MRS4738
MRS4738 is a human P2Y14-targeted inhibitor with an IC50 of 3.11 nM. MRS4738 suppresses inflammatory responses of pulmonary neutrophils and lymphocytes, reduces airway eosinophil accumulation, and alleviates mechanical hyperalgesia. MRS4738 can be applied to the research on the mechanisms of diseases associated with pulmonary inflammation, neuropathic pain and asthma.
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- No. CAS: 2801625-42-1
- Fòrmula: C30H24F3NO2
- Peso molecular:487.51
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Almacenamiento:
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
hP2Y14R 3.11 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
11 μM
Compound: 15
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Cytotoxicity against human HepG2 cells
Cytotoxicity against human HepG2 cells
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[PMID: 35113556] |
In Vitro
MRS4738 potently inhibits human P2Y14 receptor binding with an IC50 of 3.11 nM[1].
MRS4738 potently inhibits fluorescent antagonist binding to hP2Y14R-CHO cells with an IC50 of 3.11 nM[2].
MRS4738 inhibits fluorescent antagonist binding to mP2Y14R-HEK293 cells with an IC50 of 33.9 nM, showing lower affinity for mouse P2Y14R than human P2Y14R[2].
MRS4738 binds to the σ2 receptor with a Ki of 0.71 μM and shows minimal other off-target receptor binding[2].
MRS4738 (>30 μM; 24 h, 120 min) is stable in simulated gastric fluid, does not inhibit major CYP isoforms or hERG activity, and has moderate plasma and microsomal stability in mouse, rat, and human systems[2].
MRS4738 potently inhibits fluorescent antagonist binding to hP2Y14R-expressing CHO cells with an IC50 of 3.11 nM, and inhibits mP2Y14R binding with an IC50 of 33.9 nM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
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/6J (male, 6-12 weeks of age)[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily; 6 days
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Result:Significantly reduced total leukocyte counts (P < 0.001) in BALF.
Significantly reduced neutrophil counts (P < 0.05) in BALF.
Significantly reduced macrophage counts (P < 0.05) in BALF.
Significantly reduced lymphocyte counts (P < 0.001) in BALF.
Showed no significant differences in BALF concentrations of TNF-α, IL-1α, IL-1β, IFN-γ, IL-6, and CXCL1 compared to vehicle-treated mice.
Chemical Information
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No. CAS 2801625-42-1
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Peso molecular 487.51
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Fòrmula C30H24F3NO2
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SMILES
OC(C1=CC2=CC(C3=CC=C(C=C3)C(F)(F)F)=CC=C2C(C4=CC=C([C@@H]5[C@@H]6C[C@@H](NC6)C5)C=C4)=C1)=O
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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
[1]. Whitehead GS, et al. Effects of Purinergic Receptor Deletion or Pharmacologic Modulation on Pulmonary Inflammation in Mice. ACS pharmacology & translational science. 2022 Oct 14;5(10):973-984. [Content Brief]
[2]. Wen Z, et al. Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2YR Antagonist. Journal of medicinal chemistry. 2022 Feb 24;65(4):3434-3459. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MRS4738 Related Classifications
HY-143890 Related Classifications
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