BAY-u 3405A suppresor PGD2-induced migration of human eosinophils

BAY-u 3405 (CAS 116649-85-5)

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Synonym: Ramatroban
Application: A suppresor PGD2-induced migration of human eosinophils
CAS Number: 116649-85-5
Purity: >98%
Molecular Weight: 416.47
Molecular Formula: C21H21FN2O4S
* Refer to Certificate of Analysis for lot specific data (including water content).
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BAY-u 3405 suppresses PGD2-induced migration of human eosinophils (IC50 = 170 nM). Potent dual antagonist of TXA2R (TP)/DP2 (CRTH2) prostanoid receptors (Ki values are 4.3, 4.5 and > 10000 nM for hDP2, hTP and hDP1 receptors respectively).


References

1. Sundström, Ewa., et al., 2003. Interactions among three classes of mediators explain antigen-induced bronchoconstriction in the isolated perfused and ventilated guinea pig lung. The Journal of pharmacology and experimental therapeutics. 307(1): 408-18. PMID: 12954791
2. Ishizuka, Toshiaki., et al., 2004. Ramatroban (BAY u 3405): a novel dual antagonist of TXA2 receptor and CRTh2, a newly identified prostaglandin D2 receptor. Cardiovascular drug reviews. 22(2): 71-90. PMID: 15179446
3. Ulven, Trond., et al., 2005. Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist. Journal of medicinal chemistry. 48(4): 897-900. PMID: 15715457

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), ethanol (100 mM), methanol, and DMF (~30 mg/ml). Insoluble in water.
Storage :
Store at -20° C
Melting Point :
134-138° C
Boiling Point :
~654.7° C at 760 mmHg (Predicted)
Density :
~1.4 g/cm3 (Predicted)
Refractive Index :
n20D 1.66 (Predicted)
Optical Activity :
α20/D +71°, c = 1 in methanol
IC50 :
TXA2R: IC50 = 8.4 nM (human); DP2: IC50 = 21 nM (human); DP: IC50 = >10 µM (human); CYP3A4: IC50 = 15 µM (human)
Ki Data :
TXA2R: Ki= 0.58 nM (human); DP2: Ki= 4.3 nM (human); hTP: Ki= 4.5 nM; DP: Ki= >10 µM (human)
pK Values :
pKa: 4.6 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
1
RTECS :
FE3278500
PubChem CID :
123879
Merck Index :
14: 8100
MDL Number :
MFCD00887606
SMILES :
C1CC2=C(C[C@@H]1NS(=O)(=O)C3=CC=C(C=C3)F)C4=CC=CC=C4N2CCC(=O)O

Download SDS (MSDS)

Certificate of Analysis

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