OT-R antagonist 1 - CAS 364071-17-0
Catalog number:
364071-17-0
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C28H29N3O4
Molecular Weight:
471.54
COA:
Inquire
Targets:
Others
Description:
OT-R antagonist 1 is a nonpeptide OT-R antagonist, inhibitis IP3-Synthesis, rat OT-R (IC50 = 8 nM).
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Purity:
≥98%
Appearance:
Solid powder
Synonyms:
(4Z)-N-[(2S)-2-Hydroxy-2-phenylethyl]-4-(methoxyimino)-1-[(2'-methyl-4-biphenylyl)carbonyl]-L-prolinamide
Solubility:
Soluble in DMSO
Storage:
Store at -20 °C
MSDS:
Inquire
Application:
A new potent and selective nonpeptide OT-R antagonist
Quality Standard:
Enterprise Standard
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
IBXGJPAYWMFXSF-UEEONYLUSA-N
InChI:
1S/C28H29N3O4/c1-19-8-6-7-11-24(19)20-12-14-22(15-13-20)28(34)31-18-23(30-35-2)16-25(31)27(33)29-17-26(32)21-9-4-3-5-10-21/h3-15,25-26,32H,16-18H2,1-2H3,(H,29,33)/b30-23-/t25-,26+/m0/s1
Canonical SMILES:
CC1=CC=CC=C1C2=CC=C(C=C2)C(=O)N3C/C(=N\OC)/C[C@H]3C(=O)NC[C@H](C4=CC=CC=C4)O
1.Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor.
Cirillo R1, Gillio Tos E, Schwarz MK, Quattropani A, Scheer A, Missotten M, Dorbais J, Nichols A, Borrelli F, Giachetti C, Golzio L, Marinelli P, Thomas RJ, Chevillard C, Laurent F, Portet K, Barberis C, Chollet A. J Pharmacol Exp Ther. 2003 Jul;306(1):253-61. Epub 2003 Mar 26.
We have discovered a new, potent, selective, and orally active oxytocin receptor antagonist, (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino)-1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide (compound 1). We report the biochemical, pharmacological, and pharmacokinetic characterization in vitro and in vivo of this compound. Compound 1 competitively inhibits binding of [3H]oxytocin and the peptide antagonist 125I-ornithine vasotocin analog to human and rat oxytocin receptor expressed in human embryonic kidney 293-EBNA or Chinese hamster ovary cells with nanomolar potency. Selectivity against vasopressin receptor subtypes is >6-fold for V1a and >350-fold for V2 and V1b. Compound 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM). Compound 1 has no intrinsic agonist activity at the oxytocin receptor. Oxytocininduced contraction of isolated rat uterine strips is blocked by compound 1 (pA2 = 7.
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