Tryptophan-cholic acid
Based on 1 Customer Validation
Tryptophan-cholic acid (Trp-CA) is a microbial amino acid-conjugated bile acid that acts as an endogenous ligand and agonist (EC50=9.6 μM) for the orphan G protein-coupled receptor (GPCR) MRGPRE (Mas-related G protein-coupled receptor family member E). Tryptophan-cholic acid is orally effective but has poor oral absorption and does not cross the blood-brain barrier. Tryptophan-cholic acid promotes the secretion of glucagon-like peptide GLP-1, thereby improving glucose tolerance in diabetic mice. Tryptophan-cholic acid improves glucose tolerance, promotes insulin secretion, and alleviates high-fat diet-induced hepatic steatosis without causing pruritus side effects. Tryptophan-cholic acid is primarily used in research on type 2 diabetes (T2D).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 純度: 99.75%
- CAS 番号: 1630745-39-9
- 分子式: C35H50N2O6
- 分子量:594.78
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
Tryptophan-cholic acid (10 μM; 1 h) promotes glucagon-like peptide-1 (GLP-1) secretion in GLUTag, STC-1, and NCI-H716 cells, and this effect is blocked after transfection with siMrgpre[1]. Tryptophan-cholic acid (EC50=9.6 μM) activates MRGPRE-Gs signaling in G protein dissociation experiments in HEK293T cells, and specifically activated MRGPRE at 10 μM through the PRESTO-Tango system[1]. Treatment of GLUTag cells with tryptophan-cholic acid (10 μM; 10 min) induces phosphorylation of aldolase A (ALDOA) ??at the Ser39 site, increasing aldolase activity and intracellular ATP levels, and this effect was inhibited after transfection with siArrb1 or siAldoa[1]. Tryptophan-cholic acid (10 μM; 8 h) has no effect on the activity of TGR5, FXR, VDR, and PXR receptors in receptor luciferase assays in HEK293T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:GLUTag cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Induced the internalization of MRGPRE into early endosome antigen 1 (EEA1)-positive endosomes in GLUTag cells.
Co-immunostaining confirmed the colocalization of MRGPRE with GLP-1 in GLUTag cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (male, 8-week-old), high-fat diet (HFD)-induced type 2 diabetes model; Mrgpre-/- mice (male, 8-week-old), HFD-induced model; Mrgprefl/fl mice, HFD-induced model; MrgpreΔIE mice, HFD-induced model; Arrb1-/- mice, HFD-induced model; Arrb2-/- mice, HFD-induced model; GnasiKO mice, HFD-inducedmodel; shAldoa mice, HFD-induced model[1]
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Dosage:10 mg/kg
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Administration:Intragastric gavage, 3 times per week for 2 weeks
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Result:Significantly reduced the blood glucose levels and area under the curve (AUC) of OGTT in HFD-fed C57BL/6J mice.
This glucose-lowering effect was abolished in Mrgpre-/-, MrgpreΔIE, Arrb1-/-, and shAldoa mice, and partially attenuated in Arrb2-/- and GnasiKO mice.
Colonization with B. animalis subsp. lactis or E. coli-BAL BSH/T also improved glucose tolerance in HFD-fed mice, which was absent in MrgpreΔIE mice.
化学情報
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CAS 番号 1630745-39-9
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性状 Solid
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分子量 594.78
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分子式 C35H50N2O6
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Color White to off-white
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SMILES
O[C@H]1[C@@]2([H])[C@@]3([H])[C@@]([C@@](CC3)([H])[C@H](C)CCC(N[C@H](C(O)=O)CC4=CNC5=CC=CC=C45)=O)([C@H](C[C@]2([H])[C@@]6([C@](C[C@@H](CC6)O)([H])C1)C)O)C
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別名
Trp-CA
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Structure Classification
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Initial Source
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (168.13 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.20 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.20 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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データシート (279 KB)
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SDS (251 KB)
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- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
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. 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 |
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| DMSO | 1 mM | 1.6813 mL | 8.4065 mL | 16.8129 mL | 42.0323 mL |
| 5 mM | 0.3363 mL | 1.6813 mL | 3.3626 mL | 8.4065 mL | |
| 10 mM | 0.1681 mL | 0.8406 mL | 1.6813 mL | 4.2032 mL | |
| 15 mM | 0.1121 mL | 0.5604 mL | 1.1209 mL | 2.8022 mL | |
| 20 mM | 0.0841 mL | 0.4203 mL | 0.8406 mL | 2.1016 mL | |
| 25 mM | 0.0673 mL | 0.3363 mL | 0.6725 mL | 1.6813 mL | |
| 30 mM | 0.0560 mL | 0.2802 mL | 0.5604 mL | 1.4011 mL | |
| 40 mM | 0.0420 mL | 0.2102 mL | 0.4203 mL | 1.0508 mL | |
| 50 mM | 0.0336 mL | 0.1681 mL | 0.3363 mL | 0.8406 mL | |
| 60 mM | 0.0280 mL | 0.1401 mL | 0.2802 mL | 0.7005 mL | |
| 80 mM | 0.0210 mL | 0.1051 mL | 0.2102 mL | 0.5254 mL | |
| 100 mM | 0.0168 mL | 0.0841 mL | 0.1681 mL | 0.4203 mL |
Tryptophan-cholic acid 関連分類
HY-N15721 関連分類
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