RN486 free base · Synonyms: RN-486 · RN 486

RN486 is a potent, selective and orally active Btk inhibitor.

For research use only. Not for human or veterinary use.

Target Btk

Research area Inflammation/Immunology

Purity >98% Stock Inquire

Data Sheet SDS COA

RN486 structure

CAS No.: 1242156-23-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 520.00	BP-02474-250mg	In stock	Get quote
500 mg	USD 832.00	BP-02474-500mg	In stock	Get quote
1 g	USD 1,330.00	BP-02474-1g	In stock	Get quote
2 g	USD 2,120.00	BP-02474-2g	In stock	Get quote
3 g	USD 2,550.00	BP-02474-3g	In stock	Get quote
5 g	USD 3,400.00	BP-02474-5g	In stock	Get quote
10 g	Inquire	BP-02474-10g	In stock	Inquire

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Description

RN486 is a potent, selective and orally active Btk inhibitor with an IC50 of 4.0 nM and a Kd of 0.31 nM. RN486 is less active for other kinases. RN486 can be used for rheumatoid arthritis and systemic lupus erythematosus research .

Biological activity

In Vitro RN486 blocks Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC50 = 7 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC50 = 21 nM). In a co-culture system consisting of human primary synovial FLS and activated human platelets, convulxin stimulation resulted in elevated production of pro-inflammatory cytokines, IL-6 and IL-8, an effect which is dose-dependently blocked by RN486. In Vivo RN486 produces robust anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 (1-30 mg/kg) inhibits both joint and systemic inflammation, reducing both paw swelling and inflammatory markers in the blood.

Identifiers

SMILES: CN1CCN(CC1)C1=CN=C(NC2=CC(=CN(C)C2=O)C2=C(CO)C(=CC=C2)N2C=CC3=C(C2=O)C(F)=CC(=C3)C2CC2)C=C1
InChIKey: ZTUJNJAKTLHBEX-UHFFFAOYSA-N

Specifications

MW (average): 606.6892
Formula: C₃₅H₃₅FN₆O₃
CAS No.: 1242156-23-5
Physical state: Solid
Color: Off-white to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 year;

Solubility

Soluble in DMSO

Documents

References

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

[2].Hsu J, et al. Bruton's Tyrosine Kinase mediates platelet receptor-induced generation of microparticles: a potential mechanism for amplification of inflammatory responses in rheumatoid arthritis synovial joints. Immunol Lett. 2013 Feb;150(1-2):97-104.

[3].Mina-Osorio P, et al. Suppression of glomerulonephritis in lupus-prone NZB × NZW mice by RN486, a selective inhibitor of Bruton's tyrosine kinase. Arthritis Rheum. 2013 Sep;65(9):2380-91.

Same target

Search Btk

Same research area

Search Inflammation/Immunology