1. Epigenetics
    Stem Cell/Wnt
    Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
    Immunology/Inflammation
  2. JAK
    Interleukin Related
    IFNAR
  3. Deucravacitinib

Deucravacitinib  (Synonyms: BMS-986165)

Cat. No.: HY-117287 Purity: 99.79%
COA Handling Instructions

Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis.

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

Deucravacitinib Chemical Structure

Deucravacitinib Chemical Structure

CAS No. : 1609392-27-9

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Solution
10 mM * 1 mL in DMSO USD 209 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 209 In-stock
Solid
5 mg USD 190 In-stock
10 mg USD 350 In-stock
25 mg USD 550 In-stock
50 mg USD 850 In-stock
100 mg USD 1350 In-stock
200 mg USD 2250 In-stock
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Customer Review

Based on 12 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Deucravacitinib purchased from MCE. Usage Cited in: Cell Death Differ. 2021 Feb;28(2):748-763.  [Abstract]

    Cells are treated with the allosteric TYK2 inhibitor BMS-986165 (TYK2 Inh.). BMS-986165 dose-dependently inhibits upregulation of CASP5 in response to LPS in U937 macrophages. CASP4 is constitutively expressed and not further upregulated by LPS.

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    Description

    Deucravacitinib (BMS-986165) is a highly selective, orally bioavailable allosteric TYK2 inhibitor for the treatment of autoimmune diseases, which selectively binds to TYK2 pseudokinase (JH2) domain (IC50=1.0 nM) and blocks receptor-mediated Tyk2 activation by stabilizing the regulatory JH2 domain. Deucravacitinib inhibits IL-12/23 and type I IFN pathways. Deucravacitinib, the FDA's world first de novo deuterium, is available for study in moderate to severe plaque psoriasis[1][2].

    IC50 & Target[1]

    Tyk2 JH2

    0.2 nM (IC50)

    JAK1 JH2

    1 nM (IC50)

    IL-12

     

    IL-23

     

    In Vitro

    Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
    Potential advantages of deuterated compounds:
    (1) Extend the half-life in vivo. Deuterated compounds may be able to prolong the pharmacokinetic characteristics of the compound, that is, prolong the half-life in vivo. This can improve compound safety, efficacy and tolerability, and increase ease of administration.
    (2) Improve oral bioavailability. Deuterated compounds may reduce the degree of unwanted metabolism (first-pass metabolism) in the gut wall and liver, allowing a greater proportion of the unmetabolized drug to reach its target site of action. High bioavailability determines its activity at low doses and better tolerance.
    (3) Improve metabolic characteristics. Deuterated compounds may reduce the formation of toxic or reactive metabolites and improve drug metabolism.
    (4) Improve drug safety. Deuterated compounds may reduce or eliminate adverse side effects of pharmaceutical compounds and are safe.
    (5) Preserve the therapeutic properties. Deuterated compounds are expected to retain similar biochemical potency and selectivity to hydrogen analogs in previous studies.

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

    Clinical Trial
    Molecular Weight

    425.46

    Appearance

    Solid

    Formula

    C20H19D3N8O3

    CAS No.
    SMILES

    O=C(C1=NN=C(NC(C2CC2)=O)C=C1NC3=CC=CC(C4=NN(C)C=N4)=C3OC)NC([2H])([2H])[2H]

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 37.5 mg/mL (88.14 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3504 mL 11.7520 mL 23.5040 mL
    5 mM 0.4701 mL 2.3504 mL 4.7008 mL
    10 mM 0.2350 mL 1.1752 mL 2.3504 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  50% PEG300    50% saline

      Solubility: 10 mg/mL (23.50 mM); Clear solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% saline

      Solubility: 3.83 mg/mL (9.00 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.08 mg/mL (4.89 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.08 mg/mL (4.89 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.79%

    References
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    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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    Product Name:
    Deucravacitinib
    Cat. No.:
    HY-117287
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