1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. RN486

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.

For research use only. We do not sell to patients.

RN486 Chemical Structure

RN486 Chemical Structure

CAS No. : 1242156-23-5

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 174 In-stock
Solution
10 mM * 1 mL in DMSO USD 174 In-stock
Solid
1 mg USD 96 In-stock
5 mg USD 130 In-stock
10 mg USD 210 In-stock
25 mg USD 420 In-stock
50 mg USD 670 In-stock
100 mg USD 1000 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    RN486 purchased from MedChemExpress. Usage Cited in: Blood Adv. 2020 Jun 9;4(11):2439-2450.  [Abstract]

    Western blot on whole-cell lysates from B cells with indicated genotype (wild-type or C481S), inhibitor treatment (ibrutinib or RN486) and stimulation (anti-IgM and H2O2).
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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[1][2][3].

    IC50 & Target

    IC50: 4.0 nM (Btk)[1]
    Kd: 0.31 nM (Btk)[1]

    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)[1].
    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[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Molecular Weight

    606.69

    Formula

    C35H35FN6O3

    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C1C(NC2=CC=C(N3CCN(C)CC3)C=N2)=CC(C4=CC=CC(N5C=CC(C=C(C6CC6)C=C7F)=C7C5=O)=C4CO)=CN1C

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 24 mg/mL (39.56 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    (per animal)

    μL

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.87%

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.6483 mL 8.2414 mL 16.4829 mL 41.2072 mL
    5 mM 0.3297 mL 1.6483 mL 3.2966 mL 8.2414 mL
    10 mM 0.1648 mL 0.8241 mL 1.6483 mL 4.1207 mL
    15 mM 0.1099 mL 0.5494 mL 1.0989 mL 2.7471 mL
    20 mM 0.0824 mL 0.4121 mL 0.8241 mL 2.0604 mL
    25 mM 0.0659 mL 0.3297 mL 0.6593 mL 1.6483 mL
    30 mM 0.0549 mL 0.2747 mL 0.5494 mL 1.3736 mL
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    RN486 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Inquiry Information

    Product Name:
    RN486
    Cat. No.:
    HY-18018
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