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O1016

Sigma-Aldrich

OPC-21268 hydrate

≥98% (HPLC)

Synonym(e):

1-{1-[4(3-acetylaminopropoxy)benzoyl]-4-piperidyl}-3,4-dihydro-2(1H)-quinolinone hydrate, N-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide hydrate

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About This Item

Empirische Formel (Hill-System):
C26H31N3O4 · xH2O
CAS-Nummer:
131631-89-5
Molekulargewicht:
449.54 (anhydrous basis)
MDL-Nummer:
MFCD18632552
UNSPSC-Code:
51111800
PubChem Substanz-ID:
329818893
NACRES:
NA.77

Qualitätsniveau

100

Assay

≥98% (HPLC)

Form

powder

Farbe

white to off-white

Löslichkeit

DMSO: ≥20 mg/mL

Ersteller

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

Lagertemp.

2-8°C

SMILES String

O.CC(=O)NCCCOc1ccc(cc1)C(=O)N2CCC(CC2)N3C(=O)CCc4ccccc34

InChI

1S/C26H31N3O4.H2O/c1-19(30)27-15-4-18-33-23-10-7-21(8-11-23)26(32)28-16-13-22(14-17-28)29-24-6-3-2-5-20(24)9-12-25(29)31;/h2-3,5-8,10-11,22H,4,9,12-18H2,1H3,(H,27,30);1H2

InChIKey

QTCWOUIERWBMQV-UHFFFAOYSA-N

Biochem./physiol. Wirkung

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.

Leistungsmerkmale und Vorteile

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.

Piktogramme

Exclamation markEnvironment
GHS07,GHS09

Signalwort

Warning

H-Sätze

H302,H400

Gefahreneinstufungen

Acute Tox. 4 Oral - Aquatic Acute 1

Lagerklassenschlüssel

11 - Combustible Solids

WGK

WGK 3

Flammpunkt (°F)

Not applicable

Flammpunkt (°C)

Not applicable

Analysenzertifikate (COA)

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Die Dokumentenbibliothek aufrufen

[Renal action of vasopressin].
Masami Sasaki et al.
Nihon rinsho. Japanese journal of clinical medicine, 64 Suppl 2, 257-264 (2006-03-10)
C Serradeil-Le Gal et al.
Progress in brain research, 139, 197-210 (2002-11-20)
The involvement of vasopressin (AVP) in several pathological states has been reported recently and the selective blockade of the different AVP receptors could offer new clinical perspectives. During the past few years, various selective, orally active AVP V1a (OPC-21268, SR49059
A E Bogolepova
Zhurnal evoliutsionnoi biokhimii i fiziologii, 47(1), 49-53 (2011-04-08)
Active transport of sodium ions across the isolated abdominal skin of the frog Rana temporaria after application of arginine-vasotocin (AVT) and 1-deamino-arginine-vasotocin (1dAVT) was studied by measurement of the short-circuit current (SCC). The maximal increase in the SCC values (26
A B Roald et al.
Acta physiologica Scandinavica, 182(2), 197-204 (2004-09-29)
Arginine vasopressin (AVP) might influence urinary concentration ability by altering the intrarenal distribution of glomerular filtration rate (GFR). To study this possibility we have measured the intracortical distribution of GFR following acute AVP-V1 receptor stimulation in anaesthetized female Sprague-Dawley (SPD)
James Walter Ferguson et al.
Clinical science (London, England : 1979), 105(1), 1-8 (2003-03-18)
Vasopressin, or antidiuretic hormone, is a peptide hormone that is released from the posterior pituitary gland in response to changes in blood pressure and plasma osmolality. The main pathophysiological states associated with high plasma vasopressin concentrations are cirrhosis, cardiac failure
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