| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
AMG7703 targets FFA2 (GPR43), a G protein-coupled receptor that is activated by short-chain fatty acids (SCFAs) such as acetate, propionate, and butyrate. FFA2 is expressed on immune cells, including neutrophils, macrophages, and T cells, and plays a critical role in regulating inflammatory and immune responses. AMG7703 is a selective and allosteric agonist of FFA2. It is more selective for FFA2 than for FFA1 (GPR40) and FFA3 (GPR41). By activating FFA2, AMG7703 modulates immune cell function and may reduce excessive immune responses. This makes it a potential therapeutic agent for autoimmune diseases and inflammatory conditions.
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| ln Vitro |
AMG7703 (phenylacetamide 1) (30 μM) is more selective for FFA2 (GPR43) in Chinese hamster ovary cells than it is for FFA1 (GPR40) and FFA3 (GPR41) [1]. AMG7703 (0.041, 0.123, 0.37, 1.11 μM) stimulates the Gαi-coupled signaling pathway and functions as an allosteric agonist of FFA2 [1]. In adipocytes (3T3L1), AMG7703 (1, 3, 10, 30 μM) inhibits lipolysis in a Gαi-dependent manner [1]. With IC50 values of 0.7 μM (hFFA2) and 0.96 μM (mFFA2) for Gαi-coupled cAMP inhibition and 1.27 μM (mFFA2) for Gαq-coupled aequorin inhibition, AMG7703 (0.041, 0.123, 0.37, 1.11 μM) demonstrates allosteric activity[1]. In CHO cells that consistently express hFFA2 and aequorin, AMG7703 (0-1 μM) exhibits favorable synergy with acetate and increases calcium mobilization in a concentration-dependent manner [1].
In vitro studies have characterized AMG7703 as a selective and allosteric agonist of FFA2. It is more selective for FFA2 in Chinese hamster ovary cells than for FFA1 and FFA3. AMG7703 has been studied for its effects on immune cell function. By activating FFA2, it may modulate the production of inflammatory mediators and regulate immune cell activation. These in vitro findings establish AMG7703 as a potent and selective tool for studying FFA2 receptor signaling. |
| ln Vivo |
In vivo activity data for AMG7703 is limited, as the compound is primarily used as a research tool in in vitro studies. However, its mechanism of action—activating FFA2 and modulating immune responses—suggests potential in vivo applications in autoimmune diseases and inflammatory conditions. The compound could be used in animal models to study the effects of FFA2 activation on inflammation and immunity. However, specific in vivo protocols and results, such as dosing regimens, routes of administration, and pharmacokinetic parameters, are not detailed in the available literature.
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| Enzyme Assay |
The in vitro assays for AMG7703 measure its binding to FFA2 and its ability to activate FFA2-mediated signaling. Receptor binding assays are performed using membranes from cells expressing FFA2 and a radiolabeled ligand. Functional assays measure the activation of downstream signaling pathways, such as calcium mobilization or the inhibition of cAMP accumulation. These assays confirm that AMG7703 is a potent and selective agonist of FFA2.
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| Cell Assay |
In vitro cell-based assays for AMG7703 are used to study its effects on FFA2-mediated immune cell function. Immune cells (e.g., neutrophils, macrophages) are treated with AMG7703, and the production of inflammatory mediators is measured. Chemotaxis and other immune cell functions can also be assessed. These cell-based assays confirm that AMG7703 activates FFA2 and modulates immune cell function.
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| Animal Protocol |
In vivo animal experiments for AMG7703 would typically be conducted in models of autoimmune diseases or inflammatory conditions. In a typical study, AMG7703 is administered to animals, and the effects on inflammation and disease severity are assessed. However, specific protocols for AMG7703 are not detailed in the available literature. AMG7703 is an investigational compound being studied for its potential therapeutic applications.
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| ADME/Pharmacokinetics |
AMG7703 has a molecular weight of 294.80 g/mol and a molecular formula of C14H15ClN2OS. It is a solid compound. For storage, it is recommended to keep the compound at -20°C. Pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. AMG7703 is a research compound and is not intended for human or veterinary use.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for AMG7703 is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. AMG7703 is an agonist of FFA2, and its toxicity would be related to its effects on FFA2-mediated signaling in normal tissues. As with all research chemicals, standard laboratory safety precautions should be followed when handling AMG7703. Its use is limited to research applications and it is not intended for human or veterinary use.
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| References | |
| Additional Infomation |
AMG7703 is a research compound and is not approved for any clinical or therapeutic use. It is a selective and allosteric agonist of FFA2 (GPR43), the receptor for short-chain fatty acids (SCFAs). AMG7703 is more selective for FFA2 than for FFA1 and FFA3. It is an investigational compound being studied for its potential therapeutic applications in autoimmune diseases and inflammatory conditions. AMG7703 is used to study FFA2 receptor signaling and its role in inflammation and immunity. Its mechanism of action involves activating FFA2, which modulates immune cell function and may reduce excessive immune responses.
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| Molecular Formula |
C14H15CLN2OS
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| Molecular Weight |
294.797
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| Exact Mass |
294.059
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| CAS # |
1103523-24-5
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| PubChem CID |
854189
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.620
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| LogP |
4.36
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
306
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC(C)[C@@H](C1=CC=C(C=C1)Cl)C(=O)NC2=NC=CS2
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| InChi Key |
AZYDQCGCBQYFSE-LBPRGKRZSA-N
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| InChi Code |
InChI=1S/C14H15ClN2OS/c1-9(2)12(10-3-5-11(15)6-4-10)13(18)17-14-16-7-8-19-14/h3-9,12H,1-2H3,(H,16,17,18)/t12-/m0/s1
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| Chemical Name |
(2S)-2-(4-chlorophenyl)-3-methyl-N-(1,3-thiazol-2-yl)butanamide
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| Synonyms |
AMG7703 AMG 7703 AMG-7703
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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 (~339.21 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 | 3.3921 mL | 16.9607 mL | 33.9213 mL | |
| 5 mM | 0.6784 mL | 3.3921 mL | 6.7843 mL | |
| 10 mM | 0.3392 mL | 1.6961 mL | 3.3921 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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