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Merck
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Key Documents

O1016

Sigma-Aldrich

OPC-21268 hydrate

≥98% (HPLC)

同義詞:

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

經驗公式(希爾表示法):
C26H31N3O4 · xH2O
CAS號碼:
分子量::
449.54 (anhydrous basis)
MDL號碼:
分類程式碼代碼:
51111800
PubChem物質ID:
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

white to off-white

溶解度

DMSO: ≥20 mg/mL

起源

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

儲存溫度

2-8°C

SMILES 字串

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

InChI 密鑰

QTCWOUIERWBMQV-UHFFFAOYSA-N

生化/生理作用

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.

特點和優勢

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.

象形圖

Exclamation markEnvironment

訊號詞

Warning

危險聲明

危險分類

Acute Tox. 4 Oral - Aquatic Acute 1

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


分析證明 (COA)

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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
Makoto Takada et al.
Journal of comparative physiology. B, Biochemical, systemic, and environmental physiology, 180(3), 393-402 (2009-12-02)
Amphibian skin has osmoregulatory functions, with Na(+) crossing from outside to inside. Na(+) transport can be measured as the short-circuit current (SCC). We investigated the short-term and long-term effects of arginine vasotocin (AVT) and mesotocin (MT) (which modulate Na(+) transport)
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
Sho Maejima et al.
General and comparative endocrinology, 157(2), 196-202 (2008-06-17)
Anuran amphibians do not drink orally but absorb water osmotically through the highly permeable ventral skin. In this cutaneous water absorption, roles of the putative cerebral osmoreceptors and functions of arginine vasotocin (AVT) were examined in the central nervous system

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