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Nampt-IN-1

Catalog No. T4376   CAS 1698878-14-6
Synonyms: LSN3154567

Nampt-IN-1 (LSN3154567) (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Nampt-IN-1 Chemical Structure
Nampt-IN-1, CAS 1698878-14-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 33.00
2 mg In stock $ 44.00
5 mg In stock $ 76.00
10 mg In stock $ 139.00
25 mg In stock $ 272.00
50 mg In stock $ 455.00
100 mg In stock $ 672.00
1 mL * 10 mM (in DMSO) In stock $ 84.00
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Purity: 99.4%
Purity: 96.82%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Nampt-IN-1 (LSN3154567) (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.
Targets&IC50 CSF1R:0.84 μM, NAMPT:3.1 nM
In vitro LSN3154567 inhibits purified NAMPT with an IC50 of 3.1 nM. When tested against a panel of human kinases (>100; CEREP Kinase panel), it does not exhibit any significant activity (i.e.: IC50≥1 μM) against the kinases tested except CSF1R (IC50≈0.84 μM). To assess its anticancer activity, LSN3154567 is tested against a number of different types of cancer cell lines cultured in the absence or presence of nicotinic acid (NA) (10 μM). LSN3154567 exhibits a potent antiproliferative activity against many cell lines in the absence of NA.
In vivo When dosed orally with 2 mg/kg in mice, it has an exposure of 195 nM*hour in the plasma with a peak concentration of 57 nM (at 0.25 hour) and an oral bioavailability of 39%. When dosed intravenously with 2 mg/kg, it has a hepatic clearance of 158.73 mL/min/kg and a volume of distribution at 7.1 L/kg. The half-life of terminal elimination is estimated to be 2.76 hours. LSN3154567 exhibits a dose-dependent inhibition of NAD+ formation with estimated TED50 value of 2.0 mg/kg. Dogs are treated with LSN3154567 at 1 and 2.5 mg/kg. At these dose levels, the retinal toxicity is observed. Degeneration of the outer nuclear layer occurred in all four animals, but is less pronounced in the animals treated with 1 mg/kg.
Cell Research The cell lines used as following: A2780 and KM-12, KMS-11 and MKN-74, OPM-2 and Kelly; and all other cancer cells. Cells are seeded in 96-well plates, cultured overnight, and treated with LSN3154567 (0.03 to 1,000 nM)±NA (10 μM) in duplicate at 37°C in 5% CO2 for 72 hours. Staurosporine (10 μM) is used as positive control. Cell viability is determined by a CytoTox-Glo Cytotoxicity assay kit.
Animal Research Male CD-1 mice are dosed with LSN3154567 at 2 mg/kg intravenously in 20% Captisol (w/v), 25 mmol/L NaPO4, pH 2, q.s. formulation or 2 mg/kg orally in the same vehicle in a cross over design with 3-d wash period in between two arms. Blood samples are obtained through retro orbital at 0, 0.08 (IV only), 0.25, 0.75, 2, 4, 8, and 24 hours and frozen until analysis. For exposure analysis, blood samples (≈20 μL) are obtained through tail clipping at 0.5, 1, 2, 4, 8, and 24 hours. The samples are collected into EDTA-coated capillary tubes and spotted onto Whatman DMPK-C DBS collection cards.
Synonyms LSN3154567
Molecular Weight 419.49
Formula C20H25N3O5S
CAS No. 1698878-14-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 30 mg/mL

TargetMolReferences and Literature

1. Zhao G, et al. Discovery of a Highly Selective NAMPT Inhibitor That Demonstrates Robust Efficacy and Improved Retinal Toxicity with Nicotinic Acid Coadministration. Mol Cancer Ther. 2017 Dec;16(12):2677-2688.

Related compound libraries

This product is contained In the following compound libraries:
Immuno-Oncology Compound Library Anti-Metabolism Disease Compound Library Bioactive Compounds Library Max NO PAINS Compound Library Kinase Inhibitor Library Glycometabolism Compound Library Metabolism Compound Library Tyrosine Kinase Inhibitor Library Transcription Factor-Targeted Compound Library Cytokine Inhibitor Library

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Keywords

Nampt-IN-1 1698878-14-6 Metabolism Tyrosine Kinase/Adaptors c-Fms NAMPT CSF-1R PBEF Nampt IN 1 Visfatin inhibit LSN-3154567 Pre-B cell colony enhancing factor Nicotinamide phosphoribosyl transferase LSN 3154567 Inhibitor LSN3154567 NamptIN1 inhibitor

 

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