| Identification | Back Directory | [Name]
OPC 21268 | [CAS]
131631-89-5 | [Synonyms]
CS-2724
Fuscoside
OPC 21268
OPC-21268 hydrate
OPC 21268;OPC-21268;OPC21268
1-[1-[4-(3-Acetylaminopropoxy)benzoyl]-4-piperidyl]-3,4-dihydroquinolin-2(1H)-one
1-{1-[4(3-acetylaminopropoxy)benzoyl]-4-piperidyl}-3,4-dihydro-2(1H)-quinolinone hydrate
N-[3-[4-[4-(2-oxo-3,4-dihydroquinolin-1-yl)piperidine-1-carbonyl]phenoxy]propyl]acetamide
N-[3-[4-[[4-(3,4-Dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]acetamide
Acetamide, N-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-
N-[3-[4-[[4-(3,4-dihydro-2-oxo-1(2H)-quinolinyl)-1-piperidinyl]carbonyl]phenoxy]propyl]-acetamide hydrate | [Molecular Formula]
C26H31N3O4 | [MDL Number]
MFCD18632552 | [MOL File]
131631-89-5.mol | [Molecular Weight]
449.54 |
| Chemical Properties | Back Directory | [Boiling point ]
772.5±60.0 °C(Predicted) | [density ]
1?+-.0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: ≥20mg/mL | [form ]
powder | [pka]
16.17±0.46(Predicted) | [color ]
white to off-white |
| Hazard Information | Back Directory | [Description]
OPC 21268 is a nonpeptide antagonist of vasopressin V1 receptors (IC50 = 0.4 μM in rat liver membranes). It is selective for V1 over V2 receptors (IC50 = >100 μM in kidney membranes). It is also selective for rat over human V1 receptors (Kis = 25 and 8,800 nM, respectively), which can be partially attributed to the alanine residue at position 337 of the rat sequence, instead of a glycine residue in the human sequence, with differences at positions 224, 310, and 324 also contributing. OPC 21268 (0.03-1 mg/kg, i.v.) inhibits pressor responses induced by arginine vasopressin (argipressin; ) in pithed rats and arginine vasopressin-induced vasoconstriction in conscious rats (ID50 = 2 mg/kg). It induces hypotension in aged spontaneously hypertensive rats (SHRs) and stroke-prone SHRs when administered at a dose of 3 mg/kg. | [Uses]
OPC 21268 is a nonpeptide AVP (Vasopressin) Receptor V antagonist. | [storage]
Store at +4°C | [References]
[1] M THIBONNIER. A molecular model of agonist and nonpeptide antagonist binding to the human V(1) vascular vasopressin receptor.[J]. Journal of Pharmacology and Experimental Therapeutics, 2000, 294 1: 195-203.
[2] YOSHITAKA YAMAMURA. OPC-21268, an Orally Effective, Nonpeptide Vasopressin V1 Receptor Antagonist[J]. Science, 1991, 252 5005. DOI: 10.1126/science.1850553
[3] Y YAMADA. OPC-21268, a vasopressin V1 antagonist, produces hypotension in spontaneously hypertensive rats.[J]. Hypertension, 1994, 23 2: 200-204. DOI: 10.1161/01.hyp.23.2.200 |
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| Company Name: |
ChemCell Biomedicine Co.,Ltd.
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| Tel: |
020-13556033878 2965585218 13556033878 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList15061/0_EN.htm |
| Company Name: |
Twochem Co.Ltd
|
| Tel: |
021-021-58111628 15800915896 |
| Website: |
www.twochem.com |
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