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CMPD101

Name: CMPD101
Brand: TargetMol
SKU: T14989
Price: 319 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T14989Cas No. 865608-11-3

CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively.

CMPD101

🥰Excellent

Purity: 99.04%

Catalog No. T14989Cas No. 865608-11-3

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$40	In Stock	In Stock
2 mg	$54	In Stock	In Stock
5 mg	$86	In Stock	In Stock
10 mg	$143	In Stock	In Stock
25 mg	$319	-	In Stock
50 mg	Preferential	-	In Stock
1 mL x 10 mM (in DMSO)	$88	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.04%

Resource Download

COA HNMR LCMS

Product Introduction

Bioactivity

Description	CMPD101 is a membrane-permeable small-molecule inhibitor of GRK2/3 (IC50: 18 nM and 5.4 nM). Which can be used for the study of heart failure. CMPD101 exhibits less selectively against GRK1, GRK5, ROCK-2 and PKCα with IC50s of 3.1 μM , 2.3 μM, 1.4 μM and 8.1 μM, respectively.
Targets&IC50	GRK2:18 nM, ROCK2:1.4 μM, PKCα:8.1 μM, GRK3:5.4 nM
In vitro	CMPD101 (100 μM; pre-20 mins) inhibit the internalization of β2AR, significantly reduces the isoproterenol-induced formation of clathrin-coated vesicles and the β2AR-GFP fusion protein remained on the plasma membrane in HEK-B2 cell line[1]. CMPD101 (3-30 μM; pre-30 minutes) does not influence the DAMGO-induced increase in ERK1/2 and Elk-1 phosphorylation, at 30?μM. This compound produces a small increase in basal ERK1/2 phosphorylation in HEK 293 cells expressing HA-MOPrs. CMPD101 (3-30 μM; pre-30 minutes) produced a robust phosphorylation of Ser375. Which is partially inhibited by pretreatment of cells for 30 minutes with 3 μM Cmpd101 and fully blocked by pretreatment with 30 μM Cmpd101and it also inhibits phosphorylation of MOPr at Thr370, Thr376, and Thr379 residues[2].

Chemical Properties

Molecular Weight	466.46
Formula	C₂₄H₂₁F₃N₆O
Cas No.	865608-11-3
Smiles	Cn1c(CNc2cccc(c2)C(=O)NCc2ccccc2C(F)(F)F)nnc1-c1ccncc1
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (535.95 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (10.72 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1438 mL	10.7190 mL	21.4381 mL	107.1903 mL
5 mM	0.4288 mL	2.1438 mL	4.2876 mL	21.4381 mL
10 mM	0.2144 mL	1.0719 mL	2.1438 mL	10.7190 mL
20 mM	0.1072 mL	0.5360 mL	1.0719 mL	5.3595 mL
50 mM	0.0429 mL	0.2144 mL	0.4288 mL	2.1438 mL
100 mM	0.0214 mL	0.1072 mL	0.2144 mL	1.0719 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc