2. Signaling Pathways
  3. GPCR/G Protein
  4. Vasopressin Receptor
  5. V1a Receptor  Isoform
  6. V1a Receptor  Antagonist

V1a Receptor  Antagonist

V1a Receptor  Antagonists (12):

Cat. No. Product Name Effect Purity
  • HY-18347A
    Conivaptan hydrochloride
    		Antagonist 99.88%
    Conivaptan (hydrochloride) is a non-peptide antagonist of vasopressin receptor, with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively.
  • HY-18345
    SR 49059
    		Antagonist 99.92%
    SR 49059 (SR-49059) is a potent, orally active, selective vasopressin V1a antagonist with a Ki vaule of 1.4 nM.
  • HY-15010
    L-371,257
    		Antagonist 99.90%
    L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM).
  • HY-105685
    SRX246
    		Antagonist 98.77%
    SRX246 is a potent, CNS-penetrant, highly selective, orally bioavailable vasopressin 1a (V1a) receptor antagonist (Ki=0.3 nM for human V1a). SRX246 has no interaction at V1b and V2 receptors. SRX246 also displays negligible binding at 64 others receptors classes, including 35 G-proteincoupled receptors. SRX246 can be used for treatment of stress-related disorders.
  • HY-109024
    Balovaptan
    		Antagonist 99.89%
    Balovaptan (RG7314) is an orally available, selective brain-penetrant vasopressin 1a (hV1a) receptor antagonist, with Kis of 1 and 39 nM for human (hV1a) and mouse (mV1a) receptors, and is used for the research of autism.
  • HY-168742
    V1a/V2 antagonist 1
    		Antagonist
    V1a/V2 antagonist 1 (Compound 18j) is an orally active dual V1a and V2 receptor antagonist with high binding affinity for both receptors (Ki: 0.13 nM for hV1a, 0.53 nM for hV2 and 0.5 nM for mV1a; IC50: 2.2 nM for hV1a). V1a/V2 antagonist 1 inhibits Oxytocin (HY-17571)-induced scratching behavior in mice.
  • HY-118918
    YM218 free base
    		Antagonist
    YM218 free base is an orally active non-peptide vasopressin (AVP) receptor antagonist. YM218 free base has a high affinity for rat liver V1A receptors with a Ki value of 0.50 nM; it has a lower affinity for rat pituitary V1B, kidney V2, and uterine oxytocin receptors with Ki values of 1510 nM, 72.2 nM, and 150 nM, respectively. YM218 free base can be used in the study of diabetes and kidney disease.
  • HY-12981
    RG7713
    		Antagonist 99.92%
    RG7713 (RO5028442) is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Kis of 1 nM (hV1a) and 39 nM (mV1a).
  • HY-P4683
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin
    		Antagonist
    (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin is a potent vasopressin V1 receptor (VP V1R) antagonist. (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin significantly decreases the mean arterial pressure (MAP) in rats.
  • HY-108678
    TC OT 39
    		Antagonist
    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.
  • HY-P5010
    (D-Arg8)-Inotocin
    		Antagonist
    (D-Arg8)-Inotocin is a potent, selective and competitive antagonist of vasopressin receptor (V1aR), with a Ki of 1.3 nM. (D-Arg8)-Inotocin shows more than 3000-fold selectivity for the human V1aR over the other three subtypes, OTR, V1bR and V2R.
  • HY-18347
    Conivaptan
    		Antagonist
    Conivaptan (YM 087 free base) is antagonist for vasopressin V1A receptor and vasopressin V2 receptor. Conivaptan ameliorates congestive heart failure, improves cardiac systolic function.