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R1487

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Catalog No. T7667Cas No. 449811-92-1

R1487 is an orally bioavailable and highly selective p38α mitogen-activated protein kinase inhibitor.

R1487

R1487

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Purity: 99.77%
Catalog No. T7667Cas No. 449811-92-1
R1487 is an orally bioavailable and highly selective p38α mitogen-activated protein kinase inhibitor.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$133In StockIn Stock
5 mg$298In StockIn Stock
10 mg$453In StockIn Stock
25 mg$747In StockIn Stock
50 mg$1,050In StockIn Stock
100 mg$1,420-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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Purity:99.77%
Appearance:Solid
Color:White
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Product Introduction

R1487 AI Summary
R1487 exhibits a broad spectrum of bioactivities. It shows potent inhibitory effects on a variety of kinases and proteins, including p38alpha, P38beta, ADCK3, CSNK1epsilon, DDR1, GAK, JNK1, JNK2, JNK3, NLK, RSK2, and STK36, with Kd values ranging from 0.2 nM to 1000.0 nM. It also inhibits TNF-alpha-induced IL-6 and IL-1beta production and LPS-induced TNF-alpha and IL-6 production. The compound demonstrates analgesic activity in a rat model and has favorable pharmacokinetic properties such as a Tmax of 4.67 hr, Cmax of 4016.79 nM, a half-life of 22.5 hr, an AUC of 29400.0 ng.hr.mL-1, an oral bioavailability of 51.6%, and clearance of 3.05 mL.min-1.kg-1. While it binds extensively to plasma proteins in cynomolgus monkeys, it has low aqueous solubility and permeability in human Caco-2 cells. Additionally, R1487 reveals lower affinity for kinases such as CLK2, PLK3, CSNK1G2, PRKCZ, STK3 with Ki values exceeding 7943.28 nM, and for targets like CDC42BPA, AKT3, CDK5 with Ki values above 10000.0 nM. It shows moderate inhibitory activity against Plasmodium falciparum proliferation with potencies ranging from 9432.9 nM to 14950.2 nM. The compound has a LogD7.4 value of 2.76 and a solubility of 20400.0 nM at pH 7.4. Importantly, R1487 demonstrates potent antiviral activity, inhibiting the SARS-CoV-2 3CL-Pro protease by 92.81% at 20µM, and reducing SARS-CoV-2 induced cytotoxicity in VERO-6 cells at 10 µM with an inhibition rate of -0.09% after 48 hours. These attributes highlight its potential as an antiviral agent, particularly against SARS-CoV-2..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
R1487 is an orally bioavailable and highly selective p38α mitogen-activated protein kinase inhibitor.
Chemical Properties
Molecular Weight388.37
FormulaC19H18F2N4O3
Cas No.449811-92-1
SmilesCn1c2nc(NC3CCOCC3)ncc2cc(Oc2ccc(F)cc2F)c1=O
Relative Density.1.425 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: Slightly soluble

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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:
TargetMol | Animal experiments 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 DMSOTargetMol | 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 DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent 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 ddH2OTargetMol | 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.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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

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