(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. Nr.: 2502965-92-4
- Formel: C26H27F3N2O3
- Molecular Weight:472.50
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
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hEP4 16.6 nM (Ki) |
Chemical Information
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CAS. Nr. 2502965-92-4
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Molecular Weight 472.50
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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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.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)