Home Metabolism NAMPT activator SBI-797812 For research use only.

SBI-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 nicotinamide mononucleotide.

SBI-797812 Chemical Structure

SBI-797812 Chemical Structure

CAS: 2237268-08-3

Selleck's SBI-797812 has been cited by 1 publication

Purity & Quality Control

Batch: S898001 DMSO] 80 mg/mL] false] Ethanol] 2.5 mg/mL] false] Water] Insoluble] false Purity: 99.12%
99.12

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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 nicotinamide mononucleotide.
Targets
NAMPT [1]
In vitro
In vitro

SBI-797812 shifts the NAMPT reaction equilibrium towards nicotinamide mononucleotide 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 nicotinamide mononucleotide and NAD+.[1]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models 8-week-old male C57BL/6 J mice
Dosages 10 mg/kg, 20 mg/kg
Administration Oral gavage, IP

Chemical Information & Solubility

Molecular Weight 402.47 Formula

C19H22N4O4S
CAS No. 2237268-08-3 SDF --
Smiles C1CC2CN(CC1O2)S(=O)(=O)C3=CC=C(C=C3)NC(=O)NCC4=CC=NC=C4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 80 mg/mL ( (198.77 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2.5 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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