1. GPCR/G Protein
  2. GnRH Receptor
  3. Abarelix

Abarelix (R3827; PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.

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No. CAS : 183552-38-7

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
100 mg   Obtener un presupuesto  
200 mg   Obtener un presupuesto  

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Revisión del cliente

Based on 1 publication(s) in Google Scholar

Other Forms of Abarelix:

Top Publications Citing Use of Products
WB

    Abarelix purchased from MedChemExpress. Usage Cited in: Am J Physiol Endocrinol Metab. 2020 Jul 1;319(1):E81-E90.  [Abstract]

    EPHA7, ERα, and ERβ protein expression in the hypothalamus of abarelix-treated rats injected with EPHA7-Fc.
    • Actividad biológica

    • Pureza y Documentación

    • Referencias

    • Revisión del cliente

    Descripciòn

    Abarelix (R3827; PPI 149) is a potent gonadotrophin-releasing hormone (GnRH) antagonist, used for prostate cancer treatment.

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    3.5 nM
    Compound: 4 (Abarelix)
    Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
    Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
    [PMID: 11462984]
    In Vitro

    Abarelix (30 and 300 µg/mL) causes significantly increased histamine release[1]. Abarelix is the first GnRH antagonist to be developed, and can produce rapid and sustained decreases in testosterone to castrate levels without the need for co-administration of an antiandrogen, and with a very low complication rate in the short term[2]. Abarelix demonstrates to promptly and substantially reduce follicle-stimulating hormone levels to lower than LHRH agonist. Abarelix does not cause a surge in serum testosterone that can precipitate a flare phenomenon or worsening of disease, particularly dangerous for patients with metastatic, symptomatic disease, and produces medical castration more quickly[3].

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

    Ensayo clínico
    Peso molecular

    1416.06

    Fòrmula

    C72H95ClN14O14

    No. CAS
    Appearance

    Solid

    Color

    White to off-white

    Sequence Shortening

    Ac-{d-2-Nal}-{d-4-Cpa}-{d-3-Pal}-S-{NMyr}-{d-Asp}-L-K(ipr)-P-{d-Ala}-NH2

    Envío

    Room temperature in continental US; may vary elsewhere.

    Almacenamiento

    Sealed storage, away from moisture

    Powder -80°C 2 years
    -20°C 1 year

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

    Solvente y solubilidad
    In Vitro: 

    DMSO : 100 mg/mL (70.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 42 mg/mL (29.66 mM; Need ultrasonic and warming)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.7062 mL 3.5309 mL 7.0618 mL
    5 mM 0.1412 mL 0.7062 mL 1.4124 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.

    • Calculadora de molaridad

    • Calculadora de dilución

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

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

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

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    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).
    Pureza y Documentación

    Purity: 99.72%

    Referencias

    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 / DMSO 1 mM 0.7062 mL 3.5309 mL 7.0618 mL 17.6546 mL
    5 mM 0.1412 mL 0.7062 mL 1.4124 mL 3.5309 mL
    10 mM 0.0706 mL 0.3531 mL 0.7062 mL 1.7655 mL
    15 mM 0.0471 mL 0.2354 mL 0.4708 mL 1.1770 mL
    20 mM 0.0353 mL 0.1765 mL 0.3531 mL 0.8827 mL
    25 mM 0.0282 mL 0.1412 mL 0.2825 mL 0.7062 mL
    DMSO 30 mM 0.0235 mL 0.1177 mL 0.2354 mL 0.5885 mL
    40 mM 0.0177 mL 0.0883 mL 0.1765 mL 0.4414 mL
    50 mM 0.0141 mL 0.0706 mL 0.1412 mL 0.3531 mL
    60 mM 0.0118 mL 0.0588 mL 0.1177 mL 0.2942 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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    • 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.

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    Inquiry Information

    Nombre del producto:
    Abarelix
    Cat. No.:
    HY-13534
    Cantidad:
    MCE Japan Authorized Agent: