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Purity: ≥98%
Conivaptan HCl (formerly known as YM-087; YM087; YM 087, trade name Vaprisol), the hydrochloride salt of It inhibits the rat liver V1A receptor and the rat kidney V2 receptor with Ki values of 0.48 and 3.04 nM, respectively. Conivaptan was licensed in 2004 for the treatment of hyponatremia (low blood sodium levels) brought on by syndrome of inappropriate antidiuretic hormone (SIADH), including hypervolemic and euvolemic cases.There is also some indication that the drug may be useful in heart failure cases. Conivaptan suppresses the activity of the vasopressin receptor's two (V1a and V2) subtypes.
| Targets |
Vasopressin receptor 1; Vasopressin receptor 2
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| References |
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| Molecular Formula |
C32H26N4O2.HCL
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| Molecular Weight |
535.04
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| Exact Mass |
534.18
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| Elemental Analysis |
C, 71.84; H, 5.09; Cl, 6.63; N, 10.47; O, 5.98
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| CAS # |
168626-94-6
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| Appearance |
Solid powder
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| SMILES |
CC1=NC2=C(N1)CCN(C3=CC=CC=C32)C(=O)C4=CC=C(C=C4)NC(=O)C5=CC=CC=C5C6=CC=CC=C6.Cl
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| InChi Key |
BTYHAFSDANBVMJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H26N4O2.ClH/c1-21-33-28-19-20-36(29-14-8-7-13-27(29)30(28)34-21)32(38)23-15-17-24(18-16-23)35-31(37)26-12-6-5-11-25(26)22-9-3-2-4-10-22;/h2-18H,19-20H2,1H3,(H,33,34)(H,35,37);1H
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| Chemical Name |
N-[4-(2-methyl-4,5-dihydro-3H-imidazo[4,5-d][1]benzazepine-6-carbonyl)phenyl]-2-phenylbenzamide;hydrochloride
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.67 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 (4.67 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 (4.67 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 | 1.8690 mL | 9.3451 mL | 18.6902 mL | |
| 5 mM | 0.3738 mL | 1.8690 mL | 3.7380 mL | |
| 10 mM | 0.1869 mL | 0.9345 mL | 1.8690 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00851227 | Completed | Drug: conivaptan hydrochloride | Liver Disease Hyponatremia |
Cumberland Pharmaceuticals | February 2009 | Phase 1 |
| NCT00887627 | Completed | Drug: conivaptan hydrochloride | Kidney Diseases Hyponatremia |
Cumberland Pharmaceuticals | April 2009 | Phase 1 |
| NCT01370148 | Completed | Drug: conivaptan hydrochloride | Liver Disease | Cumberland Pharmaceuticals | April 2011 | Phase 1 |
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