1. GPCR/G Protein
  2. Oxytocin Receptor
  3. OT-R antagonist 1

OT-R antagonist 1 (Synonyms: Oxytocin receptor antagonist 1)

Cat. No.: HY-15015 Purity: >98.0%
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OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist.

For research use only. We do not sell to patients.

OT-R antagonist 1 Chemical Structure

OT-R antagonist 1 Chemical Structure

CAS No. : 364071-17-0

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Based on 1 publication(s) in Google Scholar

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Description

OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist. OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM). IC50 value: 8 nM Target: oxytocin receptor in vitro: OT-R antagonist 1 inhibitis IP3-Synthesis, rat OT-R (IC50=0.03 uM). [4] OT-R antagonist 1 inhibits phosphodiesterase IV with IC50 = 6.1 μM, a value about 300-fold higher than the affinity for OT-R. OT-R antagonist 1 shows a very clean selectivity profile with specific interaction with OT-R. OT-R antagonist 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. [1] in vivo: Oxytocininduced contraction of isolated rat uterine strips is blocked by OT-R antagonist 1 (pA2 = 7.82). In anesthetized nonpregnant rats, single administration of OT-R antagonist 1 by i.v. or oral routes causes dose-dependent inhibition of contractions elicited by repeated injections of oxytocin with ED50 = 3.5 mg/kg i.v. and 89 mg/kg p.o., respectively. OT-R antagonist 1 significantly inhibits spontaneous uterine contractions in pregnant rats near term when administered intravenously or orally. [1]

Molecular Weight

471.55

Formula

C₂₈H₂₉N₃O₄

CAS No.

364071-17-0

SMILES

O=C([[email protected]](C/1)N(C(C2=CC=C(C3=CC=CC=C3C)C=C2)=O)CC1=N/OC)NC[[email protected]@H](O)C4=CC=CC=C4

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Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
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OT-R antagonist 1
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HY-15015
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