2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. JAK Apoptosis
  4. Ivarmacitinib

Ivarmacitinib  (Synonyms: SHR0302)

製品番号: HY-112724 純度: 99.62%
COA 取扱説明書 Technical Support

Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Ivarmacitinib

Ivarmacitinib 構造式

CAS 番号 : 1445987-21-2

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 258 在庫あり
Solution
10 mM * 1 mL in DMSO USD 258 在庫あり
Solid
1 mg $90 在庫あり
5 mg $235 在庫あり
10 mg $380 在庫あり
25 mg $650 在庫あり
50 mg $1040 在庫あり
100 mg $1665 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 0 publication(s) in Google Scholar

Other Forms of Ivarmacitinib:

Ivarmacitinib 関連抗体

Top Publications Citing Use of Products

JAK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

Ivarmacitinib (SHR0302) is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of Ivarmacitinib for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. Ivarmacitinib inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. Ivarmacitinib has anti-proliferative and anti-inflammatory effects[1][2].

IC50 & Target[1]

JAK1

 

JAK2

 

JAK3

 

Tyk2

 

体外実験

Ivarmacitinib (SHR0302; 1 nM-10 µM; 48 hours; HSCs) treatment displays an inhibitory effect on the proliferation of HSCs in a concentration-dependent manner[2].
Ivarmacitinib (1 nM-10 µM) exerts an inhibitory effect on the activation, proliferation and migration of HSCs[2].
Ivarmacitinib (1 nM-10 µM; 48 hours; HSCs) treatment induces the apoptosis of HSCs[2].
Ivarmacitinib (1 nM-10 µM; 48 hours; HSCs) treatment significantly increases the activation of caspase-3 and Bax in HSCs, and decreases the expression of Bcl-2. SHR0302 also inhibits the activation of Akt signaling pathway[2].

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

Ivarmacitinib 関連抗体

Cell Proliferation Assay[2]

Cell Line: Hepatic stellate cells (HSCs)
Concentration: 1 nM, 10 nM, 100 nM, 1µM, 10 µM
Incubation Time: 48 hours
Result: Displayed an inhibitory effect on the proliferation of HSCs, and that inhibition ocurred in a concentration-dependent manner.

Apoptosis Analysis[2]

Cell Line: Hepatic stellate cells (HSCs)
Concentration: 1 nM, 10 nM, 100 nM, 1µM, 10 µM
Incubation Time: 48 hours
Result: Induced the apoptosis of HSCs.

Western Blot Analysis[2]

Cell Line: Hepatic stellate cells (HSCs)
Concentration: 1 nM, 10 nM, 100 nM, 1µM, 10 µM
Incubation Time: 48 hours
Result: Significantly increased the activation of caspase-3 and Bax in HSCs, and decreased the expression of Bcl-2. Also inhibited the activation of Akt signaling pathway.
体内実験

Ivarmacitinib (SHR0302; 0.3-3.0 mg/kg; intragastric administration; twice a day; for 14 days; male Sprague-Dawley (SD) rats) treatment suppresses the severity of AA rats by attenuating the arthritis index, arthritis global assessment and paw swelling degree, and alleviated histopathology of spleen and joint of AA rats[1].
Ivarmacitinib can inhibit the proliferation of T, B and fibroblast-like synoviocytes (FLS), and down-regulates cytokines TNF-α, IL-1β, IL-17 and antibody IgG1, IgG2a levels, and suppresses the proportion of Th17 and total B, and inhibits JAK1-STAT3 phosphorylation[1].

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

Animal Model: Male Sprague-Dawley (SD) rats (150-180 g) injected with complete Freund’s adjuvant (CFA)[1]
Dosage: 0.3 mg/kg,1.0 mg/kg, 3.0 mg/kg
Administration: Intragastric administration; twice a day; for 14 days
Result: Suppressed the severity of adjuvant-induced arthritis (AA) rats by attenuating the arthritis index, arthritis global assessment and paw swelling degree, and alleviated histopathology of spleen and joint of AA rats.
臨床実験
分子量

414.48

分子式

C18H22N8O2S
CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

O=C(N1C[C@@]2([H])[C@@](C[C@H](N(C)C3=C4C(NC=C4)=NC=N3)C2)([H])C1)NC5=NC(OC)=NS5
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 31.25 mg/mL (75.40 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 2.4127 mL 12.0633 mL 24.1266 mL
5 mM 0.4825 mL 2.4127 mL 4.8253 mL
10 mM 0.2413 mL 1.2063 mL 2.4127 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.02 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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.
純度とドキュメンテーション

純度: 99.62%

COA (253 KB) HNMR (284 KB) LCMS (104 KB)

取扱説明書 (2659 KB)
参考文献

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 2.4127 mL 12.0633 mL 24.1266 mL 60.3165 mL
5 mM 0.4825 mL 2.4127 mL 4.8253 mL 12.0633 mL
10 mM 0.2413 mL 1.2063 mL 2.4127 mL 6.0317 mL
15 mM 0.1608 mL 0.8042 mL 1.6084 mL 4.0211 mL
20 mM 0.1206 mL 0.6032 mL 1.2063 mL 3.0158 mL
25 mM 0.0965 mL 0.4825 mL 0.9651 mL 2.4127 mL
30 mM 0.0804 mL 0.4021 mL 0.8042 mL 2.0106 mL
40 mM 0.0603 mL 0.3016 mL 0.6032 mL 1.5079 mL
50 mM 0.0483 mL 0.2413 mL 0.4825 mL 1.2063 mL
60 mM 0.0402 mL 0.2011 mL 0.4021 mL 1.0053 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Ivarmacitinib Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

Ivarmacitinib1445987-21-2SHR0302SHR 0302SHR-0302JAKApoptosisJanus kinaseJAK1arthritisJAK1-STAT3phosphorylationanti-proliferationTh17B-cellanti-inflammatorymigrationcollagenhepaticfibrosisInhibitorinhibitorinhibit

最近チェックした製品:

オンラインお問い合わせ

Your information is safe with us. * Required Fields.

製品名

  

カスタマ需要量 *

お名前 *

 

タイトル

メールアドレス *

 

電話番号 *

デパートメント

 

組纖名 *

市区町村

都道府県

国或いは地域 *

      

必ず会社名を記載ください。個人への返信は行いません。

備考

バルクお問い合わせ

Inquiry Information

製品名:
Ivarmacitinib
製品番号:
HY-112724
数量:
MCE 日本正規代理店:

カスタマーレビュー

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

製品名

  

Lot #

お名前 *

 

メールアドレス *

電話番号 *

 

部門 *

組纖名 *

 

国或いは地域 *

備考

Request for HNMR Report

We have received your request and will respond to you as soon as possible.