L-371,257A potent oxytocin receptor inhibitor

L-371,257 (CAS 162042-44-6)

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Synonym: 1-[1-[4-(1-acetylpiperidin-4-yl)oxy-2-methoxybenzoyl]piperidin-4-yl]-4H-3,1-benzoxazin-2-one
Application: A potent oxytocin receptor inhibitor
CAS Number: 162042-44-6
Molecular Weight: 507.59
Molecular Formula: C28H33N3O6
* Refer to Certificate of Analysis for lot specific data (including water content).
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L-371,257 is a potent and selective oxytocin receptor inhibitor. It displays >800-fold selectivity over human arginine vasopressin receptors V1a and V2.


References

1. Williams, P.D., et al. 1995. J. Med. Chem. 38: 4634-4636.
2. Tahara, A., et al. 1999. Eur. J. Pharmacol. 378: 137-142.
3. Tahara, A., et al. 2000. Br. J. Pharmacol. 129: 131-139.

Physical State :
Solid
Solubility :
Soluble in DMSO (10 mM).
Storage :
Store at room temperature
Refractive Index :
n20D 1.60 (Predicted)
IC50 :
Rattus norvegicus: IC50 = 25 nM (rat); Oxytocin receptor: IC50 = 640 nM (rat)
Ki Data :
Vasopressin V1a receptor: Ki= 3.7 nM (rat); Oxytocin receptor: Ki= 4.6 nM (rat); AVP Receptor V1a: Ki= 3.2 µM (human); Vasopressin V2 receptor: Ki= >30 µM (rat)
pK Values :
pKb: 0.73 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
6918320
MDL Number :
MFCD00944944
SMILES :
CC(=O)N1CCC(CC1)OC2=CC(=C(C=C2)C(=O)N3CCC(CC3)N4C5=CC=CC=C5COC4=O)OC

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Certificate of Analysis

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