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R1487 Hydrochloride

Name: R1487 Hydrochloride
Brand: TargetMol
SKU: T7162
Price: 66 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T7162Cas No. 449808-64-4

Alias R 1487 Hydrochloride

R1487 Hydrochloride is an orally available, selective and potent inhibitor of mitogen-activated protein kinase (p38α) for the study of metabolic diseases.

R1487 Hydrochloride

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Purity: 99.42%

Catalog No. T7162Alias R 1487 HydrochlorideCas No. 449808-64-4

R1487 Hydrochloride is an orally available, selective and potent inhibitor of mitogen-activated protein kinase (p38α) for the study of metabolic diseases.

Pack Size	Price	USA Warehouse	Global Warehouse	Quantity
2 mg	$66	-	In Stock
5 mg	$107	5 days	5 days

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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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Purity:99.42%

Appearance:Solid

Color:Yellow

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Product Introduction

Bioactivity

Description	R1487 Hydrochloride is an orally available, selective and potent inhibitor of mitogen-activated protein kinase (p38α) for the study of metabolic diseases.
Targets&IC50	p38β:29 nM (Kd), IL-1β:200 nM, p38α:10 nM, p38α:0.2 nM (Kd)
In vitro	R1487 Hydrochloride is a highly potent and selective inhibitor of p38α with Kd values of 0.2 nM for p38α and 29 nM for p38β. R1487 Hydrochloride has an IC50 value of 10 nM for inhibition of p38α and 200 nM for inhibition of TNFα-induced IL-1β production. R1487 Hydrochloride inhibited p38α with an IC50 value of 10 nM and TNFα-induced IL-1β production with an IC50 value of 200 nM. R1487 Hydrochloride was able to inhibit TNFα production in a human monocyte cell line (THP-1) and effectively inhibited LPS-induced IL-1β production in human whole blood samples. [1]
In vivo	After oral administration of R1487 Hydrochloride, its serum levels of TNFα and IL-1β showed significant dose-dependent inhibition. At a dose of 10 mg/kg orally, the bioavailability of R1487 Hydrochloride in monkeys, mice and dogs reached 51.6%, 29.3% and 10.3%, respectively. [1]
Synonyms	R 1487 Hydrochloride

Chemical Properties

Molecular Weight	424.83
Formula	C₁₉H₁₉ClF₂N₄O₃
Cas No.	449808-64-4
Smiles	Cl.O=C1C(OC2=CC=C(F)C=C2F)=CC=3C=NC(=NC3N1C)NC4CCOCC4
Relative Density.	no data available

Storage & Solubility Information

Storage

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

Solubility Information

H2O: < 1 mg/mL (insoluble)

DMSO: 16 mg/mL (37.66 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.71 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	2.3539 mL	11.7694 mL	23.5388 mL	117.6941 mL
5 mM	0.4708 mL	2.3539 mL	4.7078 mL	23.5388 mL
10 mM	0.2354 mL	1.1769 mL	2.3539 mL	11.7694 mL
20 mM	0.1177 mL	0.5885 mL	1.1769 mL	5.8847 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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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