| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
pEC50: 5.53 (GPR109a)[1]
GPR109 receptor agonist-2 specifically targets GPR109a, a G protein-coupled receptor that is activated by nicotinic acid (niacin) and is a key player in lipid metabolism. GPR109a mediates the anti-lipolytic effects of niacin in adipose tissue and has been implicated in anti-inflammatory pathways. By acting as a selective agonist, this compound is used to study the receptor's physiological and pathophysiological roles. |
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| ln Vitro |
In vitro, GPR109 receptor agonist-2 acts as a selective agonist of GPR109a. Its activity is characterized by its potency, with a pEC50 value of 5.53, which corresponds to an EC50 of approximately 3 μM. This confirms its ability to activate the receptor and its utility as a pharmacological tool for studying GPR109a-mediated signaling pathways.
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| ln Vivo |
In vivo activity data for GPR109 receptor agonist-2 are not extensively detailed in the search results. As a selective GPR109a agonist, it is a valuable tool for studying the role of this receptor in various metabolic and inflammatory conditions. It could be used in animal models to investigate the effects of GPR109a activation on lipid metabolism, inflammation, and other related pathways.
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| Enzyme Assay |
For non-cellular in vitro receptor binding assays, GPR109 receptor agonist-2 is characterized using radioligand binding techniques with membrane preparations from cells expressing the GPR109a receptor. These assays confirm its binding affinity and selectivity for the receptor. Its pEC50 value is a key measure of its potency and is determined in such assays.
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| Cell Assay |
For in vitro cellular assays, the activity of GPR109 receptor agonist-2 is evaluated in cells expressing GPR109a. A typical functional assay measures the inhibition of forskolin-stimulated cAMP accumulation, as GPR109a is a Gi-coupled receptor. The compound's ability to inhibit cAMP production confirms its agonistic activity and is used to calculate its pEC50.
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| Animal Protocol |
In vivo animal studies with GPR109 receptor agonist-2 would typically be conducted in mouse or rat models to study the effects of GPR109a activation. For example, it could be used to investigate the receptor's role in atherosclerosis, inflammation, or metabolic syndrome. The compound can be administered via various routes, including oral or intraperitoneal injection, depending on the study design.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for GPR109 receptor agonist-2 are not extensively documented. As a small-molecule agonist with a molecular weight of 154.17, it is expected to have favorable oral bioavailability. It is soluble in DMSO at 200 mg/mL (1297.27 mM), which facilitates formulation for both in vitro and in vivo studies. Specific parameters such as half-life and clearance are not available.
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| Toxicity/Toxicokinetics |
Toxicological data for GPR109 receptor agonist-2 are limited. As a research compound, it is intended for laboratory use only and not for human therapeutic applications. Its safety profile has not been established for clinical use. At the concentrations used in research, it is generally considered to have low toxicity, but standard laboratory safety practices should always be followed.
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| References | |
| Additional Infomation |
GPR109 receptor agonist-2 (Compound 5) is a selective agonist for the GPR109a receptor, with a pEC50 of 5.53. It has a molecular weight of 154.17 and a molecular formula of C7H10N2O2. This compound is a valuable research tool for studying the role of GPR109a in metabolic regulation and inflammation.
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| Molecular Formula |
C7H10N2O2
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|---|---|
| Molecular Weight |
154.17
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| Exact Mass |
154.074
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| CAS # |
957129-38-3
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| PubChem CID |
3159638
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| Appearance |
White to off-white solid powder
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| Density |
1.257±0.06 g/cm3 (20 °C, 760 mmHg)
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| Boiling Point |
383.2±30.0 °C (760 mmHg)
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| LogP |
0.978
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
11
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| Complexity |
161
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCC1=C(C(=NN1)C(=O)O)C
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| InChi Key |
MFNJGDMJKJLUGC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C7H10N2O2/c1-3-5-4(2)6(7(10)11)9-8-5/h3H2,1-2H3,(H,8,9)(H,10,11)
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| Chemical Name |
5-ethyl-4-methyl-1H-pyrazole-3-carboxylic acid
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 6.4863 mL | 32.4317 mL | 64.8635 mL | |
| 5 mM | 1.2973 mL | 6.4863 mL | 12.9727 mL | |
| 10 mM | 0.6486 mL | 3.2432 mL | 6.4863 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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