2. Cell Cycle/DNA Damage
    Vitamin D Related/Nuclear Receptor
    Autophagy
  3. PPAR
    Autophagy
  4. GW 501516

GW 501516  (Synonyms: GW 1516; GSK-516)

製品番号: HY-10838 純度: 99.15%
COA 取扱説明書

GW 501516 (GW 1516) is a PPARδ agonist with an EC50 of 1.1 nM.

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GW 501516 構造式

GW 501516 構造式

CAS 番号 : 317318-70-0

容量 価格（税別） 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solution
10 mM * 1 mL in DMSO USD 61 在庫あり
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 61 在庫あり
Estimated Time of Arrival: December 31
Solid
5 mg USD 55 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 85 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 204 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 286 在庫あり
Estimated Time of Arrival: December 31
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

カスタマーレビュー

Based on 11 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GW 501516 purchased from MCE. Usage Cited in: Front Pharmacol. 2018 Jun 28;9:648.  [Abstract]

    Western blot analysis of the protein expression of caspase and Bcl-2 family members in response to GW501516.

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    PPARα PPARβ/δ PPARγ PPAR PPARδ

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    • 純度とドキュメンテーション

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    製品説明

    GW 501516 (GW 1516) is a PPARδ agonist with an EC50 of 1.1 nM[1].

    IC50 & Target[1]

    PPARδ

    1.1 nM (EC50)

    体外実験

    GW 501516 is shown to be the most potent and selective PPARδ agonists known with an EC50 of 1.1 nM against PPARδ and 1000-fold selectivity over the other human subtypes, PPARα and-γ[1]. GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    体内実験

    GW 501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats[2]. GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model[3]. GW 501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice[4].

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

    453.50

    Appearance

    Solid

    分子式

    C21H18F3NO3S2
    CAS 番号
    SMILES

    OC(COC1=CC=C(C=C1C)SCC2=C(N=C(S2)C3=CC=C(C=C3)C(F)(F)F)C)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 100 mg/mL (220.51 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2051 mL 11.0254 mL 22.0507 mL
    5 mM 0.4410 mL 2.2051 mL 4.4101 mL
    10 mM 0.2205 mL 1.1025 mL 2.2051 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (5.51 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.51 mM); Clear solution

    *All of the co-solvents are available by MCE.
    純度とドキュメンテーション

    純度: 99.15%

    COA (245 KB) LCMS (268 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [3]

    GW 501516 is dissolved in DMSO. Cells are starved by incubation in 0.2% FCS DMEM for 9 h, then pre-incubated with GW 501516, at a final concentration of 2.5 and 5 µM, or 0.05% DMSO as control for 3 hours, followed by stimulation with 150 µM palmitate bound to 8.0% BSA for 12 h[3].

    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
    [2][3]

    Rats: Female Sprague Dawley rats, 12 weeks of age, are allocated to a sham-operated group and 3 OVX groups; high-dose GW 501516 (OVX-GW5), low-dose GW 501516 (OVX-GW1), and a control group (OVX-CTR), respectively. Animals receive GW 501516 or vehicle (methylcellulose) daily for 4 months by gavage. Bone mineral density (BMD) is assessed by dual x-ray absorptiometry at the femur, spine, and whole body[2].

    Mice: Mice are randomly allocated to different groups and receive therapeutic diet and treatment. The GW 501516-containing rodent diet is made by evenly adding GW 501516 to the control diet to a final concentration of 0.04% w/w. In the control diet, 10% of the total calories are from fat (5.5% from soybean oil and 4.5% from lard)[3].

    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
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      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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    Keywords:

    GW 501516317318-70-0GW 1516 GSK-516GW501516GW-501516GW1516GW-1516GSK516GSK 516GSK-516PPARAutophagyPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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