2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. AM211

AM211  (Synonyms: AM211 free acid)

Cat. No.: HY-13213 Purity: 98.79%
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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.

For research use only. We do not sell to patients.

AM211 Chemical Structure

AM211 Chemical Structure

CAS No. : 1175526-27-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 105 In-stock
Solution
10 mM * 1 mL in DMSO USD 105 In-stock
Solid
5 mg USD 95 In-stock
10 mg USD 150 In-stock
25 mg USD 300 In-stock
50 mg USD 460 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of AM211:

AM211 Related Antibodies

Top Publications Citing Use of Products

View All Prostaglandin Receptor Isoform Specific Products:

View All Isoforms
DP EP FP IP TXA2/TP TXB2

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

IC50 & Target

IC50: 4.9 nM (Human DP2), 7.8 nM (Mouse DP2), 4.9 nM (Guinea pig DP2), 10.4 nM (Rat DP2)[1]
In Vitro

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.

AM211 Related Antibodies
In Vivo

AM211 (1, 10, and 30 mg/kg, p.o.) dose-dependently decreases in the number of DK-PGD2-induced peripheral blood leukocytes, with a calculated ED50 of 0.85 mg/kg. AM211 (30 mg/kg) also decreases antigen-induced pulmonary inflammation in guinea pigs. AM211 (10 mg/kg, p.o.) causes significant decrease in ovalbumin (OVA)-induced sneezing in a mouse model of allergic rhinitis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

500.51

Formula

C27H27F3N2O4
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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
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AM211 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AM2111175526-27-8AM 211AM-211Prostaglandin ReceptorInhibitorinhibitorinhibit

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