1. Protein Tyrosine Kinase/RTK
  2. Discoidin Domain Receptor
  3. DDR1/2 IN-4

DDR1/2 IN-4 (Compound 37) is a selective dual DDR1 and DDR2 kinase inhibitor, with a pKi of 8.6 for DDR1 and a pKi of 8.2 for DDR2. DDR1/2 IN-4 functionally inhibits the kinase activities of DDR1 and DDR2. DDR1/2 IN-4 inhibits the release of MCP-1. DDR1/2 IN-4 can be used in studies related to idiopathic pulmonary fibrosis.

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。

DDR1/2 IN-4

DDR1/2 IN-4 構造式

CAS 番号 : 3027967-95-6

容量 在庫状況
50 mg   お問い合わせ  
100 mg   お問い合わせ  
250 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.

Top Publications Citing Use of Products

Discoidin Domain Receptor アイソフォーム固有の製品をすべて表示:

  • 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

DDR1/2 IN-4 (Compound 37) is a selective dual DDR1 and DDR2 kinase inhibitor, with a pKi of 8.6 for DDR1 and a pKi of 8.2 for DDR2. DDR1/2 IN-4 functionally inhibits the kinase activities of DDR1 and DDR2. DDR1/2 IN-4 inhibits the release of MCP-1. DDR1/2 IN-4 can be used in studies related to idiopathic pulmonary fibrosis[1].

IC50 & Target[1]

DDR1

8.6 (pKi)

DDR2

8.2 (pKi)

体外実験

DDR1/2 IN-4 potently binds to DDR1 (pKi=8.6) and DDR2 (pKi=8.2)[1].
DDR1/2 IN-4 potently inhibits DDR1 activity in U2OS cells, with a pIC50 of 8.0[1].
DDR1/2 IN-4 (1-30 μM; 48 h) shows no cytotoxicity against A549 cells at concentrations up to 10 μM, and only exhibits mild cytotoxicity after 48 h treatment at 30 μM[1].

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

Cell Viability Assay[1]

Cell Line: A549 cells
Concentration: 1-30 μM
Incubation Time: 48 h
Result: Showed no cytotoxicity at concentrations up to 10 μM; reduced cell viability to 84.9% at 30 μM.
Parmacokinetics
Species Dose Route Cmax Tmax (Plasma) T1/2 AUClast
Mice[1] 1 mg/kg i.n. 117 (plasma) ng/g 0.083 (plasma) h 2 (plasma) h 141 (plasma) ng·h/mL
体内実験

DDR1/2 IN-4 (0.1-1 mg/kg; intranasal; single administration) significantly reduces collagen-induced pulmonary MCP-1 levels by 39% in male C57BL/6N mice, confirming its in vivo activity of inhibiting DDR-mediated signaling pathways[1].

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

Animal Model: C57BL/6N (male)[1]
Dosage: 0.1 mg/kg; 0.3 mg/kg; 1 mg/kg
Administration: intranasal; single dose
Result: Showed dose-dependent inhibition of pulmonary MCP-1 levels.
Caused a significant 39% reduction in pulmonary MCP-1 levels compared to the vehicle-treated, collagen-challenged group (p < 0.05) at 1 mg/kg.
分子量

467.45

分子式

C23H20F3N7O

CAS 番号
SMILES

O=C(NC1=CC(C(F)(F)F)=CN=C1)C2=CC=C(C)C(NC3CN(C4=C5C=NC=CN5N=C4)C3)=C2

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション
参考文献
  • 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.
  • 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.

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:
DDR1/2 IN-4
製品番号:
HY-181839
数量:
MCE 日本正規代理店: