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CGI1746

Cat. No. M3620
CGI1746 Structure
Synonym:

CGI-1746

Size Price Availability Quantity
10mM*1mL in DMSO USD 76.5  USD85 In stock
5mg USD 67.5  USD75 In stock
10mg USD 108  USD120 In stock
25mg USD 193.5  USD215 In stock
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Quality Control
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 579.69
Formula C34H37N5O4
CAS Number 910232-84-7
Purity 99.74%
Solubility DMSO ≥ 44 mg/mL
Storage at -20°C
References

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.

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Keywords: CGI1746, CGI-1746 supplier, BTK, inhibitors

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