1. GPCR/G Protein
  2. Vasopressin Receptor
  3. Lixivaptan

Lixivaptan (Synonyms: VPA-985; WAY-VPA 985)

製品番号: HY-14185 純度: 99.90%
取扱説明書

Lixivaptan (VPA-985, WAY-VPA 985) is an orally active and selective vasopressin receptor V2 antagonist, with IC50 values of 1.2 and 2.3 nM for human and rat V2, respectively.

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Lixivaptan 構造式

Lixivaptan 構造式

CAS 番号 : 168079-32-1

容量 価格(税別) 在庫状況 数量
無料サンプル (0.5-1 mg)   今すぐ申し込む  
10 mM * 1  mL in DMSO USD 88 在庫あり
Estimated Time of Arrival: December 31
2 mg USD 60 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 84 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 144 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 312 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 552 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 984 在庫あり
Estimated Time of Arrival: December 31
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

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Based on 1 publication(s) in Google Scholar

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製品説明

Lixivaptan (VPA-985, WAY-VPA 985) is an orally active and selective vasopressin receptor V2 antagonist, with IC50 values of 1.2 and 2.3 nM for human and rat V2, respectively.

IC50 & Target

IC50: 1.2 nM (human V2), 2.3 nM (rat V2)[1]

体外実験

Lixivaptan displays competitive antagonist activity at V2 receptors[1].

体内実験

In conscious dogs, water-loaded with 30 mL/kg (po) and arginine vasopressin (AVP)-treated (0.4 µg/kg in oil, sc), lixivaptan (1, 3, and 10 mg/kg po) increases Uvol over the AVP-treated vehicle group by 438, 1018, and 1133%, respectively, while Uosm decreases from 1222 mOsm/kg (water-loaded and AVP treated vehicle) to 307, 221, and 175 mOsm/kg, respectively. In homozygous Brattleboro rats lacking AVP, lixivaptan at 10 mg/kg po (i.e., 10 times the dose producing V2 antagonist activity) b.i.d. for 5 days, shows a sustained antagonist action without evidence of agonist effects. In a randomized double-blind placebo-controlled ascending single dose study, patients (deprived of fluids overnight before dosing) are dosed orally with 30, 75, or 150 mg of lixivaptan. All three doses increase urine flow and serum sodium concentrations and produced significant dose-related decreases in urinary osmolality[1]. Phase II clinical trials in patients with congestive heart failure, liver cirrhosis with ascites or syndrome of inappropriate antidiuretic hormone have demonstrated that lixivaptan increases water clearance without affecting renal sodium excretion or activating the neurohormonal system[2].

臨床実験
分子量

473.93

分子式

C₂₇H₂₁ClFN₃O₂

CAS 番号

168079-32-1

SMILES

O=C(C1=C(Cl)C=C(NC(C2=CC(F)=CC=C2C)=O)C=C1)N(C3)C4=CC=CC=C4CN5C3=CC=C5

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶剤 & 溶解度
体外: 

DMSO : ≥ 150 mg/mL (316.50 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1100 mL 10.5501 mL 21.1002 mL
5 mM 0.4220 mL 2.1100 mL 4.2200 mL
10 mM 0.2110 mL 1.0550 mL 2.1100 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (4.39 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.39 mM); Clear solution

*All of the co-solvents are provided by MCE.
参考文献

純度: 99.90%

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The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

LixivaptanVPA-985WAY-VPA 985VPA985VPA 985Vasopressin ReceptorInhibitorinhibitorinhibit

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製品名:
Lixivaptan
製品番号:
HY-14185
数量:
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