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SBI-797812 Sale

目录号 : GC37602

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 Chemical Structure

Cas No.:2237268-08-3

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Sample solution is provided at 25 µL, 10mM.

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.

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]

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]

[1] Stephen J Gardell, et al. Nat Commun. 2019 Jul 19;10(1):3241.

化学性质

Cas No. 2237268-08-3 SDF
Canonical SMILES O=C(NCC1=CC=NC=C1)NC2=CC=C(S(=O)(N3CC(O4)CCC4C3)=O)C=C2
分子式 C19H22N4O4S 分子量 402.47
溶解度 DMSO: 250 mg/mL (621.16 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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1 mg 5 mg 10 mg
1 mM 2.4847 mL 12.4233 mL 24.8466 mL
5 mM 0.4969 mL 2.4847 mL 4.9693 mL
10 mM 0.2485 mL 1.2423 mL 2.4847 mL
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