Description
A-484954 is a highly selective eukaryotic elongationfactor-2 (eEF2) inhibitor, with an IC50 of 280 nM.
Product information
CAS Number: 142557-61-7
Molecular Weight: 289.29
Formula: C13H15N5O3
Chemical Name: 7-amino-1-cyclopropyl-3-ethyl-2,4-dioxo-1H,2H,3H,4H-pyrido[2,3-d]pyrimidine-6-carboxamide
Smiles: CCN1C(=O)N(C2CC2)C2=NC(N)=C(C=C2C1=O)C(N)=O
InChiKey: HWODCHXORCTEGU-UHFFFAOYSA-N
InChi: InChI=1S/C13H15N5O3/c1-2-17-12(20)8-5-7(10(15)19)9(14)16-11(8)18(13(17)21)6-3-4-6/h5-6H,2-4H2,1H3,(H2,14,16)(H2,15,19)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 25 mg/mL (86.42 mM; Need ultrasonic). H2O : < 0.1 mg/mL (insoluble).
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:
A-484954 is a highly selective eEF2K inhibitor with an IC50 value of 280 nM against eEF2K in the enzymatic assay and little activity against a wide panel of serine/threonine and tyrosine kinases. In enzymatic assay, the IC50 value of A-484954 is increased as the concentration of ATP increased but unaffected by increasing concentrations of calmodulin.
In Vivo:
A484954 causes relaxation in E (+) and E (-) aorta or mesenteric artery precontracted with NA. Pretreatment with L-NAME but not indomethacin or cimetidine partially inhibits the A484954-induced relaxation in mesenteric artery. Long-term A-484954 treatment inhibits MCT-induced increases PA pressure. It is revealed that A-484954 inhibits MCT-induced PA hypertrophy and fibrosis but not impairment of endothelium-dependent and -independent relaxation. Furthermore, A-484954 inhibits MCT-induced NADPH oxidase-1 expression and ROS generation as well as matrix metalloproteinase-2 activation.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.
