2. Metabolic Enzyme/Protease
  3. Ketohexokinase
  4. PF-06835919

PF-06835919  (Synonyms: Ketohexokinase inhibitor 1)

製品番号: HY-U00461 純度: 99.53%
COA 取扱説明書 Technical Support

PF-06835919 (Ketohexokinase inhibitor 1) is an inhibitor of ketohexokinase (KHK), with IC50s of 8.4 nM and 66 nM for KHK-C and KHK-A, respectively. PF-06835919 can be used for the study of metabolic disorders driven by the overconsumption of Fructose (HY-N0395).

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。

PF-06835919

PF-06835919 構造式

CAS 番号 : 2102501-84-6

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 429 在庫あり
Solution
10 mM * 1 mL in DMSO USD 429 在庫あり
Solid
1 mg $130 在庫あり
5 mg $390 在庫あり
10 mg $660 在庫あり
25 mg $1180 在庫あり
50 mg $1600 在庫あり
100 mg $2150 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

PF-06835919 関連抗体

Top Publications Citing Use of Products

Ketohexokinase 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
KHK-A KHK-C

  • 生物活性

  • プロトコル

  • 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

PF-06835919 (Ketohexokinase inhibitor 1) is an inhibitor of ketohexokinase (KHK), with IC50s of 8.4 nM and 66 nM for KHK-C and KHK-A, respectively. PF-06835919 can be used for the study of metabolic disorders driven by the overconsumption of Fructose (HY-N0395)[1][2].

IC50 & Target

IC50: 8.4 nM (KHK-C), 66 nM (KHK-A)[1]
Cellular Effect
Cell Line Type Value Description References
HepG2 IC50
146 nM
Compound: 2; PF-06835919
Antiproliferative activity against human HepG2 cells incubated for 3 hrs by LC-MS analysis
Antiproliferative activity against human HepG2 cells incubated for 3 hrs by LC-MS analysis
[PMID: 37766386]
HepG2 IC50
> 150 μM
Compound: 2; PF-06835919
Cytotoxicity against human HepG2 cells measured after 48 hrs by microscopy based analysis
Cytotoxicity against human HepG2 cells measured after 48 hrs by microscopy based analysis
[PMID: 37766386]
HepG2 IC50
> 150 μM
Compound: 2; PF-06835919
Mitotoxicity in human HepG2 cells incubated for 2 hrs by Celltiter-Glo assay
Mitotoxicity in human HepG2 cells incubated for 2 hrs by Celltiter-Glo assay
[PMID: 37766386]
Hepatocyte IC50
> 150 μM
Compound: 2; PF-06835919
Toxicity in human Primary hepatocyte incubated for 48 hrs by Celltiter-Glo assay
Toxicity in human Primary hepatocyte incubated for 48 hrs by Celltiter-Glo assay
[PMID: 37766386]
臨床実験
分子量

356.34

分子式

C16H19F3N4O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(C[C@H]1[C@@]2(CN(C[C@]12[H])C3=NC(N4[C@H](CC4)C)=NC(C(F)(F)F)=C3)[H])O
輸送条件

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

DMSO : 100 mg/mL (280.63 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 2.8063 mL 14.0315 mL 28.0631 mL
5 mM 0.5613 mL 2.8063 mL 5.6126 mL
10 mM 0.2806 mL 1.4032 mL 2.8063 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)

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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: 2.5 mg/mL (7.02 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.02 mM); Clear solution

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: 99.53%

COA (250 KB) HNMR (337 KB) LCMS (102 KB)

取扱説明書 (2659 KB)
参考文献
キナーゼ実験
[1]

A 384-well format on a assay plate is used in the assay and monitored by UV-vis spectroscopy in continuous mode at room temperature (rt). Compounds (Ketohexokinase inhibitor 1) are prepared in DMSO as 4 mM stocks, diluted using an 11-point half-log scheme on a Biomek FX, and incubated at rt for 30 minutes with the reaction mixture containing 50 mM HEPES, pH 7.4, 140 mM KCl, 3.5 mM MgCl2, 0.8 mM fructose, 2 mM TCEP, 0.8 mM PEP, 0.7 mM NADH, 0.01% Triton X-100, 30 U/mL pyruvate kinase-lactate dehydrogenase, and 10 nM purified KHK-C. The compound concentration in each well ranged from 1 nM to 100 μM. The reaction is initiated with the addition of 0.2 mM ATP. The absorbance is measured for 30 minutes on a SpectraMax reader after ATP is added. The concentrations provided are based on the final mixture volume of 40 μL[1].

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
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 2.8063 mL 14.0315 mL 28.0631 mL 70.1577 mL
5 mM 0.5613 mL 2.8063 mL 5.6126 mL 14.0315 mL
10 mM 0.2806 mL 1.4032 mL 2.8063 mL 7.0158 mL
15 mM 0.1871 mL 0.9354 mL 1.8709 mL 4.6772 mL
20 mM 0.1403 mL 0.7016 mL 1.4032 mL 3.5079 mL
25 mM 0.1123 mL 0.5613 mL 1.1225 mL 2.8063 mL
30 mM 0.0935 mL 0.4677 mL 0.9354 mL 2.3386 mL
40 mM 0.0702 mL 0.3508 mL 0.7016 mL 1.7539 mL
50 mM 0.0561 mL 0.2806 mL 0.5613 mL 1.4032 mL
60 mM 0.0468 mL 0.2339 mL 0.4677 mL 1.1693 mL
80 mM 0.0351 mL 0.1754 mL 0.3508 mL 0.8770 mL
100 mM 0.0281 mL 0.1403 mL 0.2806 mL 0.7016 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.

PF-06835919 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:

PF-068359192102501-84-6Ketohexokinase inhibitor 1PF06835919PF 06835919Ketohexokinase inhibitor1Ketohexokinase inhibitor-1KetohexokinaseKHKketohexokinasemetabolic disordersInhibitorinhibitorinhibit

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:
PF-06835919
製品番号:
HY-U00461
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.