Deucravacitinib (Synonyms: BMS-986165)

Name: Deucravacitinib
Brand: MedChemExpress
SKU: HY-117287
Rating: 5.0 (21 reviews)

Cat. No.: HY-117287 Purity: 99.87%: Data Sheet
SDS

COA
Handling Instructions
FAQs
Technical Support

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

CAS No. : 1609392-27-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 21 publication(s) in Google Scholar

Other Forms of Deucravacitinib:

Deucravacitinib hydrochloride Get quote

20 Publications Citing Use of MCE Deucravacitinib

: Deucravacitinib purchased from MedChemExpress. 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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JAK1 JAK2 JAK3 Tyk2 JAK

View All Interleukin Related Isoform Specific Products:

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

Biological Activity
Purity & Documentation
References
Customer Review

Description

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.

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

Clinical Trial

Molecular Weight

425.46

Formula

C₂₀H₁₉D₃N₈O₃

CAS No.

1609392-27-9

Appearance

Solid

Color

Off-white to light yellow

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	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 33.33 mg/mL (78.34 mM; Need ultrasonic; 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	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

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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (23.50 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.87%

Select Batch:

Data Sheet (290 KB) SDS (418 KB)

COA (253 KB) HNMR (273 KB) LCMS (91 KB)

Handling Instructions (2659 KB)

References

[1]. Wrobleski ST, et al. Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165. J Med Chem. 2019 Jul 18. [Content Brief]

[2]. Catlett I, et al. SAT0226 A first-in-human, study of BMS-986165, a selective, potent, allosteric small molecule inhibitor of tyrosine kinase 2. Annals of the Rheumatic Diseases 2017;76:859.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.3504 mL	11.7520 mL	23.5040 mL	58.7599 mL
	5 mM	0.4701 mL	2.3504 mL	4.7008 mL	11.7520 mL
	10 mM	0.2350 mL	1.1752 mL	2.3504 mL	5.8760 mL
	15 mM	0.1567 mL	0.7835 mL	1.5669 mL	3.9173 mL
	20 mM	0.1175 mL	0.5876 mL	1.1752 mL	2.9380 mL
	25 mM	0.0940 mL	0.4701 mL	0.9402 mL	2.3504 mL
	30 mM	0.0783 mL	0.3917 mL	0.7835 mL	1.9587 mL
	40 mM	0.0588 mL	0.2938 mL	0.5876 mL	1.4690 mL
	50 mM	0.0470 mL	0.2350 mL	0.4701 mL	1.1752 mL
	60 mM	0.0392 mL	0.1959 mL	0.3917 mL	0.9793 mL

Deucravacitinib Related Classifications

Inflammation/Immunology

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.

Keywords:

Deucravacitinib1609392-27-9BMS-986165BMS986165BMS 986165JAKInterleukin RelatedIFNARIsotope-Labeled CompoundsJanus kinaseILInterferon-α/β receptorInterferon-alpha/beta receptorInhibitorinhibitorinhibit

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Deucravacitinib (Synonyms: BMS-986165)

Customer Review

Other Forms of Deucravacitinib:

Deucravacitinib Related Antibodies

20 Publications Citing Use of MCE Deucravacitinib

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All JAK Isoform Specific Products:

View All Interleukin Related Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Deucravacitinib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Deucravacitinib Related Classifications

Keywords:

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