2. Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK
  3. Phosphatase Tie
  4. Razuprotafib

Razuprotafib  (Synonyms: AKB-9778)

製品番号: HY-109041 純度: 98.0%
COA 取扱説明書 Technical Support

Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM).

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Razuprotafib

Razuprotafib 構造式

CAS 番号 : 1008510-37-9

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 645 在庫あり
Solution
10 mM * 1 mL in DMSO USD 645 在庫あり
Solid
1 mg $309 在庫あり
5 mg $500 在庫あり
10 mg $750 在庫あり
25 mg $1275 在庫あり
50 mg $1660 在庫あり
100 mg $2160 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

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Based on 4 publication(s) in Google Scholar

Other Forms of Razuprotafib:

Razuprotafib 関連抗体

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製品説明

Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM)[1].

体外実験

Razuprotafib (AKB-9778) promotes TIE2 phosphorylation and activation of downstream signaling in HUVECs and enhances angiopoietin-induced TIE2 phosphorylation[1].

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

Razuprotafib 関連抗体
体内実験

Razuprotafib (20 mg/kg; s.c.) promotes phosphorylation of TIE2 in retinal endothelial cells in vivo[1]. Razuprotafib (10-20 mg/kg; s.c.; twice daily for 7 days) suppresses subretinal neovascularization (NV)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

586.70

分子式

C26H26N4O6S3
CAS 番号
Appearance

Solid

Color

White to light yellow

SMILES

O=C([C@@H](NC(OC)=O)CC1=CC=CC=C1)N[C@H](C2=CSC(C3=CC=CS3)=N2)CC4=CC=C(NS(=O)(O)=O)C=C4
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 : 100 mg/mL (170.44 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 1.7044 mL 8.5222 mL 17.0445 mL
5 mM 0.3409 mL 1.7044 mL 3.4089 mL
10 mM 0.1704 mL 0.8522 mL 1.7044 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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Concentration
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Volume
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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

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濃度 （終了）

C2

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体積 （終了）

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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: ≥ 2.5 mg/mL (4.26 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 2

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

    Solubility: ≥ 2.5 mg/mL (4.26 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 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: 98.0%

COA (254 KB) HNMR (137 KB) LCMS (112 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7044 mL 8.5222 mL 17.0445 mL 42.6112 mL
5 mM 0.3409 mL 1.7044 mL 3.4089 mL 8.5222 mL
10 mM 0.1704 mL 0.8522 mL 1.7044 mL 4.2611 mL
15 mM 0.1136 mL 0.5681 mL 1.1363 mL 2.8407 mL
20 mM 0.0852 mL 0.4261 mL 0.8522 mL 2.1306 mL
25 mM 0.0682 mL 0.3409 mL 0.6818 mL 1.7044 mL
30 mM 0.0568 mL 0.2841 mL 0.5681 mL 1.4204 mL
40 mM 0.0426 mL 0.2131 mL 0.4261 mL 1.0653 mL
50 mM 0.0341 mL 0.1704 mL 0.3409 mL 0.8522 mL
60 mM 0.0284 mL 0.1420 mL 0.2841 mL 0.7102 mL
80 mM 0.0213 mL 0.1065 mL 0.2131 mL 0.5326 mL
100 mM 0.0170 mL 0.0852 mL 0.1704 mL 0.4261 mL
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Razuprotafib 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:

Razuprotafib1008510-37-9AKB-9778AKB9778AKB 9778PhosphataseTieAngiopoietin receptoracutekidneyinjuryTie-2diabeticnephropathyInhibitorinhibitorinhibit

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