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| Targets |
Gamma-Glu-Abu TFA specifically targets the calcium-sensing receptor (CaSR), a G-protein coupled receptor that is primarily expressed in the parathyroid gland, kidneys, and bone, but also in many other tissues. The CaSR detects extracellular calcium (Ca2+) levels and modulates parathyroid hormone (PTH) secretion, renal calcium reabsorption, and bone remodeling. As a potent CaSR agonist, Gamma-Glu-Abu activates the receptor by binding to its orthosteric site (where calcium binds) or possibly an allosteric site, leading to downstream signaling cascades that are essential for maintaining mineral ion homeostasis.
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| ln Vitro |
Gamma-Glu-Abu TFA is a potent CaSR agonist. In functional assays using HEK-293 cells expressing the CaSR, the compound activates the receptor with an EC₅0 of 0.21 uM. This indicates that it is a highly potent activator of CaSR signaling. As an agonist, it is used to study the pharmacology of CaSR and to investigate its role in various physiological processes, including the regulation of PTH secretion and renal calcium handling. It is also used as a positive control in screening assays for CaSR modulators.
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| ln Vivo |
In vivo, the activation of CaSR by agonists like Gamma-Glu-Abu leads to a decrease in parathyroid hormone (PTH) secretion and an increase in renal calcium excretion. While not a therapeutic drug, this compound is a valuable research tool for studying the downstream effects of CaSR activation. It is not intended for direct in vivo use as a drug, but studies of gamma-glutamyl dipeptides suggest they can be metabolized and may influence CaSR signaling in the gastrointestinal tract and other organs. It is primarily used in in vitro pharmacology.
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| Enzyme Assay |
An in vitro functional cell-based assay for CaSR agonism measures the mobilization of intracellular calcium (Ca2+). HEK-293 cells stably or transiently expressing the human CaSR are seeded in 96-well clear-bottom plates (1-2×10⁴ cells/well). The cells are loaded with a fluorescent calcium indicator dye (e.g., Fluo-4 AM, 2-5 uM) in assay buffer (HBSS with 20 mM HEPES, pH 7.4) for 30-60 minutes at 37degC. Following dye loading, cells are washed and placed in a fluorescence plate reader. Varying concentrations of Gamma-Glu-Abu TFA (0.1-1000 nM) are added, and the increase in fluorescence (λex/em = 494/516 nm) is recorded. The EC₅0 (0.21 uM) is calculated from the dose-response curve.
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| Cell Assay |
Not directly applicable. Gamma-Glu-Abu TFA is used in cell-based assays as described above. The standard protocol involves calcium mobilization assays in HEK-293 cells expressing the CaSR. Cells are cultured in DMEM with 10% FBS. Prior to the assay, cells are washed with HBSS and loaded with a calcium-sensitive dye. After dye loading and washing, the cells are treated with various concentrations of Gamma-Glu-Abu TFA. The resulting calcium flux is measured by a fluorescence plate reader, and the EC₅0 is calculated. The assay is typically performed in triplicate to ensure reproducibility.
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| Animal Protocol |
No standard in vivo animal protocol exists for this compound as a therapeutic agent. However, for metabolism studies, the compound can be administered to rodents (e.g., mice) via intraperitoneal (IP) injection or oral gavage. Blood and urine samples are collected over time to measure the concentration of Gamma-Glu-Abu and its metabolites by LC-MS/MS. This can be used to study the metabolic stability and bioavailability of the dipeptide. The compound is not intended for therapeutic use in animals.
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| ADME/Pharmacokinetics |
Gamma-Glu-Abu TFA (MW 346.26) is a small, polar dipeptide. It is expected to have a short plasma half-life (< 1-2 h) due to rapid metabolism by peptidases and renal clearance. The TFA salt form enhances its water solubility for in vitro use. For research use, it is typically stored as a powder at -20degC and protected from light. No detailed PK data is available for therapeutic use as it is not a drug candidate.
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| Toxicity/Toxicokinetics |
Standard safety precautions for handling research chemicals apply. Gamma-Glu-Abu TFA is for research use only and is not intended for human consumption. It may cause skin and eye irritation (H315, H319). For handling, use personal protective equipment (gloves, lab coat, eye protection), work in a fume hood, avoid inhalation and skin contact.
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| References | |
| Additional Infomation |
Gamma-Glu-Abu TFA is a research-grade dipeptide agonist of the calcium-sensing receptor (CaSR, EC₅0 = 0.21 uM). It is not an FDA-approved drug. It is used as a tool to study CaSR signaling in vitro, particularly in the context of calcium homeostasis, hormone secretion, and renal function. For research use only, not for diagnostic or therapeutic applications. Storage: powder at -20degC for 3 years, 4degC for 2 years; in solvent at -80degC for 6 months, -20degC for 1 month.
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| Molecular Formula |
C11H17F3N2O7
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| Molecular Weight |
346.26
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| Appearance |
Solid powder
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ≥ 50 mg/mL (~144.40 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8880 mL | 14.4400 mL | 28.8800 mL | |
| 5 mM | 0.5776 mL | 2.8880 mL | 5.7760 mL | |
| 10 mM | 0.2888 mL | 1.4440 mL | 2.8880 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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