Shopping Cart

Your shopping cart is currently empty

CHS-828

Name: CHS-828
Brand: TargetMol
SKU: T1998
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

Copy Product Info

🥰Excellent

Catalog No. T1998Cas No. 200484-11-3

Alias GMX1778, CHS 828

CHS-828 (GMX1778), a pyridyl cyanoguanidine, is an effective inhibitor of NAD+ biosynthesis enzyme NAMPT (IC50 <25 nM).

CHS-828

Copy Product Info

🥰Excellent

Purity: 99.9%

Catalog No. T1998Alias GMX1778, CHS 828Cas No. 200484-11-3

CHS-828 (GMX1778), a pyridyl cyanoguanidine, is an effective inhibitor of NAD+ biosynthesis enzyme NAMPT (IC50 <25 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$30	In Stock	In Stock
5 mg	$50	In Stock	In Stock
10 mg	$79	In Stock	In Stock
25 mg	$165	In Stock	In Stock
50 mg	$265	In Stock	In Stock
100 mg	$424	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$55	In Stock	In Stock

Add to Cart

Add to Quotation

In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

Questions

Batch Information

Select Batch

Purity:99.9%

Color:White

Resource Download

COA HPLC HNMR

Product Introduction

Bioactivity

Description	CHS-828 (GMX1778), a pyridyl cyanoguanidine, is an effective inhibitor of NAD+ biosynthesis enzyme NAMPT (IC50 <25 nM).
Targets&IC50	NAMPT:<25 nM
In vitro	GMX1778 induces NAD+ depletion through inhibition of NAD+ biosynthesis, followed by ATP depletion and ultimately resulted in cell death. [1] GMX1778 induces programmed cell death with apoptotic features. [2] GMX1778 suppresses nuclear factor-kappa B activity in cancer cells through downregulation of IKK activity (IC50=8 nM). [3]
In vivo	GMX1778 (250 mg/kg, p.o.) shows marked antitumoural activity against three different human neuroendocrine tumours, midgut carcinoid (GOT1), pancreatic carcinoid (BON), and medullary thyroid carcinoma (GOT2), transplanted in nude mice. [4]
Kinase Assay	In vitro coupled-enzyme NAMPT assay: Recombinant NAMPT activity is assessed using a coupled-enzyme assay based on the quantitation of NAD+. Reactions are performed at room temperature for 180 min using mixtures consisting of 50 mM HEPES (pH 7.4), 50 mM KCl, 5 mM MgCl2, 0.5 mM β-mercaptoethanol, 0.005% bovine serum albumin, 1% DMSO, 2.0 U/ml lactate dehydrogenase, 4 mM sodium L-lactate, 0.4 U/ml diaphorase, 6 μΜ resazurin sodium salt, 0.4 mM PRPP, 3.0 nM NMNAT1, 125 μM ATP, 50 μM NM, and 2 to 5 μM recombinant NAMPT. Fluorescence s measured with a Tecan Safire plate reader (excitation wavelength, 560 nm; emission wavelength, 590 nm). Ki values are calculated using Graphpad Prism 4.0 software and the Cheng-Prusoff equation.
Cell Research	Serial dilutions of GMX1778 in DMSO are performed to achieve a final concentration of 0.2% DMSO. Relative ATP levels after 72 h are determined using a ViaLight HS high-sensitivity cytotoxicity and cell proliferation BioAssay kit per the manufacturer's instructions. For GMX1778 cytotoxicity rescue experiments, cells are treated with NA (10 μM) or NMN (100 μM) simultaneously with GMX1778. Sigmoidal dose-response curves are generated by nonlinear regression analysis of variable slope using GraphPad Prism version 4.00 (GraphPad Software) to calculate 50% inhibitory (IC50) values.(Only for Reference)
Synonyms	GMX1778, CHS 828

Chemical Properties

Molecular Weight	371.86
Formula	C₁₉H₂₂ClN₅O
Cas No.	200484-11-3
Smiles	Clc1ccc(OCCCCCCNC(NC#N)=Nc2ccncc2)cc1
Relative Density.	1.18g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 69 mg/mL (185.55 mM), Sonication is recommended.

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

In Vivo Formulation

10% DMSO+90% Corn Oil: 2.5 mg/mL (6.72 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6892 mL	13.4459 mL	26.8918 mL	134.4592 mL
5 mM	0.5378 mL	2.6892 mL	5.3784 mL	26.8918 mL
10 mM	0.2689 mL	1.3446 mL	2.6892 mL	13.4459 mL
20 mM	0.1345 mL	0.6723 mL	1.3446 mL	6.7230 mL
50 mM	0.0538 mL	0.2689 mL	0.5378 mL	2.6892 mL
100 mM	0.0269 mL	0.1345 mL	0.2689 mL	1.3446 mL

Calculator

Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Molecular Weight Calculator

In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc