CGI1746 has exquisite selectivity for Btk and inhibits both auto- and transphosphorylation steps necessary for enzyme activation. CGI1746 blocks B cell receptor-dependent B cell proliferation and in prophylactic regimens reduces autoantibody levels in collagen-induced arthritis. CGI1746 decreases cytokine levels within joints and ameliorates disease. CGI1746 shows comparable efficacy to TNFα blockade and significantly reduces clinical scores, as well as joint inflammation, in mice or rats with established arthritis.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis.
Di Paolo JA, et al. Nat Chem Biol. 2011 Jan;7(1):41-50. PMID: 21113169.
|Related BTK Products|
ONO-4059 is a highly selective, orally bioavailable BTK inhibitor with a potency (IC50) of 2.2 nM.
Acalabrutinib(ACP-196) is a selective second-generation Bruton's tyrosine kinase (BTK) inhibitor, which prevents the activation of the B-cell antigen receptor (BCR) signaling pathway.BMX, and TEC, respectively) and no activity against EGFR.
ONO-4059 (GS-4059) is highly potent and selective BTK inhibitor with an IC50 of 2.2 nM.
ONO-4059 analogue is the analog of ONO-4059, ONO-4059 is a highly potent and selective Btk inhibitor with IC50 of 23.9 nM.
RN486 is a Bruton's tyrosine kinase (Btk) inhibitor with an IC50 Value of 4.0 nM.
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