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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
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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 | Availability | Quantity |
|---|---|---|---|
| 2 mg | $66 | In Stock | |
| 5 mg | $107 | 5 days |
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Purity:99.42%
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Product Introduction
Bioactivity
Chemical Properties
| 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:0.2 nM (Kd), p38α:10 nM, p38β:29 nM (Kd), IL-1β:200 nM |
| 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] |
| Alias | R 1487 Hydrochloride |
| 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. | |||||||||||||||||||||||||
| Solubility Information | H2O: < 1 mg/mL (insoluble) DMSO: 16 mg/mL (37.66 mM), Sonication is recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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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 . A total of 10 animals were administered, and the formula you used is 5% 
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 DMSO (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.
(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 main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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