2. Signaling Pathways
  3. GPCR/G Protein
  4. Oxytocin Receptor

Oxytocin Receptor

OXTR

Oxytocin Receptor

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The oxytocin receptor belongs to the G-protein-coupled seven-transmembrane receptor superfamily. Its main physiological role is regulating the contraction of uterine smooth muscle at parturition and the ejection of milk from the lactating breast. The oxytocin receptors are activated in response to binding oxytocin and a similar nonapeptide, vasopressin. Oxytocin receptor triggers Gi or Gq protein-mediated signaling cascades leading to the regulation of a variety of neuroendocrine and cognitive functions.

Oxytocin is a nonapeptide of the neurohypophyseal protein family that binds specifically to the oxytocin receptor to produce a multitude of central and peripheral physiological responses. In vivo, oxytocin acts as a paracrine and/or autocrine mediator of multiple biological effects. These effects are exerted primarily through interactions with G-protein-coupled oxytocin/vasopressin receptors, which, via Gq and Gi, stimulate phospholipase C-mediated hydrolysis of phosphoinositides.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-128351
    SHR1653
    		Antagonist 99.69%
    SHR1653 is a highly potent, selective and brain penetrated oxytocin receptor (OTR) antagonist, with an IC50 of 15 nM for hOTR.
    SHR1653
  • HY-15015
    OT-R antagonist 1
    		Antagonist ≥98.0%
    OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist.
    OT-R antagonist 1
  • HY-P3221
    [Leu3]-Oxytocin
    		99.93%
    [Leu3]-Oxytocin, an oxytocin analogue, is derived by structural variation in sequence position 3 replaced by leucine (Leu).
    [Leu3]-Oxytocin
  • HY-17571F
    Biotin-Oxytocin
    		99.25%
    Biotin-Oxytocin (Biotin-α-Hypophamine; Biotin-Oxytocic hormone) is a biological active peptide. (This is Oxytocin (HY-17571) N-terminally labeled with Biotin.)
    Biotin-Oxytocin
  • HY-15011
    L-372662
    		Antagonist 99.24%
    L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR.
    L-372662
  • HY-P1574
    [Arg8]-Vasotocin
    [Arg8]-Vasotocin is a vertebrate neurohypophyseal peptide of the vasopressin/oxytocin hormone family.
    [Arg8]-Vasotocin
  • HY-153963
    PF-06655075
    		Agonist 99.24%
    PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response.
    PF-06655075
  • HY-P3217A
    [Asp5]-Oxytocin acetate
    		Agonist 99.51%
    [Asp5]-Oxytocin acetate is the first 5-position neurohypophyseal hormone analogue possessing significant biological activity. [Asp5]-Oxytocin acetate causes uterine contractions in vitro, enhanced by Mg2+. [Asp5]-Oxytocin acetate has the ability of rat uteroconstrictor, avian vasodilator, and rat antidiuretic.
    [Asp5]-Oxytocin acetate
  • HY-P1574A
    [Arg8]-Vasotocin TFA
    		98.41%
    [Arg8]-Vasotocin (TFA) is a vertebrate neurohypophyseal peptide of the vasopressin/oxytocin hormone family.
    [Arg8]-Vasotocin TFA
  • HY-15015A
    OT-R antagonist 2
    		Antagonist 99.86%
    OT-R antagonist 2 is a nonpeptide low molecular weight OT-R antagonist.
    OT-R antagonist 2
  • HY-P3215A
    Oxytocin parallel dimer TFA
    		Activator 98.10%
    Oxytocin parallel dimer TFA is the disulfide-bridged homo peptide dimer. Oxytocin dimer has oxytocin and vasopressin-like activity with less toxic than oxytocin.
    Oxytocin parallel dimer TFA
  • HY-14778A
    (S)-Retosiban
    		Antagonist 99.12%
    (S)-Retosiban is the isomer of Retosiban (HY-14778), and can be used as an experimental control. Retosiban (GSK221149A) is a potent and selective oxytocin antagonist with a Ki of 0.65 nM.
    (S)-Retosiban
  • HY-P5213
    Vasopressin Dimer (parallel) (TFA)
    		Activator 99.55%
    Vasopressin Dimer (parallel) TFA is a parallel dimer of Vasopressin (HY-B1811). Vasopressin Dimer (parallel) TFA can activate four G protein-coupled receptors, V1aR, V1bR, V2R, and OTR.
    Vasopressin Dimer (parallel) (TFA)
  • HY-108678
    TC OT 39
    		Agonist
    TC OT 39 is a synthetic oxytocin analog, as well as a selective agonist of oxytocin receptor (OXTR, EC50=180 nM). TC OT 39 is also an Avprla vasopressin receptor antagonist with an Ki value of 330 nM. TC OT 39 exhibits sedative effects in mouse models.
    TC OT 39
  • HY-105018
    Epelsiban
    		Antagonist
    Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.
    Epelsiban
  • HY-P3866
    [Asu1,6]-Oxytocin
    [Asu1,6]-Oxytocin is an analog of oxytocin. [Asu1,6]-Oxytocin reverses insulin resistance and glucose intolerance prior to reduction of obesity. [Asu1,6]-Oxytocin has the potential for the research of obesity and diabetes.
    [Asu1,6]-Oxytocin
  • HY-15007
    L 366509
    		Antagonist
    L 366509 is a spiroindenylpiperidine camphorsulfonamide oxytocin (OT) antagonist. Modifications led to a new series of o-tolylpiperazine (TP) camphorsulfonamides, exhibiting high affinity for OT receptors and selectivity over arginine vasopressin receptors. Notably, compound 7 (L-368,899) showed excellent OT receptor affinity, potency in inhibiting OT-stimulated uterine contractions, good aqueous solubility, and oral bioavailability in multiple species. Compound 7 has entered clinical testing as an oral and intravenous tocolytic agent. Molecular modeling suggests the TP camphorsulfonamide structure mimics the D-AA2-Ile3 dipeptide, crucial in potent OT antagonists.
    L 366509
  • HY-153964A
    PF-06478939 TFA
    		Agonist
    PF-06478939 TFA is a non-brain-penetrating peptide that is an agonist at oxytocin (OT) receptor and vasopressin receptor with EC50 values of 0.01 nM and 0.078 nM, respectively.
    PF-06478939 TFA
  • HY-P4990A
    Pro8-Oxytocin TFA
    		Activator
    Pro8-Oxytocin TFA is a a modified oxytocin (OXT) ligand. Pro8-Oxytocin produces more potent and efficacious responses at primate OXTR and stronger behavioral effects than the consensus mammalian OXT ligand (Leu8-Oxytocin). Pro8-Oxytocin TFA produce a less efficacious response than Vasopressin (HY-B1811) (AVP) at human AVPR1a and higher efficacious response than AVP at marmoset AVPR1a.
    Pro8-Oxytocin TFA
  • HY-103649
    OT antagonist 3
    		Antagonist
    OT antagonist 3 is an oxytocin (OT) antagonist extracted from patent WO2007017752A1.
    OT antagonist 3
Cat. No. Product Name / Synonyms Application Reactivity