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R1487 Hydrochloride

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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

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.
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2 mg$66In Stock
5 mg$1075 days
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Purity:99.42%
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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
p38α:10 nM, p38α:0.2 nM (Kd), IL-1β:200 nM, p38β:29 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]
AliasR 1487 Hydrochloride
Chemical Properties
Molecular Weight424.83
FormulaC19H19ClF2N4O3
Cas No.449808-64-4
SmilesCl.O=C1C(OC2=CC=C(F)C=C2F)=CC=3C=NC(=NC3N1C)NC4CCOCC4
Relative Density.no data available
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: < 1 mg/mL (insoluble)
DMSO: 16 mg/mL (37.66 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3539 mL11.7694 mL23.5388 mL117.6941 mL
5 mM0.4708 mL2.3539 mL4.7078 mL23.5388 mL
10 mM0.2354 mL1.1769 mL2.3539 mL11.7694 mL
20 mM0.1177 mL0.5885 mL1.1769 mL5.8847 mL

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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:
TargetMol | Animal experimentsFor 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% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | 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 DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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