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RN486

Cat. No. M3704
RN486 Structure
Synonym:

RN-486

Size Price Availability Quantity
2mg USD 108  USD120 In stock
5mg USD 144  USD160 In stock
10mg USD 252  USD280 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

RN486 is a potently and selectively inhibitor. RN486 inhibited the Btk enzyme and displayed functional activities in human cell-based assays in multiple cell types. RN486 blocks Fcε receptor cross-linking-induced degranulation in mast cells (IC(50) = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC(50) = 7.0 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC(50) = 21.0 nM). RN486 produced robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 inhibited both joint and systemic inflammation either alone or in combination with methotrexate, reducing both paw swelling and inflammatory markers in the blood.

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 606.69
Formula C35H35FN6O3
CAS Number 1242156-23-5
Purity >98%
Solubility DMSO
Storage at -20°C
References

RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents.
Xu D, et al. J Pharmacol Exp Ther. 2012 Apr;341(1):90-103. PMID: 22228807.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: RN486, RN-486 supplier, BTK, inhibitors

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