2. GPCR/G Protein
  3. Free Fatty Acid Receptor
  4. GPR120 Agonist 3

GPR120 Agonist 3 is a selective Gpr120 agonist with a logEC50 of 7.62.

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GPR120 Agonist 3

GPR120 Agonist 3 構造式

CAS 番号 : 1599477-75-4

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10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO USD 110 在庫あり
Solid
5 mg $100 在庫あり
10 mg $180 在庫あり
25 mg $350 在庫あり
50 mg $500 在庫あり
100 mg $750 在庫あり
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Based on 2 publication(s) in Google Scholar

Other Forms of GPR120 Agonist 3:

GPR120 Agonist 3 関連抗体

Top Publications Citing Use of Products

Free Fatty Acid 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
FFAR1 FFAR2 FFAR3 FFAR4

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製品説明

GPR120 Agonist 3 is a selective Gpr120 agonist with a logEC50 of 7.62.

IC50 & Target

logEC50: 7.62[1]
Cellular Effect
Cell Line Type Value Description References
CHO-K1 EC50
33 1
Compound: 14
Agonist activity at mouse GPR120 expressed in CHOK1 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
Agonist activity at mouse GPR120 expressed in CHOK1 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
[PMID: 28105274]
CHO-K1 EC50
33 1
Compound: 14
Agonist activity at mouse GPR120 expressed in CHOK1 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
Agonist activity at mouse GPR120 expressed in CHOK1 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
[PMID: 28105274]
HEK293 EC50
>10 3
Compound: 14
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
[PMID: 28105274]
CHO-K1 EC50
66 1
Compound: 14
Agonist activity at ARMS2-PK2 -tagged human GPR120 short isoform expressed in CHOK1 cells assessed as induction of beta-arrestin2 recruitment after 90 mins by luminescence assay
Agonist activity at ARMS2-PK2 -tagged human GPR120 short isoform expressed in CHOK1 cells assessed as induction of beta-arrestin2 recruitment after 90 mins by luminescence assay
[PMID: 28105274]
CHO-K1 EC50
66 1
Compound: 14
Agonist activity at ARMS2-PK2 -tagged human GPR120 short isoform expressed in CHOK1 cells assessed as induction of beta-arrestin2 recruitment after 90 mins by luminescence assay
Agonist activity at ARMS2-PK2 -tagged human GPR120 short isoform expressed in CHOK1 cells assessed as induction of beta-arrestin2 recruitment after 90 mins by luminescence assay
[PMID: 28105274]
CHO-K1 EC50
33 1
Compound: 14
Agonist activity at mouse GPR120 expressed in CHOK1 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
Agonist activity at mouse GPR120 expressed in CHOK1 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
[PMID: 28105274]
CHO-K1 EC50
98 1
Compound: 14
Agonist activity at human GPR120 short isoform expressed in CHOK1 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
Agonist activity at human GPR120 short isoform expressed in CHOK1 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
[PMID: 28105274]
CHO-K1 EC50
98 1
Compound: 14
Agonist activity at human GPR120 short isoform expressed in CHOK1 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
Agonist activity at human GPR120 short isoform expressed in CHOK1 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
[PMID: 28105274]
U2OS EC50
54 1
Compound: 14
Agonist activity at mouse GPR120 expressed in U2OS cells assessed as induction of beta-arrestin2 recruitment after 90 mins by luminescence assay
Agonist activity at mouse GPR120 expressed in U2OS cells assessed as induction of beta-arrestin2 recruitment after 90 mins by luminescence assay
[PMID: 28105274]
HEK293 EC50
> 10000 1
Compound: 14
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
[PMID: 28105274]
HEK293 EC50
> 10000 1
Compound: 14
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
Agonist activity at human GPR40 expressed in HEK293 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
[PMID: 28105274]
CHO-K1 EC50
66 1
Compound: 14
Agonist activity at ARMS2-PK2 -tagged human GPR120 short isoform expressed in CHOK1 cells assessed as induction of beta-arrestin2 recruitment after 90 mins by luminescence assay
Agonist activity at ARMS2-PK2 -tagged human GPR120 short isoform expressed in CHOK1 cells assessed as induction of beta-arrestin2 recruitment after 90 mins by luminescence assay
[PMID: 28105274]
U2OS EC50
54 1
Compound: 14
Agonist activity at mouse GPR120 expressed in U2OS cells assessed as induction of beta-arrestin2 recruitment after 90 mins by luminescence assay
Agonist activity at mouse GPR120 expressed in U2OS cells assessed as induction of beta-arrestin2 recruitment after 90 mins by luminescence assay
[PMID: 28105274]
CHO-K1 EC50
98 1
Compound: 14
Agonist activity at human GPR120 short isoform expressed in CHOK1 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
Agonist activity at human GPR120 short isoform expressed in CHOK1 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
[PMID: 28105274]
U2OS EC50
54 1
Compound: 14
Agonist activity at mouse GPR120 expressed in U2OS cells assessed as induction of beta-arrestin2 recruitment after 90 mins by luminescence assay
Agonist activity at mouse GPR120 expressed in U2OS cells assessed as induction of beta-arrestin2 recruitment after 90 mins by luminescence assay
[PMID: 28105274]
体外実験

GPR120 Agonist 3 is fully selective for Gpr120 (logEC50= 7.62) with negligible activity towards Gpr40. GPR120 Agonist 3 produces concentration dependent increases in IP3 production from both human and mouse Gpr120 expressing cells. GPR120 Agonist 3 leads to a concentration-dependent response to recruit β-arrestin-2 in both human and mouse Gpr120 expressing cells, with EC50s of ~0.35 μM. GPR120 Agonist 3 strongly and comparably inhibits LPS-induced phosphorylation of Tak1, Ikkβ, and Jnk and blocked IκB degradation [1].

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

GPR120 Agonist 3 関連抗体
体内実験

GPR120 Agonist 3 causes improved insulin sensitivity with increased glucose infusion rates, enhanced insulin stimulated-glucose disposal rate, along with a marked increase in the ability of insulin to suppress hepatic glucose production only in WT mice. GPR120 Agonist 3 treatment has beneficial effects on hepatic lipid metabolism, causing decreased hepatic steatosis, decreased liver triglycerides, and DAGs, along with reduced saturated free fatty acid conten[1].

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

405.84

分子式

C19H23ClF3NO3
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)CC(CC1)CCC21CCN(C3=CC(OC(F)(F)F)=CC=C3Cl)CC2
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 : ≥ 50 mg/mL (123.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4640 mL 12.3201 mL 24.6403 mL
5 mM 0.4928 mL 2.4640 mL 4.9281 mL
10 mM 0.2464 mL 1.2320 mL 2.4640 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

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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

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体積 （開始）

V1

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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 (6.16 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 (6.16 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:

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(per animal)

g

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(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:
%
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% 
+
%
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%
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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).
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: 99.51%

COA (245 KB) HNMR (171 KB) LCMS (106 KB)

取扱説明書 (2659 KB)
参考文献
動物実験
[1]

Mice: Male C57Bl/6 WT or Gpr120 KO littermates are fed a normal chow (13.5% fat) or high-fat diet (60% fat) ad libitum for 15-20 weeks from 8 weeks of age. After 15 weeks on HFD, WT and Gpr120 KO mice are switched to an isocaloric HFD supplemented with ω3-FA concentrate or 30 mg/kg GPR120-IN-1 and fed for 5 weeks. Mice receive fresh diet every 3rd day, and food consumption and body weight are monitored[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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4640 mL 12.3201 mL 24.6403 mL 61.6006 mL
5 mM 0.4928 mL 2.4640 mL 4.9281 mL 12.3201 mL
10 mM 0.2464 mL 1.2320 mL 2.4640 mL 6.1601 mL
15 mM 0.1643 mL 0.8213 mL 1.6427 mL 4.1067 mL
20 mM 0.1232 mL 0.6160 mL 1.2320 mL 3.0800 mL
25 mM 0.0986 mL 0.4928 mL 0.9856 mL 2.4640 mL
30 mM 0.0821 mL 0.4107 mL 0.8213 mL 2.0534 mL
40 mM 0.0616 mL 0.3080 mL 0.6160 mL 1.5400 mL
50 mM 0.0493 mL 0.2464 mL 0.4928 mL 1.2320 mL
60 mM 0.0411 mL 0.2053 mL 0.4107 mL 1.0267 mL
80 mM 0.0308 mL 0.1540 mL 0.3080 mL 0.7700 mL
100 mM 0.0246 mL 0.1232 mL 0.2464 mL 0.6160 mL
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GPR120 Agonist 3 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

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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:

GPR120 Agonist 31599477-75-4Free Fatty Acid ReceptorFFARInhibitorinhibitorinhibit

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製品名:
GPR120 Agonist 3
製品番号:
HY-101492
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