| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Prostaglandin D2 receptor 2 (DP2/CRTh2). AM211 is a potent and selective antagonist of the DP2 receptor, blocking PGD2-induced signaling. The DP2 receptor is a G protein-coupled receptor expressed on Th2 cells, eosinophils, basophils, and other immune cells. Antagonism of this receptor reduces allergic inflammation by inhibiting chemotaxis and activation of these cells.
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| ln Vitro |
AM211 is an oral bioavailable, powerful, selective prostaglandin D2 (PGD2) type 2 receptor (DP2) antagonist. Its IC50 for DP2 in humans, mice, guinea pigs, and rats is 4.9 nM. 4.9 nM, 10.4 nM, 7.8 nM. In the presence of 0.2% serum albumin, AM211 inhibits the binding of radiolabeled PGD2 to human, mouse, guinea pig, and rat DP2 with IC50 values of 12.2, 20.1, 22.9, and 34.2 nM, respectively. AM211 has superior selectivity for DP2 as compared to other prostaglandin family receptors. It also inhibits radioligand binding to human TP, IP, DP1, and FP, with IC50 values higher than 100 μM. AM211 (100 μM) exhibits no effect against the PPAR nuclear receptor family, COX-1, or COX-2 enzymes [1].
AM211 demonstrates potent and selective antagonist activity at the DP2 receptor in vitro, with IC50 values in the low nanomolar range. The compound inhibits PGD2-induced chemotaxis of Th2 cells and eosinophils. It shows high selectivity for DP2 over other prostanoid receptors such as DP1, EP, FP, IP, and TP. Its in vitro potency and selectivity have been characterized in receptor binding and functional assays. |
| ln Vivo |
AM211 (1, 10 and 30 mg/kg, orally) dose-dependently reduced DK-PGD2-induced peripheral blood leukocyte counts with an estimated ED50 of 0.85 mg/kg. AM211 (30 mg/kg) also decreases antigen-induced lung inflammation in guinea pigs. AM211 (10 mg/kg, orally) effectively lowers ovalbumin (OVA)-induced sneeze in a mouse model of allergic rhinitis [1].
In vivo, AM211 has been shown to reduce allergic inflammation in animal models of asthma and allergic rhinitis. The compound inhibits PGD2-induced eosinophilia and Th2 cytokine production. It has demonstrated efficacy in reducing airway hyperresponsiveness and inflammation in preclinical studies. The compound is being evaluated for its potential in treating allergic diseases. |
| Enzyme Assay |
In vitro receptor binding assays for AM211 involve competition binding experiments using radiolabeled PGD2 or a selective DP2 ligand. Membranes are prepared from cells expressing the DP2 receptor. AM211 is incubated at varying concentrations, and bound radioactivity is measured. Ki values are calculated from displacement curves. Functional assays measure inhibition of PGD2-induced chemotaxis or calcium mobilization.
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| Cell Assay |
Cellular assays for AM211 involve culturing immune cells such as Th2 cells, eosinophils, or basophils. Cells are treated with AM211 and stimulated with PGD2. Chemotaxis is measured using transwell assays. Calcium mobilization is measured using fluorescent indicators. Cytokine production is measured by ELISA. The compound's ability to inhibit PGD2-induced cellular responses is assessed.
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| Animal Protocol |
In vivo animal studies for AM211 have been conducted in mouse models of allergic inflammation, such as ovalbumin-induced asthma. The compound is typically administered orally or intraperitoneally. Airway hyperresponsiveness, eosinophilia, and Th2 cytokine levels are measured. Dosing regimens vary, but the compound has been shown to be effective at reducing allergic inflammation in preclinical models.
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| ADME/Pharmacokinetics |
AM211 is a small molecule with favorable pharmacokinetic properties in preclinical studies. It is orally bioavailable and has been shown to achieve therapeutic concentrations in target tissues. The compound is metabolized in the liver and excreted via the biliary and renal routes. Detailed pharmacokinetic parameters such as half-life and bioavailability have been characterized in animal models.
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| Toxicity/Toxicokinetics |
AM211 has shown a favorable safety profile in preclinical studies, with no significant toxicity observed at therapeutic doses. The compound is generally well-tolerated in animal models. However, comprehensive toxicological data are limited. The compound is intended for research use only and is not approved for human therapeutic applications.
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| References | |
| Additional Infomation |
AM211 is a potent and selective DP2/CRTh2 receptor antagonist with potential applications in allergic and inflammatory diseases. It has shown efficacy in preclinical models of asthma and allergic rhinitis. The compound is not approved for clinical use and is available for research purposes only. Further clinical development is needed to evaluate its therapeutic potential.
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| Molecular Formula |
C27H27N2O4F3
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|---|---|
| Molecular Weight |
500.50948
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| Exact Mass |
500.192
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| CAS # |
1175526-27-8
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| Related CAS # |
1175526-27-8 (free acid);1263077-74-2 (sodium);
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| PubChem CID |
44158492
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| Appearance |
White to off-white solid powder
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| LogP |
5.944
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
36
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| Complexity |
714
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OPXIRFWNLBDKQB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H27F3N2O4/c1-3-32(26(35)31-16-18-7-5-4-6-8-18)17-20-15-21(27(28,29)30)10-11-22(20)23-13-19(14-25(33)34)9-12-24(23)36-2/h4-13,15H,3,14,16-17H2,1-2H3,(H,31,35)(H,33,34)
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| Chemical Name |
2-[3-[2-[[benzylcarbamoyl(ethyl)amino]methyl]-4-(trifluoromethyl)phenyl]-4-methoxyphenyl]acetic 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) |
DMSO : ≥ 125 mg/mL (~249.75 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.16 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.08 mg/mL (4.16 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.16 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9980 mL | 9.9898 mL | 19.9796 mL | |
| 5 mM | 0.3996 mL | 1.9980 mL | 3.9959 mL | |
| 10 mM | 0.1998 mL | 0.9990 mL | 1.9980 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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