PPARγ phosphorylation inhibitor 1

Name: PPARγ phosphorylation inhibitor 1
Brand: MedChemExpress
SKU: HY-147705
Rating: 4.5 (1 reviews)

Cat. No.: HY-147705 Purity: 99.80%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

PPARγ phosphorylation inhibitor 1 (Compound 10) is a potent PPARγ binder with the IC₅₀ of 24 nM. PPARγ phosphorylation inhibitor 1 inhibits CDK5-mediated phosphorylation of PPARγ Ser273 with the IC₅₀ of 160 nM. PPARγ phosphorylation inhibitor 1 displays negligible PPARγ agonism in a reporter gene assay. Antidiabetic effects.

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

PPARγ phosphorylation inhibitor 1 Chemical Structure

CAS No. : 2882975-84-8

Size	Price	Stock	Quantity
5 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 680	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1350	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2150	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3500	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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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

IC₅₀ & Target^[1]

PPARγ

24 nM (IC₅₀)

In Vivo

PPARγ phosphorylation inhibitor 1 (compound 10) (100 μM/kg; i.g.; lean C57/BL6 mice) has a PK profile amenable to in vivo administration^[1].
PPARγ phosphorylation inhibitor 1 (compound 10) (10-100 μM/kg; i.g.; daily, for 7 days) demonstrates a modest improvement of insulin sensitivity in ob/ob mice^[1].

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

Animal Model:	Lean C57/BL6 mice^[1]
Dosage:	100 μM/kg
Administration:	Oral gavage
Result:	Exhibited good pharmacokinetic profiles with oral bioavailability (109%), C_max (167 μM) and t_1/2 (5 h).

Animal Model:	ob/ob mouse model of diabetes^[1]
Dosage:	10 and 100 μM/kg
Administration:	Oral gavage; Daily, for 7 days
Result:	Improved insulin sensitivity and did not impact the body weight.

Molecular Weight

441.26

Formula

C₂₂H₁₄Cl₂N₂O₄

CAS No.

2882975-84-8

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NN(C(C2=C1C=CC(OC3=CC=CC=C3)=C2)=O)CC4=CC(Cl)=C(C=C4)Cl)O

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 (226.62 mM; ultrasonic and warming and heat to 60°C; 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	2.2662 mL	11.3312 mL	22.6624 mL
5 mM	0.4532 mL	2.2662 mL	4.5325 mL
10 mM	0.2266 mL	1.1331 mL	2.2662 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: ≥ 5 mg/mL (11.33 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (11.33 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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: 99.80%

Select Batch:

Data Sheet (274 KB) SDS (252 KB)

COA (249 KB) HNMR (144 KB) RP-HPLC (248 KB) LCMS (235 KB)

Handling Instructions (2659 KB)

References

[1]. Gavin O'Mahony, et al. Discovery by Virtual Screening of an Inhibitor of CDK5-Mediated PPARγ Phosphorylation. ACS Med Chem Lett. 2022 Mar 11;13(4):681-686. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.2662 mL	11.3312 mL	22.6624 mL	56.6559 mL
	5 mM	0.4532 mL	2.2662 mL	4.5325 mL	11.3312 mL
	10 mM	0.2266 mL	1.1331 mL	2.2662 mL	5.6656 mL
	15 mM	0.1511 mL	0.7554 mL	1.5108 mL	3.7771 mL
	20 mM	0.1133 mL	0.5666 mL	1.1331 mL	2.8328 mL
	25 mM	0.0906 mL	0.4532 mL	0.9065 mL	2.2662 mL
	30 mM	0.0755 mL	0.3777 mL	0.7554 mL	1.8885 mL
	40 mM	0.0567 mL	0.2833 mL	0.5666 mL	1.4164 mL
	50 mM	0.0453 mL	0.2266 mL	0.4532 mL	1.1331 mL
	60 mM	0.0378 mL	0.1889 mL	0.3777 mL	0.9443 mL
	80 mM	0.0283 mL	0.1416 mL	0.2833 mL	0.7082 mL
	100 mM	0.0227 mL	0.1133 mL	0.2266 mL	0.5666 mL