2. GPCR/G Protein
  3. LPL Receptor
  4. AM095

AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.

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。

CAS 番号 : 1345614-59-6

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 80 在庫あり
Solution
10 mM * 1 mL in DMSO USD 80 在庫あり
Solid
5 mg $76 在庫あり
10 mg $120 在庫あり
25 mg $230 在庫あり
50 mg $360 在庫あり
100 mg $560 在庫あり
200 mg $840 在庫あり
500 mg $1512 在庫あり
1 g $1950 在庫あり
5 g   お問い合わせ  
10 g   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 13 publication(s) in Google Scholar

Other Forms of AM095:

AM095 関連抗体

Top Publications Citing Use of Products

    AM095 purchased from MedChemExpress. Usage Cited in: Biomol Ther (Seoul). 2014 Feb;22(2):129-35.  [Abstract]

    Efficacies of LPE- and LPA-induced Ca2+ responses as compared to digitonin in MDA-MB-231 and SK-OV3 cells are shown as histograms.

    LPL Receptor 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
    LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

    • 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

    AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.

    IC50 & Target

    LPA1 Receptor

     

    体外実験

    AM095 is a potent LPA1 receptor antagonist because it inhibits GTPγS binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA1 with IC50 values of 0.98 and 0.73 μM, respectively. AM095 inhibits LPA-driven chemotaxis of CHO cells overexpressing mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM). The IC50 of AM095 in the human LPA1 GTPγS binding assay is comparable with that of our previously published compound AM966 (IC50=0.98±0.17 μM) and the Debio-0719 compound (IC50=0.60±0.04 μM)[1]. AM095 inhibits the LPA-induced calcium flux of CHO cells stably transfected with human or mouse LPA1. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively[2].

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

    AM095 関連抗体
    体内実験

    AM095 has high oral bioavailability and a moderate half-life and is well tolerated at the doses tested in rats and dogs after oral and intravenous dosing. After oral (10 mg/kg) dosing in rats, AM095 plasma concentrations peaked at 2 h with a Cmax of 41 μM, thereafter decreasing to 10 nM by 24 h. After intravenous (2 mg/kg) dosing, a Cmax of 12 μM is observed within 15 min, which also decreased to approximately 10 nM by 24 h, yielding a t1/2 of 1.79 h. In dogs, a single oral dose of 5 mg/kg yielded a peak plasma concentration of 21 μM within 15 min of dosing, which then decreased to 10 nM by 24 h. In contrast, an intravenous dose of 2 mg/kg resulted in a Cmax of 11 μM within 15 min and decreased to 15 nM by 8 h, yielding a t1/2 of 1.5 h[1].

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

    478.47

    分子式

    C27H23N2NaO5
    CAS 番号
    Appearance

    Solid

    Color

    Light yellow to khaki

    SMILES

    O=C(O[Na])CC1=CC=C(C2=CC=C(C3=C(NC(O[C@@H](C4=CC=CC=C4)C)=O)C(C)=NO3)C=C2)C=C1
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    溶剤 & 溶解度
    体外: 

    DMSO : 83.33 mg/mL (174.16 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 2.0900 mL 10.4500 mL 20.9000 mL
    5 mM 0.4180 mL 2.0900 mL 4.1800 mL
    10 mM 0.2090 mL 1.0450 mL 2.0900 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 (sealed storage, away from moisture). 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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (4.35 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 (4.35 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.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  Saline

      Solubility: 5 mg/mL (10.45 mM); Suspended solution; Need ultrasonic

    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).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    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: 99.72%

    COA (254 KB) LCMS (125 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [1]

    Known amounts of AM095 (diluted in DMSO) or vehicle (DMSO) are added to 25 to 40 μg of hLPA1/CHO or mLPA1/CHO membranes and 0.1 nM [35S]-GTPγS in buffer (50 mM HEPES, 0.1 mM NaCl, 10 mM MgCl2, 50 μg/mL saponin, pH 7.5) containing 0.2% fatty acid-free human serum albumin and 5 μM GDP. To test for LPA1 antagonist activity, the ability of AM095 to inhibit GTPγS binding stimulated by 900 nM LPA (18:1) is measured. Alternatively, to test for agonist effects, the ability of AM095 to stimulate GTPγS binding in the absence of LPA is measured. Reactions are incubated for 30 min at 30°C, before harvesting membranes onto glass filter binding plates (UniFilter GF/B) and washing three times with cold buffer containing 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM MgCl2 using a Brandel 96-tip cell harvester. Plates are dried and then cpm are evaluated by using a Packard TopCount NXT microplate scintillation counter[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。
    動物実験
    [1][2]

    Rats[1]
    Male Sprague-Dawley rats with surgically implanted jugular vein catheters (250-300 g) are used. In all studies, animals are fasted 15 to 24 h before dosing. For rats, AM095 is administered intraveneously at a dose of 2 mg/kg in 0.9% saline given as a 1 mL/kg bolus injection into the jugular vein. To determine oral exposure, AM095 is administered as a solution in 0.5% methylcellulose via an oral gavage at a dose of 10 mg/kg in a volume of 3 mL/kg. Blood samples (approximately 300 μL of total blood) are taken from each rat via the jugular vein catheter at times up to 24 h postdose (10-11 samples per animal) in potassium EDTA tubes. After each sampling, the catheter is flushed with an equivalent volume of saline. Plasma samples, prepared by centrifugation of whole blood, are stored frozen (−80°C) before analysis. AM095 is dosed intravenously at 2 mg/kg and orally at 5 mg/kg to male beagle dogs (n=3). Plasma samples are collected and analyzed for AM095 concentration by liquid chromatography/mass spectrometry.
    Mice[2]
    C57Bl/6 mice are administered the selective LPA1 antagonist AM095 by oral gavage (30 mg/kg) at time 0 and 8 h, and blood is collected by cardiac puncture under anesthesia in sodium EDTA tubes at 0, 4, 8, 9, 12 and 24 h. Plasma samples are stored at −40°C prior to analysis of AM095 concentrations by liquid chromatography/mass spectrometry (LC-MS/MS). Known amounts of AM095 are added to thawed mouse plasma to yield a concentration range from 0.8 to 4,000 ng/mL. Plasma samples are precipitated using acetonitrile containing the internal standard buspirone. The analyte mixture (10 μL) is injected using a Leap PAL autosampler. Calibration curves are constructed by plotting the peak-area ratio of analyzed peaks against known concentrations. The lower limit of quantitation is 1 ng/mL. The data are subjected to linear regression analysis with 1/x2 weighting. The pharmacokinetic parameters of AM095 are calculated by non-compartmental analysis using WinNonlin Professional. Cmax and time to Cmax (Tmax) are obtained directly from the measured data.

    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 (sealed storage, away from moisture). 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 2.0900 mL 10.4500 mL 20.9000 mL 52.2499 mL
    5 mM 0.4180 mL 2.0900 mL 4.1800 mL 10.4500 mL
    10 mM 0.2090 mL 1.0450 mL 2.0900 mL 5.2250 mL
    15 mM 0.1393 mL 0.6967 mL 1.3933 mL 3.4833 mL
    20 mM 0.1045 mL 0.5225 mL 1.0450 mL 2.6125 mL
    25 mM 0.0836 mL 0.4180 mL 0.8360 mL 2.0900 mL
    30 mM 0.0697 mL 0.3483 mL 0.6967 mL 1.7417 mL
    40 mM 0.0522 mL 0.2612 mL 0.5225 mL 1.3062 mL
    50 mM 0.0418 mL 0.2090 mL 0.4180 mL 1.0450 mL
    60 mM 0.0348 mL 0.1742 mL 0.3483 mL 0.8708 mL
    80 mM 0.0261 mL 0.1306 mL 0.2612 mL 0.6531 mL
    100 mM 0.0209 mL 0.1045 mL 0.2090 mL 0.5225 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.

    AM095 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:

    AM0951345614-59-6AM 095AM-095LPL ReceptorLysophospholipid ReceptorInhibitorinhibitorinhibit

    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:
    AM095
    製品番号:
    HY-16039
    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.