Conivaptan HCl (Synonyms: YM-087) |
Catalog No.GC12627
One-Click Copy Product Info
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Conivaptan(염산염)은 바소프레신 수용체의 비펩타이드성 길항제이며, 랫트 간 V1A 수용체 및 랫트 신장 V2 수용체에 대해 Ki 값이 각각 0.48 및 3.04nM입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 168626-94-6
Sample solution is provided at 25 µL, 10mM.
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Conivaptan HCl is an orally active vasopressin receptor (V1a/V2; Ki=0.48nM/3.04nM) antagonist. Conivaptan HCl modulates vascular resistance and enhances diuresis to increase serum sodium concentration. Conivaptan HCl can be used in research related to hyponatremia and heart failure[1-4].
In vitro, in the presence of anti-CD3 (2μg/ml), anti-CD28 (2μg/ml), interleukin-2 (10ng/ml), and transforming growth factor-β (10ng/ml), Conivaptan HCl (1μM) was used to treat mouse CD4⁺ T cells for 4 days. Conivaptan HCl significantly inhibited the differentiation of CD4⁺ T cells into helper T cells[5]. Conivaptan HCl (0.78-100μM) was used to pretreat HCT-8 cells for 30 minutes, followed by infection with HCoV-OC43 (MOI=0.05) for 72 hours. Conivaptan HCl inhibited the replication of HCoV-OC43 and reduced virus-induced cytopathic effects[6].
In vivo, Conivaptan HCl (0.5mg/kg/day) was intraperitoneally injected into TNBS-induced colitis Balb/c mice for 6 days. Conivaptan HCl significantly attenuated TNBS-induced colitis[7]. Conivaptan HCl (0.1 or 0.3mg/kg; single injection) was intravenously injected into Sprague-Dawley rats with myocardial infarction-induced congestive heart failure. Conivaptan HCl significantly improved cardiac hemodynamics and alleviated pulmonary congestion[8].
References:
[1] Fernández-Varo G, Ros J, Cejudo-Martín P, et al. Effect of the V1a/V2-AVP receptor antagonist, Conivaptan, on renal water metabolism and systemic hemodynamics in rats with cirrhosis and ascites. J Hepatol. 2003 Jun;38(6):755-61.
[2] Yatsu T, Tomura Y, Tahara A, et al. Cardiovascular and renal effects of conivaptan hydrochloride (YM087), a vasopressin V1A and V2 receptor antagonist, in dogs with pacing-induced congestive heart failure. Eur J Pharmacol. 1999 Jul 9;376(3):239-46.
[3] Li R, Sun H, Zheng H, et al. Intradermal Injection of Oxytocin Aggravates Chloroquine-Induced Itch Responses via Activating the Vasopressin-1a Receptor/Nitric Oxide Pathway in Mice. Front Pharmacol. 2019 Nov 15;10:1380.
[4] He Y, Bae JSH, Nowak E, et al. Rational discovery of therapeutic PAK1 allosteric activators. Cell. 2026 Mar 31:S0092-8674(26)00275-8.
[5] Dou D, Ji Y, Zheng J, et al. A New Role for Conivaptan in Ulcerative Colitis in Mice: Inhibiting Differentiation of CD4+T Cells into Th1 Cells. Dig Dis Sci. 2022 Aug;67(8):3683-3692.
[6] Yang CW, Peng TT, Hsu HY, et al. Repurposing old drugs as antiviral agents for coronaviruses. Biomed J. 2020 Aug;43(4):368-374.
[7] Dou D, Chen L, Di H, et al. Vasopressin augments TNBS-induced colitis through enteric neuronal V1a receptor-mediated COX-2-dependent prostaglandin release from mast cells in mice. Neurogastroenterol Motil. 2019 Feb;31(2):e13493.
[8] Wada K, Fujimori A, Matsukawa U, et al. Intravenous administration of conivaptan hydrochloride improves cardiac hemodynamics in rats with myocardial infarction-induced congestive heart failure. Eur J Pharmacol. 2005 Jan 10;507(1-3):145-51.
| Cell experiment [1]: | |
Cell lines | HCT-8 colon epithelial cells (human colon epithelial cell line) |
Preparation Method | HCT-8 cells were grown as monolayers in a growth medium consisting of Dulbecco's modified Eagle's medium (DMEM) and 10% fetal bovine serum (FBS). HCT-8 cells were pre-treated with solutions of the Conivaptan HCl for 30min, and then infected with human coronavirus OC43 (HCoV-OC43) at a multiplicity of infection (MOI) of 0.05, and incubated at 37°C for 72h. |
Reaction Conditions | 0.78-100μM, pre-treatment for 30min |
Applications | Conivaptan HCL exhibited inhibitory activity against HCoV-OC43 with an EC50 of 12.2 ± 4.20μM. |
| Animal experiment [2]: | |
Animal models | Balb/c mice |
Preparation Method | Colitis was induced in Balb/c mice by intrarectal administration of TNBS. After colitis induction, mice were treated with Conivaptan HCl intraperitoneally for 6 days. |
Dosage form | 0.5mg/kg/day; i.p.; for 6 days |
Applications | Conivaptan HCl significantly attenuated the aggravation of TNBS-induced colitis by AVP, resulting in lower disease activity index (DAI) and histological scores. |
References: | |
| Cas No. | 168626-94-6 | SDF | |
| Synonyms | YM-087 | ||
| Chemical Name | N-[4-(2-methyl-4,5-dihydro-3H-imidazo[4,5-d][1]benzazepine-6-carbonyl)phenyl]-2-phenylbenzamide;hydrochloride | ||
| Canonical 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 | ||
| Formula | C32H26N4O2.HCl | M.Wt | 535.04 |
| Solubility | ≥ 14.8mg/mL in DMSO | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.869 mL | 9.3451 mL | 18.6902 mL |
| 5 mM | 373.8 μL | 1.869 mL | 3.738 mL |
| 10 mM | 186.9 μL | 934.5 μL | 1.869 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)