PAR2 modulator-1
PAR2 modulator-1 is a biased protease-activated receptor 2 (PAR2) inhibitor. PAR2 modulator-1 blocks the PAR2-dependent MAPK signaling pathway with an IC50 value of 8.5 μM, without altering the PAR2-dependent Ca2+ signaling pathway. PAR2 modulator-1 blocks pain responses induced by PAR2 agonists. PAR2 modulator-1 can be used in the research of chronic pain.
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- No. CAS: 2378159-28-3
- Fòrmula: C27H41N5O5
- Peso molecular:515.64
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
PAR2 8.5 μM (IC50) |
In Vitro
PAR2 modulator-1 (C781) (30-300 nM) inhibits 2AT-induced PAR2 responses in a dose-dependent manner, with almost complete inhibition observed at 300 nM[1].
PAR2 modulator-1 (100 nM-100 μM) significantly reduces MAPK phosphorylation in cells expressing PAR2, with an IC50 of 8.5 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PAR2 modulator-1 (30 mg/kg; i.p.; single dose) effectively blocks 2AT-induced systemic mechanical hyperalgesia.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1]
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Dosage:1 μg
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Administration:intraplantar injection; single dose
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Result:Effectively blocked 2AT-induced persistent mechanical hypersensitivity and did not itself cause pain.
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Animal Model:Mice[1]
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Dosage:30 mg/kg
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Administration:i.p.; single dose
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Result:Effectively blocked 2AT-induced systemic mechanical hypersensitivity.
Chemical Information
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No. CAS 2378159-28-3
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Peso molecular 515.64
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Fòrmula C27H41N5O5
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SMILES
O=C(C1=CC=CO1)N2C3N(C([C@H](C2)NC(CC(C)C)=O)=O)[C@H](C(N(C3)CC4CCNCC4)=O)CC(C)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PAR2 modulator-1 Related Classifications
HY-171096 Related Classifications
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