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CGI1746

Cat. No. M3620
CGI1746 Structure
Synonym:

CGI-1746

Size Price Availability Quantity
10mM*1mL in DMSO USD 85  USD85 In stock
5mg USD 70  USD70 In stock
10mg USD 110  USD110 In stock
25mg USD 170  USD170 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 579.69
Formula C34H37N5O4
CAS Number 910232-84-7
Solubility (25°C) DMSO ≥ 44 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Di Paolo JA, et al. Nat Chem Biol. Specific Btk inhibition suppresses B cell- and myeloid cell-mediated arthritis.

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

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