Nampt activator-4

Cat. No.: HY-157421 Purity: 98.87%: Data Sheet
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Nampt activator-4 is an orally active NAMPT activator, with an EC₅₀ of 58 nM and a K_a of 85.38 nM against human NAMPT. Nampt activator-4 effectively relieves the feedback inhibition of nicotinamide and NAD⁺, thereby enhancing enzymatic activity and significantly increasing intracellular NAD⁺ levels. Nampt activator-4 exhibits moderate stability in human and mouse liver microsomes. Nampt activator-4 shows low to moderate inhibitory effects on cytochrome P450 (especially CYP3A4). Nampt activator-4 can be used for the research of type 2 diabetes and related metabolic disorders.

For research use only. We do not sell to patients.

Nampt activator-4 Chemical Structure

CAS No. : 2847156-05-0

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

EC50: 0.058 μM (NAMPT)^[1].

In Vitro

Nampt activator-4 (Compound 63) allosterically activates recombinant human NAMPT, with an EC₅₀ of 58 nM and a K_d of 85.38 nM^[1].
Nampt activator-4 (Compound 63) (0.001-10 μM; 24 h) increases NAD⁺levels in THP-1 human leukemia monocytic cells, with an EC₅₀ of 85 nM, and reaches approximately 140% of the control level after 24 h of treatment at 10 μM^[1].
Nampt activator-4 (3 μM; 24 h) competes with the NAMPT inhibitor FK866 for binding to NAMPT in human leukemia monocytic cells THP-1, and reduces the inhibitory potency of FK866^[1].
Nampt activator-4 is rapidly metabolized in mouse and human liver microsomes, with half-lives of 2.3 min and 4.2 min, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Nampt activator-4 (30 mg/kg; p.o.; single dose), administered in male C57BL/6 mice, achieves plasma concentrations that align with its in vitro NAMPT activation potency^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 mice (male, 20-40 g)^[1]
Dosage:	30 mg/kg
Administration:	p.o.; single dose
Result:	Achieved a maximal plasma concentration of 3.2 μM. Reached a plasma concentration of 180 nM at 3 h post-administration.

Molecular Weight

537.56

Formula

C₂₆H₂₂F₃N₇OS

CAS No.

2847156-05-0

Appearance

Solid

Color

White to off-white

SMILES

O=C([C@@H]1CN(CCN1)C2=NC=NC3=NN(C=C32)C4=CC=C(C=C4)C(F)(F)F)NCC5=CC=C6SC=CC6=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (186.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8603 mL	9.3013 mL	18.6026 mL
5 mM	0.3721 mL	1.8603 mL	3.7205 mL
10 mM	0.1860 mL	0.9301 mL	1.8603 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.87%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (247 KB) HNMR (146 KB) RP-HPLC (166 KB) NP-HPLC (127 KB) LCMS (109 KB)

Handling Instructions (2659 KB)

References

[1]. Shen Z, et al. Synthesis, Optimization, and Structure-Activity Relationships of Nicotinamide Phosphoribosyltransferase (NAMPT) Positive Allosteric Modulators (N-PAMs). J Med Chem. 2023;66(24):16704-16727. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8603 mL	9.3013 mL	18.6026 mL	46.5064 mL
	5 mM	0.3721 mL	1.8603 mL	3.7205 mL	9.3013 mL
	10 mM	0.1860 mL	0.9301 mL	1.8603 mL	4.6506 mL
	15 mM	0.1240 mL	0.6201 mL	1.2402 mL	3.1004 mL
	20 mM	0.0930 mL	0.4651 mL	0.9301 mL	2.3253 mL
	25 mM	0.0744 mL	0.3721 mL	0.7441 mL	1.8603 mL
	30 mM	0.0620 mL	0.3100 mL	0.6201 mL	1.5502 mL
	40 mM	0.0465 mL	0.2325 mL	0.4651 mL	1.1627 mL
	50 mM	0.0372 mL	0.1860 mL	0.3721 mL	0.9301 mL
	60 mM	0.0310 mL	0.1550 mL	0.3100 mL	0.7751 mL
	80 mM	0.0233 mL	0.1163 mL	0.2325 mL	0.5813 mL
	100 mM	0.0186 mL	0.0930 mL	0.1860 mL	0.4651 mL