2. GPCR/G Protein
  3. Vasopressin Receptor
  4. Conivaptan hydrochloride

Conivaptan (hydrochloride)  (Synonyms: コニバプタン塩酸塩; YM 087)

製品番号: HY-18347A 純度: 99.95%
COA 取扱説明書 Technical Support

Conivaptan (hydrochloride) is a non-peptide antagonist of vasopressin receptor, with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively.

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Conivaptan hydrochloride

Conivaptan (hydrochloride) 構造式

CAS 番号 : 168626-94-6

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 54 在庫あり
Solution
10 mM * 1 mL in DMSO USD 54 在庫あり
Solid
5 mg $46 在庫あり
10 mg $72 在庫あり
25 mg $160 在庫あり
50 mg $288 在庫あり
100 mg $480 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 14 publication(s) in Google Scholar

Other Forms of Conivaptan hydrochloride:

Conivaptan (hydrochloride) 関連抗体

Top Publications Citing Use of Products

Vasopressin Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
V1a Receptor  V1b Receptor  V2 Receptor 

  • 生物活性

  • プロトコル

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

Conivaptan (hydrochloride) is a non-peptide antagonist of vasopressin receptor, with Ki values of 0.48 and 3.04 nM for rat liver V1A receptor and rat kidney V2 receptor respectively.

IC50 & Target

V2 Receptor 

 

体内実験

Conivaptan (0.03, 0.1 and 0.3 mg/kg, i.v.) dose-dependently increases urine volume and reduces urine osmolality in both myocardial infarction and sham-operated rats. Conivaptan (0.3 mg/kg i.v.) significantly reduces right ventricular systolic pressure, left ventricular end-diastolic pressure, lung/body weight and right atrial pressure in myocardial infarction rats. Conivaptan (0.3 mg/kg i.v.) significantly increases dP/dt(max)/left ventricular pressure in myocardial infarction rats[1]. Conivaptan produces an acute increase in urine volume (UV), a reduction in osmolality (UOsm) and, at the end of the investigation, cirrhotic rats receiving the V(1a)/V(2)-AVP receptor antagonist does not show hyponatremia or hypoosmolality. Conivaptan also normalizes U(Na)V without affecting creatinine clearance and arterial pressure[2]. Conivaptan (0.01 to 0.1 mg/kg, i.v.) exerts a dose-dependent diuretic effect in dogs without an increase in the urinary excretion of electrolytes, inhibits the pressor effect of exogenous vasopressin in a dose-dependent manner (0.003 to 0.1 mg/kg i.v.) and, at the highest dose (0.1 mg/kg i.v.), almost completely blocks vasoconstriction caused by exogenous vasopressin. Conivaptan (0.1 mg/kg, i.v.) improves cardiac function, as evidenced by significant increases in left ventricular dP/dtmax, cardiac output and stroke volume, and reduces preload and afterload, as evidenced by significant decreases in left ventricular end-diastolic pressure and total peripheral vascular resistance in dogs with congestive heart failure[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

535.04

分子式

C32H27ClN4O2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=CC=C1C2=CC=CC=C2)NC3=CC=C(C(N4CCC(N=C(C)N5)=C5C6=CC=CC=C64)=O)C=C3.Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
体外: 

DMSO : ≥ 100 mg/mL (186.90 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8690 mL 9.3452 mL 18.6904 mL
5 mM 0.3738 mL 1.8690 mL 3.7381 mL
10 mM 0.1869 mL 0.9345 mL 1.8690 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.67 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.95%

COA (258 KB) HNMR (124 KB) LCMS (95 KB)

取扱説明書 (2659 KB)
参考文献
動物実験
[1]

At 4 weeks after the operation, 39 myocardial infarction rats survived. Thirty are randomly selected without bias and divided into five groups such that the distribution of infarct size and body weight among groups are similar, and given vehicle, conivaptan (0.03, 0.1 and 0.3 mg/kg) or SR121463A (0.3 mg/kg) by intravenous administration. Sham rats are also divided into four groups and given vehicle or conivaptan (0.03, 0.1 and 0.3 mg/kg) by intravenous administration. Rats are then placed individually in metabolic cages and urine is collected for 3 h. Urine osmolality is measured by the freezing point depression method using an osmometer.

MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8690 mL 9.3452 mL 18.6904 mL 46.7259 mL
5 mM 0.3738 mL 1.8690 mL 3.7381 mL 9.3452 mL
10 mM 0.1869 mL 0.9345 mL 1.8690 mL 4.6726 mL
15 mM 0.1246 mL 0.6230 mL 1.2460 mL 3.1151 mL
20 mM 0.0935 mL 0.4673 mL 0.9345 mL 2.3363 mL
25 mM 0.0748 mL 0.3738 mL 0.7476 mL 1.8690 mL
30 mM 0.0623 mL 0.3115 mL 0.6230 mL 1.5575 mL
40 mM 0.0467 mL 0.2336 mL 0.4673 mL 1.1681 mL
50 mM 0.0374 mL 0.1869 mL 0.3738 mL 0.9345 mL
60 mM 0.0312 mL 0.1558 mL 0.3115 mL 0.7788 mL
80 mM 0.0234 mL 0.1168 mL 0.2336 mL 0.5841 mL
100 mM 0.0187 mL 0.0935 mL 0.1869 mL 0.4673 mL
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Conivaptan hydrochloride Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Conivaptan168626-94-6YM 087YM087YM-087Vasopressin ReceptorInhibitorinhibitorinhibit

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