Ertiprotafib (Synonyms: PTP 112)

Cat. No.: HY-19383 Purity: 98.86%: FAQs
Data Sheet SDS COA Handling Instructions

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Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC₅₀ of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC₅₀ of ~1 μM for PPARα/PPARβ.

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Ertiprotafib Chemical Structure

CAS No. : 251303-04-5

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Description

IC₅₀ & Target

IC50: 1.6 μM (PTP1B), 400 nM (IKK-β)^[1], EC50: ~1 μM (PPARα/PPARβ)^[2].

In Vitro

Ertiprotafib is a potent inhibitor of IKK-β, with an IC₅₀ value of 400±40 nM, which is much lower than that required for the half-maximal inhibition of the p-nitrophenyl phosphatase activity of PTP1B. The reported IC₅₀ value of Ertiprotafib against PTP1B ranges from 1.6 to 29 μM depending on the assay conditions^[2]. Ertiprotafib is at least a dual PPARα and PPARβ agonist with EC₅₀ values for transactivation of 1 μM. Such activities readily explain the observations with suprapharmacologic doses of these^[1].

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

In Vivo

As seen with treatment of ob/ob mice, both Ertiprotafib and compound 3 seem to significantly improve glucose metabolism in rats. At 25 mg/kg/day, these compounds decrease both fasting blood glucose and insulin levels compared with vehicle treated rats. Furthermore, both Ertiprotafib and compound 3 increase glucose disposal after an oral challenge. It is noteworthy that lipid levels are also reduced in treated animals. Both triglyceride and free fatty acid levels are substantially reduced in rats treated with 25 mg/kg/day of either compound. To summarize, both Ertiprotafib and compound 3 seem to be robust agents in improving glucose utilization in fa/fa rats while also decreasing lipid levels in these animals. Decreased lipid levels may be unexpected for a pure PTP1b inhibitor. It is more telling, as mentioned above, that rats treated with suprapharmacologic doses of Ertiprotafib show signs of PPAR family activation^[2].

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

Molecular Weight

559.51

Formula

C₃₁H₂₇BrO₃S

CAS No.

251303-04-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

OC([C@@H](CC1=CC=CC=C1)OC2=C(C)C=C(C3=C(C(C)=C(C)S4)C4=C(Br)C5=CC=CC=C53)C=C2C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (178.73 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	1.7873 mL	8.9364 mL	17.8728 mL
5 mM	0.3575 mL	1.7873 mL	3.5746 mL
10 mM	0.1787 mL	0.8936 mL	1.7873 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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

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 (4.47 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (4.47 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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: 98.86%

Select Batch:

Data Sheet (281 KB) SDS (252 KB)

COA (257 KB) HNMR (275 KB) RP-HPLC (268 KB) LCMS (100 KB)

Handling Instructions (2659 KB)

Animal Administration
^[2]

Mice, Rats^[2]
Male Ob/ob mice and Zucker fa/fa rats are used. They are kept on a 12-h/12-h light/dark cycle and fed Rodent Diet 5001 (for mice and rats) from Purina Mills. Compounds are dosed orally by gavage in an aqueous suspension of 2% Tween 80 and 0.5% methylcellulose. Whole blood (5 μL) is used for glucose readings via tail nick for measurement using the Ascensia Elite XL glucometer and glucose strips by preloading a strip into the meter and touching the end to a small drop of blood on each tail. Insulin levels are quantified by enzyme-linked immunosorbent assay^[2].

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

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.7873 mL	8.9364 mL	17.8728 mL	44.6820 mL
	5 mM	0.3575 mL	1.7873 mL	3.5746 mL	8.9364 mL
	10 mM	0.1787 mL	0.8936 mL	1.7873 mL	4.4682 mL
	15 mM	0.1192 mL	0.5958 mL	1.1915 mL	2.9788 mL
	20 mM	0.0894 mL	0.4468 mL	0.8936 mL	2.2341 mL
	25 mM	0.0715 mL	0.3575 mL	0.7149 mL	1.7873 mL
	30 mM	0.0596 mL	0.2979 mL	0.5958 mL	1.4894 mL
	40 mM	0.0447 mL	0.2234 mL	0.4468 mL	1.1170 mL
	50 mM	0.0357 mL	0.1787 mL	0.3575 mL	0.8936 mL
	60 mM	0.0298 mL	0.1489 mL	0.2979 mL	0.7447 mL
	80 mM	0.0223 mL	0.1117 mL	0.2234 mL	0.5585 mL
	100 mM	0.0179 mL	0.0894 mL	0.1787 mL	0.4468 mL

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:

Ertiprotafib251303-04-5PTP 112PTP112PTP-112Inhibitorinhibitorinhibit

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Ertiprotafib (Synonyms: PTP 112)

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