2. GPCR/G Protein Neuronal Signaling
  3. Melanocortin Receptor
  4. Setmelanotide

Setmelanotide  (Synonyms: RM-493; BIM-22493; IRC-022493)

製品番号: HY-19870 純度: 99.99%
COA 取扱説明書 Technical Support

Setmelanotide (RM-493) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively.

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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。

カスタムペプチド

CAS 番号 : 920014-72-8

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 276 在庫あり
Solution
10 mM * 1 mL in DMSO USD 276 在庫あり
Solid
5 mg $140 在庫あり
10 mg $225 在庫あり
25 mg $360 在庫あり
50 mg $540 在庫あり
100 mg $780 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 8 publication(s) in Google Scholar

Other Forms of Setmelanotide:

Setmelanotide 関連抗体

Top Publications Citing Use of Products

    Setmelanotide purchased from MedChemExpress. Usage Cited in: Sci Transl Med. 2025 Jan 15;17(781):eadr6459.  [Abstract]

    Setmelanotide (2 mg/kg; i.p.; once daily for 9 d) reduced body weights and food intake and improved glucose tolerance of HFD-fed OtpQ153R/+ mice, which quickly regained body weight after the treatment was discontinued.

    Setmelanotide purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Jul 5;218(7):e20202484.  [Abstract]

    Setmelanotide (100 nM) blocked the risperidone-induced hyperpolarization of MC4RPVH neurons.

    Setmelanotide purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Jul 5;218(7):e20202484.  [Abstract]

    A single dose of Setmelanotide (SET) (2 mg/kg; i.p.) suppressed fast-induced refeeding in Mc4rfl/fl mice.

    Setmelanotide purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Jul 5;218(7):e20202484.  [Abstract]

    Infusion of Setmelanotide (SET) (2 mg/kg; once daily for 14 d) attenuated hyperphagia in C57BL/6 mice fed with risperidone.

    Setmelanotide purchased from MedChemExpress. Usage Cited in: J Exp Med. 2021 Jul 5;218(7):e20202484.  [Abstract]

    Setmelanotide (SET) (2 mg/kg; once daily for 14 d) caused accelerated glucose clearance of C57BL/6 mice fed with risperidone in a GTT.

    Melanocortin 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
    MC1R MC3R MC2R MC4R MC5R

    • 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

    Setmelanotide (RM-493) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively[1].

    IC50 & Target

    Ki:3.9 nM (hMC1R), 10 nM (hMC3R), 2.1 nM (hMC4R), 430 nM (hMC5R), 2.7 nM (rMC4R)[1]
    EC50: 5.8 nM (hMC1R), 5.3nM (hMC3R), 0.27 nM (hMC4R), 0.28 (rMC4R), 1600 nM (hMC5R)[1]
    体外実験

    Melanocortin receptor agonists act in the brain to regulate food intake and body weight and, independently of these actions. Setmelanotide exhibits agonist activity to human and rat MC4R with Kis of 2.1 and 2.7 nM and EC50s of 0.27 and 0.28 nM, respectively[1].

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

    Setmelanotide 関連抗体
    体内実験

    Inhibition of refeeding after an overnight fast by Setmelanotide is dependent on functional MC4R, and does not require MC3R. BIM-22493 acutely improves glucose homeostasis. Lepob/Lepob mice treated with BIM-22493 exhibits significantly improved glucose clearance when compared to controls. Chronic BIM-22493 treatment was associated with significantly lower levels of serum glucose and HOMA-IR values[1].
    Treatment with setmelanotide results in transient decreases in food intake (35%), with persistent weight loss over 8 weeks of treatment (13.5%) in a diet-induced obese nonhuman primate model[2].

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

    1117.31

    分子式

    C49H68N18O9S2
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    Sequence

    Ac-Arg-Cys-{d-Ala}-His-{d-Phe}-Arg-Trp-Cys-NH2 (Disulfide bridge:Cys2-Cys8)
    Sequence Shortening

    Ac-RC-{d-Ala}-H-{d-Phe}-RWC-NH2 (Disulfide bridge:Cys2-Cys8)
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Sealed storage, away from moisture
    Powder -80°C 2 years
      -20°C 1 year
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (89.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 58.33 mg/mL (52.21 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 0.8950 mL 4.4750 mL 8.9501 mL
    5 mM 0.1790 mL 0.8950 mL 1.7900 mL
    10 mM 0.0895 mL 0.4475 mL 0.8950 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
    ×
    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 (2.24 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 (2.24 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.
    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

    純度: 99.99%

    COA (260 KB) RP-HPLC (263 KB) MS (68 KB) Elemental Analysis Report (119 KB)

    取扱説明書 (2659 KB)
    参考文献
    動物実験
    [1]

    Mice: Mice are weighed. Baseline blood glucose is measured and 2 g/kg body weight of D-glucose injected by i.p. BIM-22493 is administered chronically at a dose of 300 nmol/kg/day for 14 days by sc. osmotic pump. Controls are administered with 0.9% saline during the same period. Blood glucose is measured at 15, 30, 60, and 120 minutes post injection[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。
    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 / DMSO 1 mM 0.8950 mL 4.4750 mL 8.9501 mL 22.3752 mL
    5 mM 0.1790 mL 0.8950 mL 1.7900 mL 4.4750 mL
    10 mM 0.0895 mL 0.4475 mL 0.8950 mL 2.2375 mL
    15 mM 0.0597 mL 0.2983 mL 0.5967 mL 1.4917 mL
    20 mM 0.0448 mL 0.2238 mL 0.4475 mL 1.1188 mL
    25 mM 0.0358 mL 0.1790 mL 0.3580 mL 0.8950 mL
    30 mM 0.0298 mL 0.1492 mL 0.2983 mL 0.7458 mL
    40 mM 0.0224 mL 0.1119 mL 0.2238 mL 0.5594 mL
    50 mM 0.0179 mL 0.0895 mL 0.1790 mL 0.4475 mL
    DMSO 60 mM 0.0149 mL 0.0746 mL 0.1492 mL 0.3729 mL
    80 mM 0.0112 mL 0.0559 mL 0.1119 mL 0.2797 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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    Setmelanotide 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:

    Setmelanotide920014-72-8RM-493 BIM-22493 IRC-022493RM493RM 493BIM22493BIM 22493BIM-22493IRC022493IRC 022493IRC-022493Melanocortin ReceptorMC ReceptorInhibitorinhibitorinhibit

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    製品名:
    Setmelanotide
    製品番号:
    HY-19870
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