2. Membrane Transporter/Ion Channel
  3. SGLT
  4. Ertugliflozin L-pyroglutamic acid

Ertugliflozin L-pyroglutamic acid  (Synonyms: PF-04971729 L-pyroglutamic acid)

製品番号: HY-15461A 純度: 99.84%
COA 取扱説明書 Technical Support

Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2. Has the potential for the treatment of type 2 diabetes mellitus.

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Ertugliflozin L-pyroglutamic acid

Ertugliflozin L-pyroglutamic acid 構造式

CAS 番号 : 1210344-83-4

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 62 在庫あり
Solution
10 mM * 1 mL in DMSO USD 62 在庫あり
Solid
5 mg $50 在庫あり
10 mg $70 在庫あり
50 mg $120 在庫あり
100 mg   お問い合わせ  
200 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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カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Other Forms of Ertugliflozin L-pyroglutamic acid:

Ertugliflozin L-pyroglutamic acid 関連抗体

Top Publications Citing Use of Products

SGLT 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
SGLT1 SGLT2

  • 生物活性

  • 純度とドキュメンテーション

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製品説明

Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2[1]. Has the potential for the treatment of type 2 diabetes mellitus[2].

IC50 & Target

SGLT2

 

体外実験

Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) demonstrates >2000-fold selectivity for SGLT2 inhibition (relative to SGLT1) in vitro[3].

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

Ertugliflozin L-pyroglutamic acid 関連抗体
体内実験

Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) reveals a concentration-dependent glucosuria after oral administration to rats[3].

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

566.00

分子式

C27H32ClNO10
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C([C@]23O[C@@](CO)(CO3)[C@@H](O)[C@H](O)[C@H]2O)C=C1CC4=CC=C(OCC)C=C4.O=C5CC[C@@H](C(O)=O)N5
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 (176.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 5 mg/mL (8.83 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7668 mL 8.8339 mL 17.6678 mL
5 mM 0.3534 mL 1.7668 mL 3.5336 mL
10 mM 0.1767 mL 0.8834 mL 1.7668 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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 (3.67 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 (3.67 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: 99.84%

COA (254 KB) LCMS (90 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
H2O / DMSO 1 mM 1.7668 mL 8.8339 mL 17.6678 mL 44.1696 mL
5 mM 0.3534 mL 1.7668 mL 3.5336 mL 8.8339 mL
DMSO 10 mM 0.1767 mL 0.8834 mL 1.7668 mL 4.4170 mL
15 mM 0.1178 mL 0.5889 mL 1.1779 mL 2.9446 mL
20 mM 0.0883 mL 0.4417 mL 0.8834 mL 2.2085 mL
25 mM 0.0707 mL 0.3534 mL 0.7067 mL 1.7668 mL
30 mM 0.0589 mL 0.2945 mL 0.5889 mL 1.4723 mL
40 mM 0.0442 mL 0.2208 mL 0.4417 mL 1.1042 mL
50 mM 0.0353 mL 0.1767 mL 0.3534 mL 0.8834 mL
60 mM 0.0294 mL 0.1472 mL 0.2945 mL 0.7362 mL
80 mM 0.0221 mL 0.1104 mL 0.2208 mL 0.5521 mL
100 mM 0.0177 mL 0.0883 mL 0.1767 mL 0.4417 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Ertugliflozin L-pyroglutamic acid 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:

Ertugliflozin L-pyroglutamic acid1210344-83-4PF-04971729 L-pyroglutamic acidSGLTSodium-dependent glucose cotransportersInhibitorinhibitorinhibit

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