PKR1 antagonist-2
PKR1 antagonist-2 is a non-peptide prokineticin receptor antagonist that preferentially binds to and blocks PK-R1 signaling while also blocking PK-R2. PKR1 antagonist-2 shifts the autoimmune response against myelin from a Th1/Th17 profile toward a Th2 profile, reducing myelin antigen-specific T cell proliferation and the production of proinflammatory cytokines (IFN-γ, TNF, IL-6, IL-17), and increasing the levels of anti-inflammatory cytokines IL-4/IL-10. PKR1 antagonist-2 significantly alleviates disease severity in relapsing-remitting and chronic experimental autoimmune encephalomyelitis (EAE). PKR1 antagonist-2 can be used in research related to multiple sclerosis .
For research use only. We do not sell to patients.
- CAS No.: 910113-34-7
- Formula: C21H24FN7O3
- Molecular Weight:441.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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]|
PKR 1 |
PKR 2 |
IL-6 |
IL-17 |
IL-4 |
IL-10 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.033 μM
Compound: 16
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Antagonist activity at human PKR1 expressed in HEK293 cells assessed as inhibition of PK1-induced calcium mobilization by FLIPR assay
Antagonist activity at human PKR1 expressed in HEK293 cells assessed as inhibition of PK1-induced calcium mobilization by FLIPR assay
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[PMID: 19375913] |
In Vitro
PKR1 antagonist-2 (Compound PC7) (500 μg/kg, i.p., daily) is administered for in vivo prophylactic injection, after which mouse draining lymph node cells are collected and restimulated in vitro with myelin antigens (PLP139-151 (HY-P0129) or MOG35-55 (HY-P1240)), resulting in significantly reduced antigen-specific T cell proliferation and decreased production of inflammatory Th1/Th17 cytokines (IFN-γ, TNF, IL-6, IL-17), while the levels of anti-inflammatory Th2 cytokines IL-4/IL-10 are elevated[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SJL mice (female, 8-12 weeks old) were immunized subcutaneously with PLP139-151 (100 μg/mouse) and complete Freund's adjuvant (CFA) to induce relapsing-remitting EAE[1]
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Dosage:500 μg/kg
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Administration:i.p.; daily initiate; d on the day of immunization (day 0) for the preventive study, or upon the onset of initial symptoms (day 11) for the therapeutic study
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Result:The group injected on the day of immunization (day 0) showed an incidence of 90% (control 100%), an onset time of 11.4 days (control 10.4 days), a peak disease score of 2.2 (control 3.5), and a cumulative disease score of 21.2 (control 45.1).
The group injected at the onset of initial symptoms (day 11) showed an incidence of 100%, a peak disease score of 2.6 (control 3.4), and a cumulative disease score of 42.3 (control 69.6).
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Animal Model:Female C57BL/6 mice were immunized subcutaneously with MOG35-55 (100 μg/mouse) and CFA, followed by intraperitoneal injection of pertussis toxin (PTX, 400 ng/mouse) to induce chronic EAE[1]
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Dosage:500 μg/kg
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Administration:i.p.; daily initiate; d on the day of immunization (day 0) for the preventive study, or upon the onset of initial symptoms (day 12) for the therapeutic study.
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Result:The group injected on the day of immunization (day 0) showed an incidence of 90% (control 100%), an onset time of 11.4 days (control 10.4 days), a peak disease score of 2.2 (control 3.5), and a cumulative disease score of 21.2 (control 45.1).
The group injected at the onset of initial symptoms (day 11) showed an incidence of 100%, a peak disease score of 2.6 (control 3.4), and a cumulative disease score of 42.3 (control 69.6).
- Naïve CD4+ T-cell subset differentiation/polarization
- BrdU Incorporation Assay
- Somatic Cell Culture
- CFSE Dye Dilution Proliferation Assay
- Dye-dilution cell tracking and proliferation staining
- CCK-8/WST-8 Cell Proliferation Assay
- Protocol for Cell Cycle
- Cell Counting-Based Growth Curve Assay
- Research Protocol for Inflammation-related Diseases
- Colony Formation (Clonogenic) Assay
- Research Protocol for Cancer Immunology
- Cell Viability Determination by MTT Colorimetric Assay
- EdU Incorporation Assay (Click Chemistry-Based DNA Synthesis Measurement)
- Ki-67 Immunostaining Proliferation Assay
- PCNA Immunodetection Proliferation Assay
- LPS-Induced Endotoxemia/Systemic Inflammation
- Protocol for Cell Counting and Cell Density Analysis
- MTT Cell Proliferation Assay
Chemical Information
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CAS No. 910113-34-7
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Molecular Weight 441.47
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Formula C21H24FN7O3
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SMILES
O=C1N=C(NCCNC(=N)N)N(C(=O)N1CC2=CC=C(F)C=C2)CC3=CC=C(OC)C=C3
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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)
PKR1 antagonist-2 Related Classifications
HY-153201 Related Classifications
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