AMG 853

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Cat.No. 5701 - AMG 853 | C28H27Cl2FN2O6S | CAS No. 1169483-24-2
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% (HPLC)
Datasheet
Citations
Literature

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
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1169483-24-2
PubChem ID 42641863
InChI Key PFWVGKROPKKEDW-UHFFFAOYSA-N
Smiles ClC1=CC(C2CC2)=CC=C1S(NC3=CC(C(NC(C)(C)C)=O)=CC=C3OC4=C(Cl)C=C(CC(O)=O)C(F)=C4)(=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 60.95 100
ethanol 60.95 100

Preparing Stock Solutions

The following data is based on the product molecular weight 609.49. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.64 mL 8.2 mL 16.41 mL
5 mM 0.33 mL 1.64 mL 3.28 mL
10 mM 0.16 mL 0.82 mL 1.64 mL
50 mM 0.03 mL 0.16 mL 0.33 mL

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Product Datasheets

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References

References are publications that support the products' biological activity.

Liu et al (2011) Discovery of AMG 853, a CRTH2 and DP dual antagonist. ACS Med.Chem.Lett. 2 326 PMID: 24900313


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Keywords: AMG 853, supplier, AMG853, CRTH2, chemoattractant, receptor-homologous, molecule, expressed, on, Th2, cells, PGD2, prostaglandin, receptor, dual, antagonists, antagonism, orally, bioavailable, Prostanoid, Receptors, Tocris Bioscience

Citations for AMG 853

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