SBI-797812

For research use only.

Catalog No.S8980

SBI-797812 Chemical Structure

CAS No. 2237268-08-3

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.

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Biological Activity

Description 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.
Targets
NAMPT [1]
()
In vitro

SBI-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+.[1]

In vivo

Plasma 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+.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: Human A549 lung carcinoma cells
  • Concentrations: 10 μM
  • Incubation Time: 4 h
  • Method:

    Human A549 lung carcinoma cells are grown in DMEM, 4.5 g l−1 D-(+)-glucose, 10% fetal bovine serum, penicillin/streptomycin mixture; 10 cm dishes and treated with DMSO (vehicle control) or SBI-797812 for 4 h.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: 8-week-old male C57BL/6 J mice
  • Dosages: 10 mg/kg, 20 mg/kg
  • Administration: Oral gavage, IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 80 mg/mL (198.77 mM)
Water Insoluble
Ethanol '2.5 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 402.47
Formula

C19H22N4O4S

CAS No. 2237268-08-3
Storage powder
in solvent
Synonyms N/A
Smiles C1CC2CN(CC1O2)S(=O)(=O)C3=CC=C(C=C3)NC(=O)NCC4=CC=NC=C4

In vivo Formulation Calculator (Clear solution)

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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID