Tryptophan-cholic acid (Synonyms: Trp-CA)

Cat. No.: HY-N15721 Purity: 99.75%: Data Sheet
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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).

For research use only. We do not sell to patients.

Tryptophan-cholic acid Chemical Structure

CAS No. : 1630745-39-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Description

In Vitro

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.

Immunofluorescence^[1]

Cell Line:	GLUTag cells
Concentration:	10 μM
Incubation Time:	24 h
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.

In Vivo

Tryptophan-cholic acid (10 mg/kg; oral gavage; 3 times/week; 2 weeks) improved glucose tolerance, reduced body weight and fat mass, and promoted glucagon-like peptide-1 (GLP-1) and insulin secretion in high-fat diet (HFD)-induced, Mrgpre^-/-, Arrb1^-/-, Arrb2^-/-, and intestine-specific Gnas knockout mouse models. This effect was completely blocked in Mrgpre^-/-, Mrgpre^ΔIE, Arrb1^-/-, and shAldoa mice, and partially attenuated in Arrb2^-/- and Gnas^iKO mice^[1]. Tryptophan-cholic acid (2×10⁸ CFUs Bifidobacterium animalis subsp. lactis/ Escherichia coli-BAL BSH/T; oral gavage; 1 time/week; 2 weeks) improved glucose tolerance and increased GLP-1 and insulin secretion in HFD-induced, Mrgpre^fl/fl, and Mrgpre^ΔIE mouse models. This effect was only observed in Mrgpre^fl/fl mice and completely absent in Mrgpre^ΔIE mice^[1].

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

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; Mrgpre^fl/fl mice, HFD-induced model; Mrgpre^ΔIE mice, HFD-induced model; Arrb1^-/- mice, HFD-induced model; Arrb2^-/- mice, HFD-induced model; Gnas^iKO mice, HFD-inducedmodel; shAldoa mice, HFD-induced model^[1]
Dosage:	10 mg/kg
Administration:	Intragastric gavage, 3 times per week for 2 weeks
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^-/-, Mrgpre^ΔIE, Arrb1^-/-, and shAldoa mice, and partially attenuated in Arrb2^-/- and Gnas^iKO 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 Mrgpre^ΔIE mice.

Molecular Weight

594.78

Formula

C₃₅H₅₀N₂O₆

CAS No.

1630745-39-9

Appearance

Solid

Color

White to off-white

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

Structure Classification

Initial Source

Endogenous metabolite

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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 (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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.20 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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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:

DMSO +

Tween-80 +

Saline

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.

Purity & Documentation

Purity: 99.75%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (251 KB) HNMR (217 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Lin J, et al. A microbial amino-acid-conjugated bile acid, tryptophan-cholic acid, improves glucose homeostasis via the orphan receptor MRGPRE. Cell. 2025 Aug 21;188(17):4530-4548.e25. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

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 Related Classifications

Metabolic Disease

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:

Tryptophan-cholic acid1630745-39-9Trp-CAOrphan GPCRGLP ReceptorRrphan G protein-coupled receptorbile acidGPCRdiabetic micetype 2 diabetesInhibitorinhibitorinhibit

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Tryptophan-cholic acid (Synonyms: Trp-CA)

Tryptophan-cholic acid Related Antibodies

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