AMG 853

Catalog # Availability Size / Price Qty
5701/10
Cat.No. 5701 - AMG 853 | C28H27Cl2FN2O6S | CAS No. 1169483-24-2
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Description: Potent dual CRTH2 and prostaglandin D2 (PGD2) receptor antagonist

Chemical Name: 5-Chloro-4-[2-[[(2-chloro-4-cyclopropylphenyl)sulfonyl]amino]-4-[[(1,1-dimethylethyl)amino]carbonyl]phenoxy]-2-fluorobenzeneacetic acid

Purity: ≥98%

Product Details
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Reviews (1)

Biological Activity

Potent dual CRTH2 and prostaglandin D2 (PGD2) receptor antagonist (IC50 values are 8 and 35 nM, respectively in plasma). Inhibits PGD2-induced down modulation of CRTH2 on CD16- granulocytes in human whole blood as well as PGD2-induced cAMP response in platelets. Inhibits PGD2-induced airway constriction in vivo. Also inhibits BRD4 (Kd = 170 nM). Orally bioavailable.

Technical Data

M.Wt:
609.49
Formula:
C28H27Cl2FN2O6S
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
1169483-24-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Discovery of AMG 853, a CRTH2 and DP dual antagonist.
    Liu et al.
    ACS Med.Chem.Lett., 2011;2:326

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AMG 853 blocks p38 phosphorylation in 15d-PGJ2 treated cardiomyocytes
By Chintan Koyani on 12/10/2018
Species: Mouse

HL-1 cardiomyocytes were pre-incubated with AMG 853 (1 µM, 30 min) followed by treatment with 15d-PGJ2 (15 µM, 30 min) to follow p38 activation using Western blot analysis. AMG 853 inhibited 15d-induced p38 phosphorylation.


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