COX-2/CaV2.2-IN-1
COX-2/CaV2.2-IN-1 is an orally active and selective dual COX-2/CaV2.2 inhibitor, exhibiting a COX-2 IC50 of 0.26 μM and a CaV2.2 IC50 of 0.29 μM. COX-2/CaV2.2-IN-1 suppresses inflammatory responses and inflammatory mediator (IL-6, TNF-α, NO) production. COX-2/CaV2.2-IN-1 produces pronounced analgesic effects in diverse models of inflammatory, neuropathic, and visceral pain. COX-2/CaV2.2-IN-1 can be used for the research of chronic pain.
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- Formule: C25H21F3N2O3S
- Masse moléculaire:486.51
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Stockage:
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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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
COX-2 0.26 μM (IC50) |
CaV2.2 0.29 μM (IC50) |
IL-6 |
In Vitro
COX-2/CaV2.2-IN-1 (Compound 5d) potently and selectively inhibits recombinant human COX-2 with an IC50 of 257.4 ± 166.0 nM[1].
COX-2/CaV2.2-IN-1 potently and selectively inhibits human CaV2.2 channels in transfected HEK293T cells with an IC50 of 288.7 ± 75.5 nM[1].
COX-2/CaV2.2-IN-1 (10-50 μM; 24 h) dose-dependently suppresses LPS (HY-D1056)-induced inflammatory mediator (IL-6, TNF-α, NO) production in mouse BV2 microglial cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Mouse BV2 microglial cells
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Concentration:10, 50 μM
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Incubation Time:24 h
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Result:Dose-dependently suppressed LPS-induced IL-6, TNF-α, and NO production at 10 μM and 50 μM.
Exhibited a stronger anti-inflammatory effect than Rofecoxib (HY-17372) at 10 μM, as evidenced by superior suppression of IL-6, TNF-α, and NO levels.
Parmacokinetics
In Vivo
COX-2/CaV2.2-IN-1 (62.0 μmol/kg; i.g.; single dose) reduces inflammatory pain-related paw-licking behavior in the formalin test in mice[1].
COX-2/CaV2.2-IN-1 (62.0 μmol/kg; i.g.; single dose) reduces visceral pain-related writhing behavior in mice[1].
COX-2/CaV2.2-IN-1 (62.0 μmol/kg; i.g.; single dose) reduces neuropathic pain in the CCI model in mice[1].
COX-2/CaV2.2-IN-1 (62.0 μmol/kg; i.g.; single dose) reduces cold allodynia in the PTX (HY-B0715)-induced neuropathic pain model in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (6−8 weeks old; inflammatory pain model via intraplantar CFA injection)[1]
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Dosage:30, 60,120 μmol/kg
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Administration:I.g.; single dose
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Result:Produced dose-dependent antinociceptive effects, with a median effective dose (ED50) of 41.3 μmol/kg.
Exhibited a favorable peak analgesic efficacy at 62.0 μmol/kg, with an area under the curve (AUC) of 1320.0 ± 73.2, which was significantly greater than the Rofecoxib (HY-17372) group.
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Animal Model:C57BL/6 (6−8 weeks old; neuropathic pain model via intraperitoneal PTX injection)[1]
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Dosage:62.0 μmol/kg
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Administration:I.g.; single dose
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Result:Conferred pronounced antinociceptive effects, with a significantly increased PWT compared to the vehicle group, and an AUC significantly higher than the Rofecoxib group.
Chemical Information
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Masse moléculaire 486.51
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Formule C25H21F3N2O3S
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SMILES
O=S(C1=CC=C(C=C1)N2C(C3=CC=CC=C3)=CC(COCC4=CC=C(C=C4)C(F)(F)F)=N2)(C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
COX-2/CaV2.2-IN-1 Related Classifications
HY-181612 Related Classifications
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