1. GPCR/G Protein
  2. Prostaglandin Receptor

AM211 (Synonyms: AM211 free acid)

Cat. No.: HY-13213 Purity: 99.94%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 590 In-stock
Estimated Time of Arrival: December 31
100 mg USD 990 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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].

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].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (249.75 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" 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
10 mM 0.1998 mL 0.9990 mL 1.9980 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.16 mM); Clear solution

  • 3.

    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

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
Molecular Weight

500.51

Formula

C₂₇H₂₇F₃N₂O₄

CAS No.

1175526-27-8

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Product Name:
AM211
Cat. No.:
HY-13213
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AM211

Cat. No.: HY-13213