2. GPCR/G Protein
  3. GCGR
  4. Adomeglivant

Adomeglivant  (Synonyms: LY2409021)

製品番号: HY-19904 純度: 98.18%
COA 取扱説明書

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Adomeglivant (LY2409021) is a potent, selective glucagon receptor (GluR) allosteric antagonist. Adomeglivant is widely used in the research for type 2 diabetes mellitus.

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Adomeglivant 構造式

Adomeglivant 構造式

CAS 番号 : 1488363-78-5

容量 価格（税別） 在庫状況 数量
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 110 在庫あり
Solution
10 mM * 1 mL in DMSO USD 110 在庫あり
Solid
5 mg USD 90 在庫あり
10 mg USD 150 在庫あり
25 mg USD 250 在庫あり
50 mg USD 450 在庫あり
100 mg USD 750 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 5 publication(s) in Google Scholar

Adomeglivant 関連抗体

Top Publications Citing Use of Products

    Adomeglivant purchased from MedChemExpress. Usage Cited in: Cells. 2023 Apr 6, 12(7), 1098.

    Adomeglivant (50 μM; 24 h) significantly reduces the expression of PGC-1α in hepatocytes.

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    製品説明

    Adomeglivant (LY2409021) is a potent, selective glucagon receptor (GluR) allosteric antagonist. Adomeglivant is widely used in the research for type 2 diabetes mellitus[1][2][3].

    IC50 & Target

    GluR[1][2]
    体外実験

    Adomeglivant dose-dependently blocks glucagon-induced the raise levels of cAMP in HEK293-GluR cells[2].
    Adomeglivant fails to block cAMP-elevating actions of adenosine[2].
    Adomeglivant exhibits high selectivity for family B GPCRs, and specifically interacts with a conserved binding motif within the GluR, GLP-1R, and GIP-R[2].

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

    Adomeglivant 関連抗体
    体内実験

    Adomeglivant (5 mg/kg; i.p.) completely abolishes the hyperglycaemic action of CNO (clozapine-N-oxide) in Avpires-Cre+ mice. (CNO is a specific, pharmacologically inert agonist for hM3Dq-induced membrane depolarisation and increased the firing rate in hM3Dq-expressing arginine-vasopressin (AVP) neurons.)[3]

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

    Animal Model: Avpires-Cre+ mice[3]
    Dosage: 5 mg/kg
    Administration: Intraperitoneal injection, 30 minutes prior to CNO
    Result: Completely abolished the hyperglycaemic action of CNO.
    臨床実験
    分子量

    555.63

    分子式

    C32H36F3NO4
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)CCNC(C1=CC=C([C@@H](OC2=CC(C)=C(C3=CC=C(C(C)(C)C)C=C3)C(C)=C2)CCC(F)(F)F)C=C1)=O
    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 (179.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7998 mL 8.9988 mL 17.9976 mL
    5 mM 0.3600 mL 1.7998 mL 3.5995 mL
    10 mM 0.1800 mL 0.8999 mL 1.7998 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.

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    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: ≥ 2.5 mg/mL (4.50 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 (4.50 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      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
    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 1.7998 mL 8.9988 mL 17.9976 mL 44.9940 mL
    5 mM 0.3600 mL 1.7998 mL 3.5995 mL 8.9988 mL
    10 mM 0.1800 mL 0.8999 mL 1.7998 mL 4.4994 mL
    15 mM 0.1200 mL 0.5999 mL 1.1998 mL 2.9996 mL
    20 mM 0.0900 mL 0.4499 mL 0.8999 mL 2.2497 mL
    25 mM 0.0720 mL 0.3600 mL 0.7199 mL 1.7998 mL
    30 mM 0.0600 mL 0.3000 mL 0.5999 mL 1.4998 mL
    40 mM 0.0450 mL 0.2250 mL 0.4499 mL 1.1248 mL
    50 mM 0.0360 mL 0.1800 mL 0.3600 mL 0.8999 mL
    60 mM 0.0300 mL 0.1500 mL 0.3000 mL 0.7499 mL
    80 mM 0.0225 mL 0.1125 mL 0.2250 mL 0.5624 mL
    100 mM 0.0180 mL 0.0900 mL 0.1800 mL 0.4499 mL
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    Adomeglivant Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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

    Adomeglivant1488363-78-5LY2409021LY 2409021LY-2409021GCGRGlucagon Receptortype2diabetesmellitusInhibitorinhibitorinhibit

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    製品名:
    Adomeglivant
    製品番号:
    HY-19904
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