OPC 21268
- Product Name
- OPC 21268
- CAS No.
- 131631-89-5
- Chemical Name
- OPC 21268
- Synonyms
- CS-2724;Fuscoside;OPC 21268;OPC-21268 hydrate;Fuscoside, 10 mM in DMSO;OPC 21268;OPC-21268;OPC21268;Inhibitor,Vasopressin Receptor,OPC21268,Fuscoside,OPC-21268,inhibit;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
- CBNumber
- CB61356814
- Molecular Formula
- C26H31N3O4
- Formula Weight
- 449.54
- MOL File
- 131631-89-5.mol
OPC 21268 Property
- Boiling point:
- 772.5±60.0 °C(Predicted)
- Density
- 1?+-.0.06 g/cm3(Predicted)
- storage temp.
- 2-8°C
- solubility
- DMSO: ≥20mg/mL
- pka
- 16.17±0.46(Predicted)
- form
- powder
- color
- white to off-white
N-Bromosuccinimide Price
- Product number
- O1016
- Product name
- OPC-21268 hydrate
- Purity
- ≥98% (HPLC)
- Packaging
- 25mg
- Price
- $756
- Updated
- 2025/07/31
- Product number
- O1016
- Product name
- OPC-21268 hydrate
- Purity
- ≥98% (HPLC)
- Packaging
- 5mg
- Price
- $267
- Updated
- 2023/01/07
- Product number
- 27226
- Product name
- OPC 21268
- Packaging
- 10mg
- Price
- $275
- Updated
- 2024/03/01
- Product number
- 27226
- Product name
- OPC 21268
- Packaging
- 25mg
- Price
- $606
- Updated
- 2024/03/01
- Product number
- 27226
- Product name
- OPC 21268
- Packaging
- 5mg
- Price
- $153
- Updated
- 2024/03/01
OPC 21268 Chemical Properties,Usage,Production
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
OPC 21268 Preparation Products And Raw materials
Raw materials
Preparation Products
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