InformationSBI-797812 SBI-797812 is a NAMPT activator which is structurally similar to active-site directed NAMPT inhibitors and blocks binding of these inhibitors to NAMPT . SBI-797812 turns NAMPT into a "super catalyst" that more efficiently generates NMN.SBI-797812 is an orally active nicotinamide phosphoribosyltransferase (NAMPT) activator. SBI-797812 shifts NAMPT to NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD+. SBI-797812 increases intracellular nicotinamide mononucleotide (NMN) and elevates liver NAD+ in mice。TargetsNAMPTIn vitroSBI-797812 shifts the NAMPT reaction equilibrium towards NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT at His247, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD+. Treatment of cultured cells with SBI-797812 increases intracellular NMN and NAD+.In vivoPlasma concentrations of SBI-797812 after oral administration are low. Higher plasma levels of SBI-797812 are seen after i.p. dosing. The potency of SBI-797812 against mouse NAMPT is investigated. The apparent affinity (EC50) of SBI-797812 for mouse NAMPT is approximately 8-fold less than for human NAMPT, whereas maximal fold activation by SBI-797812 is comparable between the mouse and human NAMPT. Dosing of mice with SBI-797812 elevates liver NAD+.Cell Research(from reference)Cell lines：Human A549 lung carcinoma cells Concentrations：10 μM Incubation Time：4 h. Specification: 0.98 Molecular Formula: C19H22N4O4S Molecular Weight: 402.47 PubChem CID: 135222620 Isomeric SMILES: C1CC2CN(CC1O2)S(=O)(=O)C3=CC=C(C=C3)NC(=O)NCC4=CC=NC=C4
- UPC:
- 51162627
- Condition:
- New
- Availability:
- 1 day
- Weight:
- 0.96 Ounces
- HazmatClass:
- No
- WeightUOM:
- LB
- MPN:
- S414308-5mg
- CAS:
- 2237268-08-3
- Product Size:
- 5mg
