Free shipping on all orders over $ 500

RN486

Cat. No. M3704
RN486 Structure
Synonym:

RN-486

Size Price Availability Quantity
2mg USD 120 In stock
5mg USD 160 In stock
10mg USD 280 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

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 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.

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.

Related BTK Products
GDC-0853

GDC-0853 is an orally BTK inhibitor with potential antineoplastic activity.

Btk inhibitor 2

Btk inhibitor 2 (BGB-3111) is a Brutons tyrosine kinase (BTK) inhibitor.

BMS-935177

BMS-935177 is a potent, reversible Bruton's Tyrosine Kinase (BTK) inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective.

LFM-A13

LFM-A13 is a specific Bruton's tyrosine kinase (BTK) inhibitor with IC50 of 2.5 μM.

ONO-4059

ONO-4059 is a highly selective, orally bioavailable BTK inhibitor with a potency (IC50) of 2.2 nM.

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.