is a nonsteroidal anti-inflammatory compound that selectively inhibits cyclooxygenase-2 (COX-2). Enflicoxib does not inhibit cyclooxygenase-1 (COX-1). E-6087 shows anti-inflammatory, analgesic and antipyretic activities in animal models.
DC47699	(Rac)-γ-Tocopherol	(Rac)-γ-Tocopherol (DMPBQ) is a Vitamin E isoform, which is converted by tocopherol cyclase to γ-Tcopherol.
DC47698	Clematomandshurica saponin B	Clematomandshurica saponins B shows significant inhibitory activity on cyclooxygenase-2 (IC50=2.58 mM).
DC47697	CXCR4 antagonist 2	CXCR4 antagonist 2 is a CXCR4 antagonist with an IC50 value of 47 nM.
DC46293	Rofecoxib (D5)	Rofecoxib D5 (MK 966 D5) is the deuterium labeled Rofecoxib. Rofecoxib is a potent, specific and orally active COX-2 inhibitor, with IC50s of 26 and 18 nM for human COX-2 in human osteosarcoma cells and Chinese hamster ovary cells, with a 1000-fold selectivity for COX-2 over human COX-1 (IC50 > 50 μM in U937 cells and > 15 μM in Chinese hamster ovary cells).
DC46292	Ketorolac D4	Ketorolac D4 (RS37619 D4) is the deuterium labeled Ketorolac. Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
DC45862	Plantanone B	Plantanone B is a moderate antioxidant-agent with an IC50 of 169.8±5.2 μM. Plantanone B shows significant ovine COX-1 and moderate COX-2 inhibitory activities. Plantanone B has the potential for inflammation-related diseases research.
DC45811	Humulone	Humulone (α-Lupulic acid), a prenylated phloroglucinol derivative, is a potent cyclooxygenase-2 (COX-2) inhibitor. Humulone acts as a positive modulator of GABAA receptor at low micromolar concentrations. Humulone is an inhibitor of bone resorption. Humulone possesses antioxidant, anti-angiogenic and apoptosis-inducing properties.
DC44842	(±)-Catechin	(±)-Catechin (rel-Cianidanol) is the racemate of Catechin. (±)-Catechin has two steric forms of (+)-Catechin and its enantiomer (-)-Catechin. (+)-Catechin inhibits cyclooxygenase-1 (COX-1) with an IC50 of 1.4 μM. Anticancer, anti-obesity, antidiabetic, anticardiovascular, anti-infectious, hepatoprotective, and neuroprotective effects.