2. GPCR/G Protein Neuronal Signaling MAPK/ERK Pathway PI3K/Akt/mTOR
  3. mAChR p38 MAPK Akt
  4. Darifenacin hydrobromide

Darifenacin (hydrobromide)  (Synonyms: UK-88525 (hydrobromide); ダリフェナシン 臭化水素酸塩)

製品番号: HY-A0012 純度: 99.78%
COA 取扱説明書 Technical Support

Darifenacin (UK-88525) hydrobromide is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin hydrobromide binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin hydrobromide can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin hydrobromide inhibits tumor growth in colorectal cancer cells and has anti-tumor effects.

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 : 133099-07-7

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 28 在庫あり
Solution
10 mM * 1 mL in DMSO USD 28 在庫あり
Solid
5 mg $25 在庫あり
10 mg $30 在庫あり
25 mg $42 在庫あり
50 mg $50 在庫あり
100 mg $60 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 7 publication(s) in Google Scholar

Other Forms of Darifenacin hydrobromide:

Darifenacin (hydrobromide) 関連抗体

Top Publications Citing Use of Products

    Darifenacin hydrobromide purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Apr 5;7(14):18085-94.  [Abstract]

    MACC1 is up-regulated by ACh through p-AMPK. A. ACh stimulates AMPK phosphorylation via M3R. B. Inhibition of AMPK activity by Dorsomorphin (8 μM) suppresses the induction of MACC1 expression by ACh. p-AMPK levels increase after ACh stimulation, and pretreatment of Darifenacin attenuates the ACh-induced increase of p-AMPK.

    mAChR 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
    mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

    p38 MAPK 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
    p38 MAPK Akt1 p38α p38β MAPK13 p38δ p38γ

    Akt 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
    Akt Akt1 Akt2 Akt3

    • 生物活性

    • 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

    Darifenacin (UK-88525) hydrobromide is a selective and orally active M3 muscarinic receptor (M3R) antagonist with a pKi of 8.9. Darifenacin hydrobromide binds >20-fold more specifically to M3R than to other muscarinic receptors. Darifenacin hydrobromide can be used in the study of urinary incontinence and other symptoms of overactive bladder. Darifenacin hydrobromide inhibits tumor growth in colorectal cancer cells and has anti-tumor effects[1][2][3][4][5][6].

    IC50 & Target[3]

    mAChR3

     

    MMP-1

     

    ERK1

     

    ERK2

     

    体外実験

    Non-salt dose:
    Darifenacin (0.01-100 μM; 5 min) inhibits the Kv currents in concentration-dependent manners with an IC50 value of 0.34 μM and a Hill coefficient of 0.84 in coronary arterial smooth muscle cells[2].
    Darifenacin (0.01-10 μM; 1-48 h) inhibits cell viability, invasion and MMP-1 expression in colorectal cancer cells, and inhibits the phosphorylation of p38, ERK1/2 and Akt induced by muscarinic acetylcholine [3].

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

    Darifenacin (hydrobromide) 関連抗体

    Cell Viability Assay[3]

    Cell Line: HT-29 and SW480 cells
    Concentration: 0.01, 0.1, 1 and 10 μM
    Incubation Time: 48 h
    Result: Reduced viability and proliferation at a concentration of 10 µM in both cell lines HT29 and SW480.

    Western Blot Analysis[3]

    Cell Line: HT-29 cells
    Concentration: 0.1, 1 and 10 μM
    Incubation Time: 1 h
    Result: Inhibited the phosphorylation levels of p38, ERK1/2 and Akt.
    体内実験

    Non-salt dose:
    Darifenacin (2.5 mg/kg; intraperitoneal injection; 42 days) has an antitumor effect in a xenograft mouse model of colorectal cancer[3].
    Darifenacin (0.1 mg/kg; intravenous injection; Single dose) decreases the afferent activity of bladder Aδ and C fibers in female rats[4].
    Darifenacin (3 mg/kg/day; subcutaneous osmotic pump; 14 weeks) increases the severity of liver damage caused by Azoxymethane (HY-111375)[5].

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

    Animal Model: HT-29 cells treated male BALB/cnu/nu nude mice aged 6-10 weeks old (20-25 g)[3]
    Dosage: 2.5 mg/kg
    Administration: Intraperitoneal injection (i.p.); 42 days
    Result: Reduced primary tumor volume and weight, as well as liver metastases.
    Had no significant effect on the weight of mice.
    Animal Model: Azoxymethane (HY-111375) treated male mice [genetic background: 129S6/SvEv X CF1 (50%:50%)][5]
    Dosage: 3 mg/kg/day
    Administration: Subcutaneous osmotic pump; 14 weeks
    Result: Caused the mice weigh less, reduced liver-weight-to-body-weight ratios.
    Increased liver nodularity and Ishak fibrosis scores.
    Increased in ductular proliferation.
    臨床実験
    分子量

    507.46

    分子式

    C28H31BrN2O2
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(C(C1=CC=CC=C1)([C@@H]2CCN(CCC3=CC4=C(OCC4)C=C3)C2)C5=CC=CC=C5)N.Br
    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 : 33.33 mg/mL (65.68 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 1.9706 mL 9.8530 mL 19.7060 mL
    5 mM 0.3941 mL 1.9706 mL 3.9412 mL
    10 mM 0.1971 mL 0.9853 mL 1.9706 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: ≥ 2.5 mg/mL (4.93 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 (4.93 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).

    *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: 99.78%

    COA (253 KB) LCMS (101 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 (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 1.9706 mL 9.8530 mL 19.7060 mL 49.2650 mL
    5 mM 0.3941 mL 1.9706 mL 3.9412 mL 9.8530 mL
    10 mM 0.1971 mL 0.9853 mL 1.9706 mL 4.9265 mL
    15 mM 0.1314 mL 0.6569 mL 1.3137 mL 3.2843 mL
    20 mM 0.0985 mL 0.4926 mL 0.9853 mL 2.4632 mL
    25 mM 0.0788 mL 0.3941 mL 0.7882 mL 1.9706 mL
    30 mM 0.0657 mL 0.3284 mL 0.6569 mL 1.6422 mL
    40 mM 0.0493 mL 0.2463 mL 0.4926 mL 1.2316 mL
    50 mM 0.0394 mL 0.1971 mL 0.3941 mL 0.9853 mL
    60 mM 0.0328 mL 0.1642 mL 0.3284 mL 0.8211 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.

    Darifenacin hydrobromide 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:

    Darifenacin133099-07-7UK-88525UK88525UK 88525mAChRp38 MAPKAktMuscarinic acetylcholine receptorPKBProtein kinase BLiver damage modelColorectal cancer modelHT-29 cellsSW480 cellsCoronary arterial smooth muscle cellsM3 Muscarinic Receptor AntagonistInhibitorinhibitorinhibit

    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:
    Darifenacin hydrobromide
    製品番号:
    HY-A0012
    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.