Description
SC-560 is a potent and selective COX-1 inhibitor with an IC50 of 9 nM.
Product information
CAS Number: 188817-13-2
Molecular Weight: 352.74
Formula: C17H12ClF3N2O
Chemical Name: 5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole
Smiles: COC1C=CC(=CC=1)N1N=C(C=C1C1C=CC(Cl)=CC=1)C(F)(F)F
InChiKey: PQUGCKBLVKJMNT-UHFFFAOYSA-N
InChi: InChI=1S/C17H12ClF3N2O/c1-24-14-8-6-13(7-9-14)23-15(10-16(22-23)17(19,20)21)11-2-4-12(18)5-3-11/h2-10H,1H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (283.49 mM; Need ultrasonic).
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
How to use
In Vitro:
Preincubation of COX-1 with SC-560 inhibits the conversion of arachidonic acid to PGE2 in a concentration-dependent manner. The IC50 of SC-560 for COX-2 is 6.3 μM, nearly 1,000-fold higher than with COX-1. SC-560 shows a dose and time dependent inhibitory effect on HCC cell growth. SC-560 also inhibits colony formation in soft agar and induces apoptosis in HCC cells in a dose-dependent manner. Moreover, SC-560 decreases the levels of the anti-apoptotic proteins survivin and XIAP and activates caspase 3 and 7 in a dose and time dependent fashion.
In Vivo:
Oral dosing with either 10 or 30 mg/kg SC-560 1 hour before assay completely inhibits ionophore-stimulated TxB2production, indicating that SC-560 is orally bioavailable and inhibits COX-1 in vivo. SC-560 extensively distributes into rat tissues, and has a CL approaching hepatic plasma flow. The drug displays low less than 15% and formulation dependent bioavailability after oral administration and demonstrates kidney toxicity.
Products are for research use only. Not for human use.
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