AM211
Based on 1 Customer Validation
AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
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- Purity: 98.79%
- CAS No.: 1175526-27-8
- 화학식: C27H27F3N2O4
- 분자량:500.51
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
IC50: 4.9 nM (Human DP2), 7.8 nM (Mouse DP2), 4.9 nM (Guinea pig DP2), 10.4 nM (Rat DP2)[1]
AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively. In the presence of 0.2% serum albumin, AM211 inhibits radiolabeled PGD2 binding to human, mouse, guinea pig, and rat DP2 with IC50 values of 12.2, 20.1, 22.9, and 34.2 nM, respectively. AM211 displays high selectivity for DP2 versus other receptors in the prostanoid family, with IC50 values for the inhibition of radioligand binding to human TP, IP, DP1, and FP of more than 100 μM. AM211 (100 μM) shows no activity at COX-1, COX-2 enzymes as well as PPAR family of nuclear receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1175526-27-8
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Appearance Solid
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분자량 500.51
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화학식 C27H27F3N2O4
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Color White to off-white
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SMILES
O=C(O)CC1=CC(C2=CC=C(C(F)(F)F)C=C2CN(CC)C(NCC3=CC=CC=C3)=O)=C(OC)C=C1
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Synonyms
AM211 free acid
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
DMSO : ≥ 125 mg/mL (249.75 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.16 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (4.16 mM); Suspended solution; Need ultrasonic and warming
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Mice[1]
In brief, mice are immunized by an intraperitoneal injection of 10 μg of ovalbumin (OVA) complexed with Imject Alum in a volume of 0.2 mL on days 1 and 8. Seven days later (day 15) mice are challenged intranasally with 20 μL of a 10 mg/mL solution of OVA. The challenge period occurs daily from days 15 to 19. Mice (seven/group) are randomLy assigned to receive either compound (AM211, 10 mg/kg) or vehicle (methyl cellulose, 10 mL/kg) and treated by oral gavage 1 h before each OVA challenge. The number of sneezes are counted for 8 min immediately after the OVA challenge on days 15, 17, and 19 by an independent observer who is blinded to the treatment groups[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
순도&문서
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Data Sheet (277 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9980 mL | 9.9898 mL | 19.9796 mL | 49.9491 mL |
| 5 mM | 0.3996 mL | 1.9980 mL | 3.9959 mL | 9.9898 mL | |
| 10 mM | 0.1998 mL | 0.9990 mL | 1.9980 mL | 4.9949 mL | |
| 15 mM | 0.1332 mL | 0.6660 mL | 1.3320 mL | 3.3299 mL | |
| 20 mM | 0.0999 mL | 0.4995 mL | 0.9990 mL | 2.4975 mL | |
| 25 mM | 0.0799 mL | 0.3996 mL | 0.7992 mL | 1.9980 mL | |
| 30 mM | 0.0666 mL | 0.3330 mL | 0.6660 mL | 1.6650 mL | |
| 40 mM | 0.0499 mL | 0.2497 mL | 0.4995 mL | 1.2487 mL | |
| 50 mM | 0.0400 mL | 0.1998 mL | 0.3996 mL | 0.9990 mL | |
| 60 mM | 0.0333 mL | 0.1665 mL | 0.3330 mL | 0.8325 mL | |
| 80 mM | 0.0250 mL | 0.1249 mL | 0.2497 mL | 0.6244 mL | |
| 100 mM | 0.0200 mL | 0.0999 mL | 0.1998 mL | 0.4995 mL |
AM211 Related Classifications
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