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Purity: ≥98%
RN486 (RN-486) is a novel, potent, reversible and selective BTK (Bruton's tyrosine kinase) inhibitor with potential anti-inflammatory activity. It inhibits BTK with an IC50 of 4 nM. RN486 exhibits strong in vivo anti-inflammatory and bone-protective effects in mouse CIA and rat adjuvant-induced arthritis (AIA) models. In the AIA model, RN486 inhibits both joint and systemic inflammation either alone or in combination with methotrexate, reducing both paw swelling and inflammatory markers in the blood.
| ln Vitro |
Fcγ receptor engagement-mediated tumor necrosis factor α production in monocytes (IC50 = 7 nM), Fcε receptor cross-linking-induced degranulation in mast cells (IC50 = 2.9 nM), and B cell antigen receptor-induced expression of an activation marker, CD69, in B cells in whole blood (IC50 = 21 nM) are all blocked by RN486[1]. Convulxin stimulation led to increased production of pro-inflammatory cytokines, IL-6 and IL-8, in a co-culture system including human primary synovial FLS and activated human platelets. This effect is dose-dependently inhibited by RN486[2].
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| ln Vivo |
In rat adjuvant-induced arthritis (AIA) and mouse CIA models, RN486 has strong anti-inflammatory and bone-protective properties. In the AIA model, paw edema and inflammatory markers in the blood are decreased by RN486 (1–30 mg/kg), which also reduces joint and systemic inflammation[1].
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| 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. |
| Molecular Formula |
C35H35FN6O3
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| Molecular Weight |
606.69
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| CAS # |
1242156-23-5
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| Related CAS # |
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| SMILES |
O=C1N(C2=CC=CC(C(C=C3NC4=NC=C(N5CCN(C)CC5)C=C4)=CN(C)C3=O)=C2CO)C=CC6=C1C(F)=CC(C7CC7)=C6
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| InChi Key |
ZTUJNJAKTLHBEX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C35H35FN6O3/c1-39-12-14-41(15-13-39)26-8-9-32(37-19-26)38-30-18-25(20-40(2)34(30)44)27-4-3-5-31(28(27)21-43)42-11-10-23-16-24(22-6-7-22)17-29(36)33(23)35(42)45/h3-5,8-11,16-20,22,43H,6-7,12-15,21H2,1-2H3,(H,37,38)
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| Chemical Name |
6-cyclopropyl-8-fluoro-2-(2-hydroxymethyl-3-{1-methyl-5-[5-(4-methyl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-pyridin-3-yl}-phenyl)-2H-isoquinolin-1-one
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| Synonyms |
RN-486; RN 486; RN486;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6483 mL | 8.2414 mL | 16.4829 mL | |
| 5 mM | 0.3297 mL | 1.6483 mL | 3.2966 mL | |
| 10 mM | 0.1648 mL | 0.8241 mL | 1.6483 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Inhibitory effect of RN486 on the effector phase of immune arthritis in mice.J Pharmacol Exp Ther.2012 Apr;341(1):90-103. |
Anti-inflammatory and disease-modifying effects of RN486 in the rat AIA model.J Pharmacol Exp Ther.2012 Apr;341(1):90-103. |
Additive inhibitory effects of RN486 and MTX on inflammation and bone erosions in the rat AIA model.J Pharmacol Exp Ther.2012 Apr;341(1):90-103. |
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