| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| ln Vitro |
Tryptophan-cholic acid (10 μM; 1 h) promotes the secretion of glucagon-like peptide-1 (GLP-1) in GLUTag, STC-1 and NCI-H716 cells, while this effect is blocked after transfection with siMrgpre[1]. Tryptophan-cholic acid (EC50=9.6 μM) activates the MRGPRE-Gs signaling pathway in G protein dissociation experiments in HEK293T cells and specifically activates MRGPRE at a concentration of 10 μM via 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, thereby increasing aldolase activity and intracellular ATP levels, while this effect is inhibited after transfection with siArrb1 or siAldoa[1]. Tryptophan cholic acid (10 μM; 8 hours) had no effect on the activity of TGR5, FXR, VDR and PXR receptors in HEK293T cell receptor luciferase assays [1].
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| ln Vivo |
Tryptophan-cholic acid (10 mg/kg; gavage; 3 times a week; for 2 weeks) improved glucose tolerance in high-fat diet (HFD) induced Mrgpre-/-, Arrb1-/-, Arrb2-/- and gut-specific Gnas knockout mouse models, reduced body weight and fat mass, and promoted glucagon-like peptide-1 (GLP-1) and insulin secretion. This effect was completely blocked in Mrgpre-/-, MrgpreΔIE, Arrb1-/- and shAldoa mice, and partially attenuated in Arrb2-/- and GnasiKO mice [1]. Tryptophan-cholic acid (2 × 10⁸ CFU Bifidobacterium lactis/Escherichia coli-BAL BSH/T; gavage; once a week; for 2 weeks) improved glucose tolerance in high-fat diet induced Mrgprefl/fl and MrgpreΔIE mouse models and increased GLP-1 and insulin secretion. This effect was observed only in Mrgprefl/fl mice and was completely absent in MrgpreΔIE mice [1].
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| Cell Assay |
Immunofluorescence [1]
Cell Types: GLUTag cells Tested Concentrations: 10 μM Incubation Duration: 24 hours Experimental Results: MRGPRE was induced to internalize into early endosome antigen 1 (EEA1) positive endosomes in GLUTag cells. Co-immunostained staining confirmed that MRGPRE and GLP-1 were co-localized in GLUTag cells. |
| Animal Protocol |
Animal/Disease Models: C57BL/6J mice (male, 8 weeks old), a high-fat diet (HFD) induced model of type 2 diabetes; Mrgpre-/- mice (male, 8 weeks old), an HFD induced model; Mrgprefl/fl mice, an HFD induced model; MrgpreΔIE mice, an HFD induced model; Arrb1-/- mice, an HFD induced model; Arrb2-/- mice, an HFD induced model; GnasiKO mice, an HFD induced model; shAldoa mice, a high-fat diet induced model [1]
Doses: 10 mg/kg Route of Administration: Gavage, 3 times a week for 2 weeks Experimental Results: It significantly reduced blood glucose levels and the area under the curve (AUC) of the oral glucose tolerance test (OGTT) in C57BL/6J mice fed a high-fat diet. This hypoglycemic effect was lost in Mrgpre-/-, MrgpreΔIE, Arrb1-/-, and shAldoa mice, and partially attenuated in Arrb2-/- and GnasiKO mice. Colonization with Bifidobacterium lactis or Escherichia coli-BAL BSH/T also improved glucose tolerance in high-fat diet-fed mice, an improvement not observed in MrgpreΔIE mice. |
| References |
| Molecular Formula |
C35H50N2O6
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|---|---|
| Molecular Weight |
594.78
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| CAS # |
1630745-39-9
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| Appearance |
White to off-white solid
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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
|
| Synonyms |
Trp-CA
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~168.13 mM; with sonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.20 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of physiological saline: Dissolve 0.9 g of sodium chloride in double-distilled water and dilute to 100 mL to obtain clear physiological saline. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.20 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you canAdd 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD saline (4°C, store for one week): Dissolve 2 g of SBE-β-CD powder in 10 mL of saline until completely dissolved and clear. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.20 mM)(saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6813 mL | 8.4065 mL | 16.8129 mL | |
| 5 mM | 0.3363 mL | 1.6813 mL | 3.3626 mL | |
| 10 mM | 0.1681 mL | 0.8406 mL | 1.6813 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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