Factor B-IN-8
Factor B-IN-8 (Compound (3R ,4R )-15) is a potent, selective and orally active factor B inhibitor with an IC50 of 10.2 nM. Factor B-IN-8 can effectively inhibit the binding of factor B to C3b and the subsequent formation of C3 convertase (C3bBb). Factor B-IN-8 can inhibit the deposition of membrane attack complex (MAC) mediated by alternativepathway with an IC50 of 59.3 nM. Factor B-IN-8 can reduce the cleavage of factor B protein and decrease the deposition of complement C3d in the glomeruli and renal tubules. Factor B-IN-8 can be used for researches of arthritis and paroxysmal nocturnal hemoglobinuria (PNH).
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- CAS No.: 3049710-19-9
- Formule: C24H25F3N2O4
- Masse moléculaire:462.46
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
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Help & FAQs
Activité biologique
Description
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax | AUC0-t | AUC0-∞ | Vss | Tmax | F |
|---|---|---|---|---|---|---|---|---|---|
| Dog[1] | 3 mg/kg | i.v. | 3.16 h | 14947 ng/mL | 8333 ng·h/mL | 9487 ng·h/mL | 1.23 L/kg | / | / |
| Dog[1] | 6 mg/kg | i.g. | 5.83 h | 4680 ng/mL | 14388 ng·h/mL | 16738 ng·h/mL | / | 0.46 h | 86.77 % |
| Rat[1] | 10 mg/kg | i.v. | 10.58 h | 16788 ng/mL | 11413 ng·h/mL | 15313 ng·h/mL | 9.18 L/kg | / | / |
| Rat[1] | 20 mg/kg | i.g. | 9.28 h | 2659 ng/mL | 8793 ng·h/mL | 13505 ng·h/mL | / | 0.38 h | 51.82 % |
Chemical Information
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CAS No. 3049710-19-9
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Masse moléculaire 462.46
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Formule C24H25F3N2O4
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SMILES
CC(C=C1OC)=C(NC=C2)C2=C1O[C@H]3[C@H](C4=CC=C(C=C4)C(O)=O)CN(CC3)CC(F)(F)F
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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)
Factor B-IN-8 Related Classifications
HY-181040 Related Classifications
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