G-744
G-744 is a highly potent, selective and orally active Btk inhibitor with an IC50 of 2 nM. G-744 is metabolically stable, well tolerated and efficacious to treat arthritis.
For research use only. We do not sell to patients.
- CAS No.: 1346669-54-2
- Formula: C29H29N5O3S
- Molecular Weight:527.64
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
IC50: 2 nM (Btk), 64 nM (CD86)[1].
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Lewis rat based CIA models[1].
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Dosage:6.25, 12.25, 25 mg/kg.
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Administration:Orally, b.i.d., daily for 17 days.
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Result:All three doses resulted in a significant dose-dependent inhibition of ankle thickness between day 10 and day 17 (onset of increase in ankle diameter on day 9).
Chemical Information
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CAS No. 1346669-54-2
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Molecular Weight 527.64
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Formula C29H29N5O3S
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SMILES
CN(C1=O)C=C(C2=CC=CC(N3C(C(SC4=C5CC(C)(C)C4)=C5CC3)=O)=C2CO)C=C1NC6=CC=NC=N6
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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.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)