OPC-21268 hydrate

≥98% (HPLC)

N-3-4-4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinylcarbonylphenoxypropyl-acetamide hydrate, 1-{1-4(3-acetylaminopropoxy)benzoyl-4-piperidyl}-3,4-dihydro-2(1H)-quinolinone hydrate
Empirical Formula (Hill Notation):
C26H31N3O4 · xH2O
Molecular Weight:
449.54 (anhydrous basis)
MDL number:
PubChem Substance ID:
Pricing and availability is not currently available.


≥98% (HPLC)




white to off-white


DMSO: ≥20 mg/mL


Merck & Co., Inc., Kenilworth, NJ, U.S.

storage temp.


SMILES string




InChI key



5, 25 mg in glass bottle

Biochem/physiol Actions

OPC-21268 is one of 2 non-peptide V1a selective antagonists, along with SR-49059. Arginine vasopressin (AVP) is a hormone that plays an important part in circulatory and water homoeostasis and is important in renal hemodynamic alterations, water retention, and cardiac remodeling in congestive heart failure (CHF). There are three AVP receptor subtypes-V1a, V1b, and V2 - all belong to the large rhodopsin-like G-protein-coupled receptor family. V(1a) antagonists improve water balance and cardiac hypertrophy in CHF and might be beneficial for the treatment of water retention and cardiac remodeling in CHF.

Features and Benefits

This compound was developed by Merck & Co., Inc., Kenilworth, NJ, U.S.. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.


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Hazard Statements

Precautionary Statements

Hazard Codes


Risk Statement


Safety Statement



UN 3077 9 / PGIII

WGK Germany


Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificate of Analysis
Certificate of Origin
Tatjana A Karavashkina et al.
General and comparative endocrinology, 170(3), 460-467 (2010-11-06)
1-Deamino-arginine vasotocin (1dAVT) induced diuresis and a considerable increase in urinary sodium excretion in female Wistar rats. Sodium fractional excretion rose up to 19.3 ± 1.1%. An increase in urine flow rate after 1dAVT (0.5 nmol/kg body-weight [bw]) injection was...
Kazuo Kato et al.
Brain research, 1022(1-2), 182-194 (2004-09-09)
In this study, we examined the quantitative relationship between centrally administered hypertonic saline (HS) concentrations and the expression of Fos-like immunoreactivity (FLI) in brain regions involved in the homeostasis of body fluids. The regions examined were the organum vasculosum laminae...
Nina Japundzić-Zigon et al.
Journal of pharmacological sciences, 95(1), 47-55 (2004-05-22)
Effects of V(1) (OPC-21268) and V(2) (OPC-31260) vasopressin antagonists on blood pressure (BP) short-term variability were investigated in adult spontaneously hypertensive rats (SHR) under basal conditions and after the stimulation of vasopressin release by hemorrhage. BP was recorded intra-arterially and...
Iu V Natochin et al.
Rossiiskii fiziologicheskii zhurnal imeni I.M. Sechenova, 93(6), 625-634 (2007-09-14)
In experiments on non-anesthetized female Wistar rats, it has been shown that injection of 1-deamino-arginine-vasotocin (1dAVT) increases sodium excretion and solute-free water reabsorption. Antagonists of V1-receptors (OPC-31260, Otsuka Pharmaceutical Co., Ltd., Japan) eliminates the effect water reabsorption whereas antagonist of...
Toshiki Yamada et al.
General and comparative endocrinology, 157(1), 63-69 (2008-05-02)
Physiological function of arginine vasotocin (AVT) and effect of receptor antagonists of vasopressin were electrophysiologically investigated on transepithelial transport of ions in the abdominal skin of Hyla japonica and Rana nigromaculata by means of the Ussing chamber system. Administrations of...

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