2. Metabolic Enzyme/Protease
  3. Glucokinase
  4. Nerigliatin

Nerigliatin  (Synonyms: PF-04937319)

Cat. No.: HY-108328 Purity: 99.94%
COA Handling Instructions

Molarity Calculator

Nerigliatin (PF-04937319) is a glucokinase activator (GKA) with EC50 value of 154.4 μM, one of the most promising strategies for the treatment of type 2 diabetes mellitus. Nerigliatin is designed to maintain glucose-lowering efficacy while mitigating the risk of hypoglycaemia observed with many other GKAs.

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

Nerigliatin Chemical Structure

Nerigliatin Chemical Structure

CAS No. : 1245603-92-2

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 In-stock
Solution
10 mM * 1 mL in DMSO USD 121 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 190 In-stock
25 mg USD 390 In-stock
50 mg USD 710 In-stock
100 mg USD 1280 In-stock
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This product is a controlled substance and not for sale in your territory.

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Based on 1 publication(s) in Google Scholar

Nerigliatin Related Antibodies

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Description

Nerigliatin (PF-04937319) is a glucokinase activator (GKA) with EC50 value of 154.4 μM, one of the most promising strategies for the treatment of type 2 diabetes mellitus[1]. Nerigliatin is designed to maintain glucose-lowering efficacy while mitigating the risk of hypoglycaemia observed with many other GKAs[2].

IC50 & Target

EC50: 154.4 μM (GSA) (PF-04937319)[1]
Molecular Weight

432.43

Formula

C22H20N6O4
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C(C1=NC=C(OC2=C3C=C(C)OC3=CC(C(NC4=NC=C(C)N=C4)=O)=C2)C=N1)N(C)C
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 (231.25 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 2.3125 mL 11.5626 mL 23.1251 mL
5 mM 0.4625 mL 2.3125 mL 4.6250 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
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.78 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.78 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

Purity: 99.94%

COA (253 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
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 2.3125 mL 11.5626 mL 23.1251 mL 57.8128 mL
5 mM 0.4625 mL 2.3125 mL 4.6250 mL 11.5626 mL
10 mM 0.2313 mL 1.1563 mL 2.3125 mL 5.7813 mL
15 mM 0.1542 mL 0.7708 mL 1.5417 mL 3.8542 mL
20 mM 0.1156 mL 0.5781 mL 1.1563 mL 2.8906 mL
25 mM 0.0925 mL 0.4625 mL 0.9250 mL 2.3125 mL
30 mM 0.0771 mL 0.3854 mL 0.7708 mL 1.9271 mL
40 mM 0.0578 mL 0.2891 mL 0.5781 mL 1.4453 mL
50 mM 0.0463 mL 0.2313 mL 0.4625 mL 1.1563 mL
60 mM 0.0385 mL 0.1927 mL 0.3854 mL 0.9635 mL
80 mM 0.0289 mL 0.1445 mL 0.2891 mL 0.7227 mL
100 mM 0.0231 mL 0.1156 mL 0.2313 mL 0.5781 mL
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Nerigliatin Related Classifications

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.

Keywords:

Nerigliatin1245603-92-2PF-04937319PF04937319PF 04937319GlucokinaseHexokinase IVHexokinase DInhibitorinhibitorinhibit

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