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| Targets |
vasopressin V1 ( IC50 = 0.4 μM ); vasopressin V1 ( Ki = 0.14 μM )
Vasopressin V1 receptor. OPC-21268 is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM. Vasopressin V1 receptors are G protein-coupled receptors that mediate the effects of arginine vasopressin (AVP) on vascular smooth muscle contraction, vasoconstriction, and cardiac function. By antagonizing the V1 receptor, OPC-21268 blocks AVP-mediated vasoconstriction, reducing vascular resistance and potentially improving cardiac function. The compound is also described as a selective alpha-2 adrenergic receptor agonist. OPC-21268 has shown promise in preclinical studies for improving heart function and reducing vascular resistance. Its effects on the central nervous system may also offer neuroprotective benefits. OPC-21268 has also been studied for its protective effects against ethanol-induced gastric damage. |
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| ln Vitro |
Fuscoside (OPC-21268) has an IC50 of 0.4 μM for VI receptors and 100 μM for V2 receptors, which means that it displaces 50% of specific AVP binding. Fuscoside (OPC-21268) has an inhibition constant (Ki) of 0.14 μM for V1 receptors[1].
OPC-21268 is a nonpeptide vasopressin V1 receptor antagonist with an IC50 of 0.4 μM. The compound demonstrates antagonist activity at the V1 receptor, blocking AVP-mediated vasoconstriction. OPC-21268 has been characterized in receptor binding assays and functional assays measuring V1 receptor-mediated signaling. The compound's selectivity for V1 receptors over other vasopressin receptor subtypes (e.g., V2) contributes to its specificity. OPC-21268 has shown promise in preclinical studies for improving heart function and reducing vascular resistance. Its effects on the central nervous system may also offer neuroprotective benefits. The compound has also been studied for its protective effects against ethanol-induced gastric damage. |
| ln Vivo |
Fuscoside (OPC-21268) specifically and competitively inhibits pressor responses to AVP in vivo. In a dose- and time-dependent manner, oral administration of Fuscoside (OPC-21268) (10 mg/kg) inhibits the vasoconstriction induced by exogenous AVP, with an effect that lasts for more than 8 hours at 30 mg/kg[1]. Fuscoside (OPC-21268) works well to treat cold-induced vasogenic brain edema because it primarily provides protection where the blood-brain barrier is most likely to be broken down. Both hemispheres' brain water content is markedly decreased by fuscoside (OPC-21268) treatment at doses of 200 and 300 mg/kg. At dosages of 200 and 300 mg/kg, the injured hemispheres' swelling is also markedly decreased[2].
OPC-21268 is an orally effective vasopressin V1 receptor antagonist that has been studied in vivo for its effects on cardiovascular function and gastric protection. The compound has shown promise in preclinical studies for improving heart function and reducing vascular resistance. Its effects on the central nervous system may also offer neuroprotective benefits. OPC-21268 has also been studied for its protective effect against ethanol-induced damage of the rat gastric wall. The compound's oral bioavailability makes it suitable for in vivo studies. Detailed in vivo pharmacokinetic and pharmacodynamic data are available from preclinical studies. OPC-21268 is for research use only and is not for human therapeutic use. |
| Enzyme Assay |
Vasopressin V1 receptor binding assays are performed using membranes prepared from cells expressing recombinant V1 receptors or from tissue sources (e.g., liver, vascular smooth muscle). Radioligand binding studies use [³H]-AVP or [³H]-[Phe²]AVP as labeled ligands. Membrane preparations are incubated with varying concentrations of OPC-21268 and a fixed concentration of radioligand in binding buffer (50 mM Tris-HCl pH 7.4, 5 mM MgCl₂, 1 mM EDTA, 0.1% BSA) for 60-120 minutes at room temperature. Non-specific binding is determined using excess unlabeled AVP or a V1 receptor antagonist (e.g., SR-49059). Bound radioactivity is measured by scintillation counting after filtration through GF/B filters. IC50 and Ki values are calculated by non-linear regression. The IC50 for OPC-21268 is 0.4 μM.
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| Cell Assay |
Cellular V1 receptor antagonism is evaluated in cell lines expressing recombinant V1 receptors (e.g., HEK-293 cells). Cells are cultured in appropriate media at 37°C with 5% CO₂ and treated with OPC-21268 at various concentrations. Functional assays measure receptor-mediated calcium mobilization (Gq-coupled receptor) in response to AVP stimulation. The compound's antagonist activity is assessed by its ability to inhibit AVP-induced calcium responses. Cell viability is assessed using MTT or LDH assays. Each experiment includes known V1 receptor antagonists (e.g., SR-49059) as positive controls and vehicle controls.
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| Animal Protocol |
Rats: Fuscoside (OPC-21268) is injected subcutaneously (0.1, 0.3, or 1 mg/kg) into male Sprague-Dawley rats weighing 300–400 g. Two minutes prior to the injection of AVP (30 mU/kg i.v.), angiotensin II (0.3 μg/kg i.v.), and noradrenaline (3 μg/kg i.v.), fuscoside (OPC-21268) is administered[1].
In vivo efficacy of OPC-21268 is evaluated in animal models of cardiovascular disease and gastric injury. The compound is administered orally at doses determined by preclinical studies. In models of heart failure, the compound's effects on cardiac function, hemodynamics, and vascular resistance are assessed. In models of gastric injury (e.g., ethanol-induced gastric damage), the compound's protective effects are assessed by measuring gastric mucosal damage and inflammation. Sample sizes typically range from 6-10 animals per group. |
| ADME/Pharmacokinetics |
Molecular Weight: 449.55. Formula: C26H31N3O4. CAS No.: 131631-89-5. IUPAC Name: N-(3-(4-(4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidine-1-carbonyl)phenoxy)propyl)acetamide. Synonyms: OPC-21268; OPC21268; Fuscoside. Appearance: Solid. Purity: Typically ≥98%. Solubility: Soluble in DMSO and alcohol. Storage: 0°C (short term), -20°C (long term), desiccated. OPC-21268 is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM.
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| Toxicity/Toxicokinetics |
No comprehensive toxicology data are publicly available for OPC-21268. The compound is intended for research use only and has not undergone full preclinical toxicology evaluation required for clinical development. As a vasopressin V1 receptor antagonist, potential toxicities may include hypotension, flushing, and other cardiovascular effects. Standard toxicity studies would include acute toxicity assessment in rodents, repeated dose toxicity studies (14-day and 28-day), and genotoxicity screening (Ames test, micronucleus assay). The compound is for research use only and not for human therapeutic use.
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| References | |
| Additional Infomation |
OPC-21268 is also known as OPC21268 and Fuscoside. Its IUPAC name is N-(3-(4-(4-(2-oxo-3,4-dihydroquinolin-1(2H)-yl)piperidine-1-carbonyl)phenoxy)propyl)acetamide. OPC-21268 is an orally effective, nonpeptide, vasopressin V1 receptor antagonist with an IC50 of 0.4 μM. It is also described as a selective alpha-2 adrenergic receptor agonist. The compound has shown promise in preclinical studies for improving heart function and reducing vascular resistance. OPC-21268 has also been studied for its protective effect against ethanol-induced gastric damage. No clinical trials have been reported for this compound. OPC-21268 is for research use only.
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| Molecular Formula |
C26H31N3O4
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|---|---|
| Molecular Weight |
449.55
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| Exact Mass |
449.231
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| Elemental Analysis |
C, 69.47; H, 6.95; N, 9.35; O, 14.24
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| CAS # |
131631-89-5
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| Related CAS # |
131631-89-5
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| PubChem CID |
114904
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
772.5±60.0 °C at 760 mmHg
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| Flash Point |
421.0±32.9 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.596
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| LogP |
2.22
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
33
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| Complexity |
683
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CC1)N(C2CCN(C(C3=CC=C(OCCCNC(C)=O)C=C3)=O)CC2)C4=C1C=CC=C4
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| InChi Key |
KSNUCNRMDYJBKT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H31N3O4/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)
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| Chemical Name |
N-[3-[4-[4-(2-oxo-3,4-dihydroquinolin-1-yl)piperidine-1-carbonyl]phenoxy]propyl]acetamide
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| Synonyms |
OPC-21268; Fuscoside; OPC21268; OPC 21268
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~111.2 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.56 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2244 mL | 11.1222 mL | 22.2445 mL | |
| 5 mM | 0.4449 mL | 2.2244 mL | 4.4489 mL | |
| 10 mM | 0.2224 mL | 1.1122 mL | 2.2244 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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