R1487 Hydrochloride

SKU: orb1685518

Description

R1487 Hydrochloride

Research Area

Cell Biology, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	449808-64-4
MW	424.83
Purity	99.42%
Formula	C₁₉H₁₉ClF₂N₄O₃
SMILES	Cl.O=C1C(OC2=CC=C(F)C=C2F)=CC=3C=NC(=NC3N1C)NC4CCOCC4
Target	Autophagy,p38 MAPK
Solubility	H2O:< 1 mg/mL (insoluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.71 mM);DMSO:16 mg/mL (37.66 mM)

Bioactivity

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Target IC50	IL-1β:200 nM\|p38β:29 nM (Kd)\|p38α:0.2 nM (Kd)\|p38α:10 nM
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 Read more...
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. Read more...

Storage & Handling

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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.
Disclaimer	For research use only

Alternative Names

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Autophagy, IL-1β, TNFα, R1487 (Hydrochloride), R1487 Hydrochloride, R1487, R-1487, R-1487 Hydrochloride, THP-1, R 1487, R 1487 Hydrochloride, p38MAPK, p38α, p38 MAPK

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Compound Identifiers

PubChem CID

54580957 ↗

Key Properties

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No computed properties available.

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