2. Metabolic Enzyme/Protease Autophagy
  3. Renin Autophagy
  4. Aliskiren hemifumarate

Aliskiren (hemifumarate)  (Synonyms: CGP 60536 (hemifumarate); CGP60536B (hemifumarate); SPP 100 (hemifumarate); ヘミフマル酸アリスキレン)

製品番号: HY-12177 純度: 99.62%
COA 取扱説明書 Technical Support

Aliskiren (CGP 60536; CGP60536B; SPP 100) hemifumarate is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hemifumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia.

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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 : 173334-58-2

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 88 在庫あり
Solution
10 mM * 1 mL in Water USD 88 在庫あり
Solid
5 mg $42 在庫あり
10 mg $66 在庫あり
50 mg $145 在庫あり
100 mg $238 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 11 publication(s) in Google Scholar

Other Forms of Aliskiren hemifumarate:

Aliskiren (hemifumarate) 関連抗体

Top Publications Citing Use of Products

    Aliskiren hemifumarate purchased from MedChemExpress. Usage Cited in: Lipids Health Dis. 2018 Jul 31;17(1):183.  [Abstract]

    Protein abundance of ER stress markers (BiP, IRE1α, PERK, ATF4, pS51-eIF2α, eIF2α, and CHOP) are upregulated after palmitic acid (PA) treatment, which is prevented by cotreatment with chymostatin (50μM) and Aliskiren (10 nM).

    Aliskiren hemifumarate purchased from MedChemExpress. Usage Cited in: National Sun Yat-Sen University. 2015 Sep.

    Effects of Aliskiren (AK) produce efficacious antagonism of the protein expression of c-Fos (A), GFAP (B) and OX-42 (C) in SC, aCSF+MCAO, AK+MCAO or AK alone group one day after stroke.

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    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    Aliskiren (CGP 60536; CGP60536B; SPP 100) hemifumarate is an orally active and selective renin inhibitor, with IC50 of 1.5 nM. Aliskiren hemifumarate can be used for the research of hypertension, cardiovascular diseases and cancer cachexia[1][2][3].

    IC50 & Target

    IC50: 1.5 nM (renin)[1]; 0.6 nM (human renin), 2 nM (marmoset renin), 80 nM (rat renin), 7 nM (dog renin), 11 nM (rabbit renin), 63 nM (guinea pig renin), 150 nM (pig renin)[2]
    体外実験

    Aliskiren hemifumarate inhibits plasma renin activity (PRA) in vitro with IC50s of 2.9 nM (human PRA), 8.0 nM (monkey PRA), respectively[1].
    Aliskiren hemifumarate (5 μM; 24 h) inhibits prorenin-induced human aortic smooth muscle cell migration[2].
    Aliskiren hemifumarate (1-10 μM; 24 h) inhibits both the lamellipodia formation and morphological changes induced by prorenin with no significant effect on PDGF-BB activity[2].

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

    Aliskiren (hemifumarate) 関連抗体

    Cell Viability Assay[2]

    Cell Line: Smooth muscle cell (SMC)
    Concentration: 1-10 μM
    Incubation Time: 24 hours
    Result: Inhibited human aortic smooth muscle cell migration induced by prorenin (10 nM) at 10 μM.
    体内実験

    Aliskiren hemifumarate (3 mg/kg, 10 mg/kg; p.o.; daily; 0-12 d) inhibit renin and lower blood pressure without affecting heart rate in sodium-depleted marmosets[3].
    Aliskiren hemifumarate (10 mg/kg; p.o.; single dose) delays cachexia development, reduces tumor, and prolongs mouse survival. And also improves whole‑body strength, mobility and coordination, enhances locomotor activity, and inhibits muscle wasting[4].
    Aliskiren hemifumarate (10 mg/kg; p.o.; single dose; 20 d after C26 injection) reduces oxidative stress associated with cancer cachexia[4].

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

    Animal Model: Sodium-depleted marmosets[3]
    Dosage: 3 mg/kg, 10 mg/kg
    Administration: Oral gavage; once daily; 12 days
    Result: Increased plasma immunoreactive renin levels, and lowered blood pressure without affecting heart rate.
    Showed no rebound increase in BP following the end of treatment with either dose of aliskiren.
    Inhibited the RAS and controls the upregulation of pro‑inflammatory cytokines.
    Animal Model: Cancer cachexia model in BALB/c mice injected with C26 mouse colon carcinoma cells[4]
    Dosage: 10 mg/kg
    Administration: Oral gavage; on day 5 (as a preventive strategy, AP group) or on day 12 (as a therapeutic strategy, AT group) after C26 injection; for 20 days after C26 injection
    Result: Enhanced grip strength, coordination, and locomotor activity.
    Inhibited serum Ang I and Ⅱ levels and both serum and muscular tumor necrosis factor‑α (TNF‑α) and inter‑ leukin‑6 (IL‑6) levels.
    臨床実験
    分子量

    1219.59

    分子式

    C64H110N6O16
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)/C=C/C(O)=O.O=C(NCC(C)(C(N)=O)C)[C@@H](C[C@@H]([C@H](C[C@@H](C(C)C)CC1=CC=C(OC)C(OCCCOC)=C1)N)O)C(C)C.O=C(NCC(C)(C(N)=O)C)[C@H](C(C)C)C[C@H](O)[C@@H](N)C[C@@H](C(C)C)CC2=CC=C(OC)C(OCCCOC)=C2
    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: 

    H2O : ≥ 50 mg/mL (41.00 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.8199 mL 4.0997 mL 8.1995 mL
    5 mM 0.1640 mL 0.8199 mL 1.6399 mL
    10 mM 0.0820 mL 0.4100 mL 0.8199 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.

    * 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
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    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

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    体積 （終了）

    V2

    体内:

    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:  PBS

      Solubility: 50 mg/mL (41.00 mM); Clear solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

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    Dosing volume
    (per animal)

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    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, 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
    H2O 1 mM 0.8199 mL 4.0997 mL 8.1995 mL 20.4987 mL
    5 mM 0.1640 mL 0.8199 mL 1.6399 mL 4.0997 mL
    10 mM 0.0820 mL 0.4100 mL 0.8199 mL 2.0499 mL
    15 mM 0.0547 mL 0.2733 mL 0.5466 mL 1.3666 mL
    20 mM 0.0410 mL 0.2050 mL 0.4100 mL 1.0249 mL
    25 mM 0.0328 mL 0.1640 mL 0.3280 mL 0.8199 mL
    30 mM 0.0273 mL 0.1367 mL 0.2733 mL 0.6833 mL
    40 mM 0.0205 mL 0.1025 mL 0.2050 mL 0.5125 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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    Aliskiren hemifumarate 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:

    Aliskiren hemifumarate173334-58-2CGP 60536 hemifumarate CGP60536B hemifumarate SPP 100 hemifumarateReninAutophagyHypertensioncardiovascular diseasescancercachexiaC26colon carcinomaInhibitorinhibitorinhibit

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