XY-280
XY-280 is a blood-brain barrier-penetrant ST2 inhibitor. XY-280 inhibits the binding of ST2/IL-33 (IC50 = 5.85 μM), thereby suppressing activation of the downstream NF-κB pathway and reducing the transcription and release of pro-inflammatory cytokines and chemokines. XY-280 can be used for research on neuroinflammation.
For research use only. We do not sell to patients.
- Formula: C24H28N4O2
- Molecular Weight:404.50
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
ST2 5.85 μM (IC50) |
NF-κB |
IL-6 |
IL-1β |
TNF-α |
PGE2 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:primary mouse microglial cells isolated from mouse cortex, hippocampus, and striatum
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Concentration:10 μM
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Incubation Time:pre-treated with the compound for 15 minutes, followed by stimulation with LPS (100 ng/mL) overnight
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Result:Significantly suppressed the LPS-induced release of the inflammatory lipid mediator prostaglandin E2 (PGE2) and the pro-inflammatory cytokines IL-1β and IL-6 in primary microglial cells, bringing their levels down to match those of the unstimulated control group; the release of TNF-α was also reduced.
Effectively inhibited ST2/IL-33 signaling and block downstream NF-κB activation in vitro.
Parmacokinetics
| Species | Dose | Route | T1/2 |
|---|---|---|---|
| Mice[1] | 20 mg/kg | i.p. | 10.64 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6[1]
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Dosage:20 mg/kg
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Administration:i.p.; single administration at 30 min after LPS; mice were dissected and hippocampus RNA was extracted 5 hours after LPS stimulation
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Result:In LPS-challenged mice, hippocampal mRNA expression of IL-1β, IL-6, TNF-α, CCL2, CCL3, and CCL4 was reduced relative to LPS + vehicle.
IL-1β and IL-6 mRNA were substantially suppressed, and the chemokine mRNAs CCL2, CCL3, and CCL4 were also reduced.
Chemical Information
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Molecular Weight 404.50
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Formula C24H28N4O2
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SMILES
C[C@@H]1CC[C@@H](C2=CC=C(N(C)C)C=C2)N1CC3=CC=C(C4=CC=C([N+]([O-])=O)C=C4)N3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
XY-280 Related Classifications
HY-186397 Related Classifications
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