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| 1mg |
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| 10mg |
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| Other Sizes |
| Targets |
The primary target of TLQP-21 TFA is the complement component 3a receptor 1 (C3aR1), a GPCR involved in the complement system and immune response. TLQP-21 acts as a potent agonist for this receptor, with half-maximal effective concentration (EC50) values of 10.3 microM for the mouse receptor and 68.8 microM for the human receptor [38L20-L21]. Activation of C3aR1 by TLQP-21 induces an increase in intracellular calcium (Ca2+) levels, a classic signaling event of GPCR activation. Its target pathway is the complement system and the immunology/inflammation signaling pathways.
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| ln Vitro |
The peptide TLQP-21 TFA is made up of 21 amino acids. TLQP-21 induces up to 69% of the equivalent contraction induced by acetylcholine at a concentration of 3 μM [1][2].
In vitro, TLQP-21 TFA has demonstrated significant biological activity. At a dose of 3 microM, it induces up to ~69% of the corresponding contraction promoted by acetylcholine, indicating potent activity in functional assays. This activity is mediated through its binding to the C3aR1 receptor. The peptide also protects cerebellar granule cells (CGCs) from apoptosis induced by serum and potassium deprivation, highlighting a key neuroprotective function. It is a tool for investigating the effects of VGF-derived peptides on basic cellular functions. |
| ln Vivo |
In vivo studies have demonstrated that TLQP-21 TFA can affect whole-body metabolism. It increases energy expenditure and prevents the early phase of diet-induced diabetes in animal models, suggesting potential applications in metabolic research. The peptide is involved in the regulation of nociception (pain sensation) and other relevant physiologic functions, which are being actively explored in scientific studies. Its in vivo activity is a subject of ongoing research to understand its role as an endocrine hormone.
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| Enzyme Assay |
Cell-free binding assays can be used to determine the affinity of TLQP-21 for the C3aR1 receptor. A common method is a radioligand binding assay using membranes from cells that overexpress the C3aR1 receptor. The membranes are incubated with a fixed concentration of a radiolabeled C3aR1 antagonist (e.g., [125I]-C3a) in the presence of increasing concentrations of unlabeled TLQP-21. After incubation at room temperature for 1 hour, the reaction is filtered through a glass fiber filter to separate bound from free ligand. The filters are washed, and the remaining radioactivity (bound ligand) is counted using a gamma counter. The IC50 value for TLQP-21 in displacing the radiolabeled antagonist can be calculated.
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| Cell Assay |
For cellular assays, a commonly used method is a Ca2+ mobilization assay, as C3aR1 is a GPCR that signals through G proteins to increase intracellular Ca2+. Cells expressing the human or mouse C3aR1 are loaded with a fluorescent Ca2+ indicator dye (e.g., Fluo-4 AM) for 30-60 minutes at 37degC. After washing, the cells are placed on a fluorescence plate reader (e.g., FLIPR). Varying concentrations of TLQP-21 TFA are added to the cells, and the resulting increase in fluorescence (which is proportional to the intracellular Ca2+ level) is measured in real-time. The EC50 values for the agonist can be calculated from the concentration-response curves.
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| Animal Protocol |
In vivo efficacy studies are typically conducted in rodent models of diabetes or obesity. For a metabolic study, male C57BL/6J mice are fed a high-fat diet (HFD) for several weeks to induce obesity and insulin resistance. TLQP-21 TFA is administered via intraperitoneal (IP) or intracerebroventricular (ICV) injection at a dose of 10-100 microg/mouse, either acutely or chronically (e.g., daily for 2 weeks). Energy expenditure is measured using metabolic cages (indirect calorimetry) to monitor oxygen consumption (VO2) and carbon dioxide production (VCO2). Glucose tolerance tests (GTT) and insulin tolerance tests (ITT) are performed by administering a glucose load (e.g., 2 g/kg IP) or insulin (e.g., 0.75 U/kg IP) and measuring blood glucose levels at various time points.
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| ADME/Pharmacokinetics |
The pharmacokinetic (PK) properties of the 21-amino acid peptide TLQP-21 TFA are not well-characterized in the public domain, as it is primarily a research tool. As a peptide, it is likely to be rapidly degraded by proteases in the bloodstream and has a relatively short half-life. This is a common characteristic of small peptide therapeutics and necessitates multiple dosing or specific formulations for in vivo studies. The TFA salt counterion is used to improve the solubility and stability of the peptide for handling and storage. It is commonly provided as a lyophilized powder from a 0.1% TFA in water solution.
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| Toxicity/Toxicokinetics |
Formal toxicity data for TLQP-21 TFA is not publicly available. As a peptide derived from the VGF protein, it is generally considered to have a low toxicity profile in research settings. However, the C3aR1 receptor is involved in the complement system, which is a key part of the innate immune response. Overactivation of this system could lead to unwanted inflammation. This product is for research use only, and safety precautions should be followed. In in vivo studies reported in the literature, the peptide was administered at the specified doses without reported adverse effects. Standard laboratory safety practices should be followed when handling the compound.
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| References |
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| Additional Infomation |
TLQP-21 TFA is a biologically active VGF-derived peptide and a potent agonist of the G protein-coupled receptor C3aR1 (complement 3a receptor 1). It has 21 amino acids with the sequence TLQPPASSRRRHFHHALPPAR [38L3-L6]. Research indicates it plays roles in energy balance, neuroprotection, and nociception. It is a valuable chemical probe for studying the C3aR1 receptor and the pleiotropic functions of the VGF protein in metabolic and neurological diseases. This product is strictly for research use only and is not intended for clinical or therapeutic applications.
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| Molecular Formula |
C109H171F3N40O28
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| Molecular Weight |
2546.77
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| Related CAS # |
TLQP-21;869988-94-3
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| Appearance |
White to off-white 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 (~19.63 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 | 0.3927 mL | 1.9633 mL | 3.9265 mL | |
| 5 mM | 0.0785 mL | 0.3927 mL | 0.7853 mL | |
| 10 mM | 0.0393 mL | 0.1963 mL | 0.3927 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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