(R)-Vorbipiprant
(R)-Vorbipiprant ((R)-CR6086) is an orally active antagonist for prostaglandin E2 receptor 4 (EP4) with Ki of 16.6 nM for human EP4. (R)-Vorbipiprant inhibits PGE2 (HY-101952)-induced cAMP production with an IC50 of 22 nM. (R)-Vorbipiprant exhibits immunomodulatory and anti-angiogenic activities, and ameliorates the collagen-induced arthritis in mice.
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- CAS No.: 2502965-92-4
- Formule: C26H27F3N2O3
- Masse moléculaire:472.50
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Description
IC50 & Target
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hEP4 16.6 nM (Ki) |
Chemical Information
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CAS No. 2502965-92-4
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Masse moléculaire 472.50
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Formule C26H27F3N2O3
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SMILES
O=C(C1=CC=C(C2(CC2)NC([C@@H]3N(CCC4(C3)CC4)CC5=CC=C(C(F)(F)F)C=C5)=O)C=C1)O
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Synonyms
(R)-CR6086
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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.
Protocole
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Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)