1. Metabolic Enzyme/Protease
  2. NAMPT Cytochrome P450
  3. Nampt-IN-5

Nampt-IN-5 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 also inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively.

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

Nampt-IN-5 Chemical Structure

Nampt-IN-5 Chemical Structure

CAS No. : 2380013-17-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 352 In-stock
Solution
10 mM * 1 mL in DMSO USD 352 In-stock
Solid
5 mg USD 320 In-stock
10 mg USD 560 In-stock
25 mg USD 890 In-stock
50 mg USD 1220 In-stock
100 mg USD 1650 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Nampt-IN-5 is a potent nicotinamide phosphoribosyltransferase (NAMPT) inhibitor. Nampt-IN-5 also inhibits CYP3A4 activity and has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively[1].

IC50 & Target

CYP3

0.7 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
A2780 IC50
0.7 nM
Compound: 27
Antiproliferative activity against human A2780 cells incubated for 72 hrs by CellTiterGlo assay
Antiproliferative activity against human A2780 cells incubated for 72 hrs by CellTiterGlo assay
[PMID: 31749905]
COR-L23 IC50
3.9 nM
Compound: 27
Antiproliferative activity against human COR-L23 cells incubated for 72 hrs by CellTiterGlo assay
Antiproliferative activity against human COR-L23 cells incubated for 72 hrs by CellTiterGlo assay
[PMID: 31749905]
In Vitro

Nampt-IN-5 (compound 27) (0-10 nM; 3 days) has cellular IC50s of 0.7 nM and 3.9 nM against A2780 and COR-L23, respectively [1].
Nampt-IN-5 shows a good ADME data: mouse microsomal clearance (110 μl/min•mg), CYP3A4 inhibition value (0.75 μM), Sol6.8: 0.056 mM; MDCK Papp AB: 18.6[1].

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

In Vivo

Nampt-IN-5 (5-30 mg/kg; p.o. twice daily for 4 days) causes a significant amount of body weight loss in nude mice relative to vehicle[1].
Nampt-IN-5 (10 mg/kg; p.o.) exhibits T1/2 (2.1 h), Cmax (29112 nM), and AUC (61984 nM•h) in mice[1].

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

Molecular Weight

427.50

Formula

C25H25N5O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CC(C2=CC=CN=C2)C1)NC3=CC=C(CN4C5=CC=CC=C5N=C4OCC)C=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (116.96 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 2.3392 mL 11.6959 mL 23.3918 mL
5 mM 0.4678 mL 2.3392 mL 4.6784 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)

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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 (5.85 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 (5.85 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)

g

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
References

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3392 mL 11.6959 mL 23.3918 mL 58.4795 mL
5 mM 0.4678 mL 2.3392 mL 4.6784 mL 11.6959 mL
10 mM 0.2339 mL 1.1696 mL 2.3392 mL 5.8480 mL
15 mM 0.1559 mL 0.7797 mL 1.5595 mL 3.8986 mL
20 mM 0.1170 mL 0.5848 mL 1.1696 mL 2.9240 mL
25 mM 0.0936 mL 0.4678 mL 0.9357 mL 2.3392 mL
30 mM 0.0780 mL 0.3899 mL 0.7797 mL 1.9493 mL
40 mM 0.0585 mL 0.2924 mL 0.5848 mL 1.4620 mL
50 mM 0.0468 mL 0.2339 mL 0.4678 mL 1.1696 mL
60 mM 0.0390 mL 0.1949 mL 0.3899 mL 0.9747 mL
80 mM 0.0292 mL 0.1462 mL 0.2924 mL 0.7310 mL
100 mM 0.0234 mL 0.1170 mL 0.2339 mL 0.5848 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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