MozavaptanCAS# 137975-06-5 |
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Quality Control & MSDS
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| Cas No. | 137975-06-5 | SDF | Download SDF |
| PubChem ID | 119369 | Appearance | Powder |
| Formula | C27H29N3O2 | M.Wt | 427.54 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | OPC-31260; OPC31260l | ||
| Solubility | DMSO : 6.2 mg/mL (14.50 mM; Need warming) H2O : < 0.1 mg/mL (insoluble) | ||
| Chemical Name | N-[4-[5-(dimethylamino)-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide | ||
| SMILES | CC1=CC=CC=C1C(=O)NC2=CC=C(C=C2)C(=O)N3CCCC(C4=CC=CC=C43)N(C)C | ||
| Standard InChIKey | WRNXUQJJCIZICJ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C27H29N3O2/c1-19-9-4-5-10-22(19)26(31)28-21-16-14-20(15-17-21)27(32)30-18-8-13-24(29(2)3)23-11-6-7-12-25(23)30/h4-7,9-12,14-17,24H,8,13,18H2,1-3H3,(H,28,31) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Mozavaptan (OPC31260) is a orally effective, nonpeptide vasopressin V2 receptor antagonist with an IC50 of 14 nM.In Vitro:Mozavaptan causes a competitive displacement of [3H]-arginine vasopressin (AVP) binding to both V1 and V2 receptors with IC50 values of 1.2 μM and 14 nM, respectively. The Kd of [3H]-AVP is reduced significantly in both rat liver and kidney in the presence of mozavaptan (Kd=1.1 nM in liver, Kd=1.38 nM in kidney)[1].In Vivo:Mozavaptan at doses of 10 to 100 μg/kg, i.v., inhibits the antidiuretic action of exogenously administered arginine vasopressin in water-loaded, alcohol-anaesthetized rats in a dose-dependent manner. Mozavaptan does not exert an antidiuretic activity suggesting that it is not a partial V2 receptor agonist. Mozavaptan dose-dependently increases urine flow and decreases urine osmolality after oral administration at doses of 1 to 30 mg/kg in normal conscious rats[1]. References: | |||||
Mozavaptan Dilution Calculator
Mozavaptan Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.339 mL | 11.6948 mL | 23.3896 mL | 46.7792 mL | 58.4741 mL |
| 5 mM | 0.4678 mL | 2.339 mL | 4.6779 mL | 9.3558 mL | 11.6948 mL |
| 10 mM | 0.2339 mL | 1.1695 mL | 2.339 mL | 4.6779 mL | 5.8474 mL |
| 50 mM | 0.0468 mL | 0.2339 mL | 0.4678 mL | 0.9356 mL | 1.1695 mL |
| 100 mM | 0.0234 mL | 0.1169 mL | 0.2339 mL | 0.4678 mL | 0.5847 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Mozavaptan is a novel competitive vasopressin receptor antagonist for both V1 and V2 receptors with IC50 of 1.2 μM and 14 nM, respectively.
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Small cell gall bladder carcinoma complicated by syndrome of inappropriate secretion of antidiuretic hormone (SIADH) treated with mozavaptan.[Pubmed:23761568]
BMJ Case Rep. 2013 Jun 11;2013. pii: bcr-2013-010039.
Small cell gall bladder carcinoma (Scc-GB) is a very rare entity. Although some cases present with endocrine manifestations, paraneoplastic hyponatraemia has been reported in only one previous case. Recently, the antidiuretic hormone (ADH) receptor antagonist Mozavaptan has become available. Herein we report a case with Scc-GB complicated with syndrome of inappropriate secretion of antidiuretic hormone (SIADH) treated with Mozavaptan. A 47-year-old woman was referred to our hospital for hyponatraemia. Physical examination revealed elevated serum ADH, a gall bladder mass. She was clinically diagnosed with Scc-GB with SIADH as a paraneoplastic syndrome. Mozavaptan was used for SIADH. Serum sodium was quickly normalised after Mozavaptan treatment. Two months later, metastasis to the subcutis of the abdominal wall was observed. The metastatic nodule was resected, and small cell carcinoma (Scc) was identified pathologically. Mozavaptan was effective for improvement of hyponatraemia in this patient with Scc-GB complicated with SIADH.
Clinical implication of the antidiuretic hormone (ADH) receptor antagonist mozavaptan hydrochloride in patients with ectopic ADH syndrome.[Pubmed:21087977]
Jpn J Clin Oncol. 2011 Jan;41(1):148-52.
Ectopic antidiuretic hormone syndrome is a medical emergency characterized by dilutional hyponatremia. Clinical effectiveness of the vasopressin V2 receptor antagonist Mozavaptan was evaluated in 16 patients. In short-term (7-day) treatment with the drug, serum sodium concentration (mean +/- standard deviation) significantly (P = 0.002) increased from 122.8 +/- 6.7 to 133.3 +/- 8.3 mEq/l, and symptoms due to hyponatremia were improved. On the basis of these results, Mozavaptan (Physuline((R))) was approved as an orphan drug for the treatment of the syndrome in 2006 in Japan. During the 43 months following its launch, 100 patients have been treated with the drug; overall clinical effects of the drug were found similar to those of this clinical trial. Clinically, Mozavaptan may allow hyponatremic patients to be treated by aggressive cancer chemotherapy with platinum-containing drugs. Moreover, the drug may free patients from strict fluid-intake restrictions and thereby improve their quality of life.
