| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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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].
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| 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].
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| References |
| 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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