L-161,982 CAS: 147776-06-5
MF: C32H29F3N4O4S2
MW: 654.72
An EP4 receptor antagonist.

L-161,982 (CAS 147776-06-5)

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Synonym: N-[[4'-[[3-Butyl-1,5-dihydro-5-oxo-1-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-4-yl]methyl][1,1'-biphenyl]-2-yl]sulfonyl]-3-methyl-2-thiophenecarboxamide
Application: An EP4 receptor antagonist
CAS Number: 147776-06-5
Purity: >99%
Molecular Weight: 654.72
Molecular Formula: C32H29F3N4O4S2
* Refer to Certificate of Analysis for lot specific data (including water content).
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L-161,982 is an EP4 (EP4 receptor) antagonist that is selective over all other members of the prostanoid receptor family (Ki values are 0.024, 0.71, 1.90, 5.10, 5.63, 6.74, 19 and 23 μM for human EP4, TP, EP3, DP, FP, IP, EP1 and EP2 receptors respectively).


References

1. Machwate, M., et al. 2001. Mol. Pharmacol. 60: 36-41. PMID: 11408598
2. Oliva, P., et al. 2006. Eur. J. Pharmacol. 530: 40-47. PMID: 16360148
3. Balzary, R.W., et al. 2006. J. Pharmacol. Exp. Ther. 317: 806-812. PMID: 16464966

Physical State :
Solid
Solubility :
Soluble in DMSO (100 mM), and DMF (~10 mg/ml).
Storage :
Store at 4° C
Density :
1.37 g/cm3 (Predicted)
Refractive Index :
n20D 1.63 (Predicted)
IC50 :
AT1: IC50 = 0.81 nM (human); Angiotensin II type 2 receptor: IC50 = 80 nM (rat)
Ki Data :
EP4: Ki= 3.16 nM (human); TXA2R: Ki= 0.71 µM (human); EP3: Ki= 1.90 µM (human); DP: Ki= 5.10 µM (human); PGF2Rα: Ki= 5.63 µM (human)
pK Values :
pKa: 4.57 (Predicted), pKb: 2.1 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
RTECS :
DV8455000
PubChem CID :
9961192
MDL Number :
MFCD09959710
SMILES :
CCCCC1=NN(C(=O)N1CC2=CC=C(C=C2)C3=CC=CC=C3S(=O)(=O)NC(=O)C4=C(C=CS4)C)C5=CC=CC=C5C(F)(F)F

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Certificate of Analysis

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L-161,982  Product Citations

See how others have used L-161,982. Click on the entry to view the PubMed entry .

Citations 1 to 1 of 1 total

PMID: # 31518663  Int. J. Biochem. Cell Biol. 116: 105610.

Citations 1 to 1 of 1 total
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