الصفحة الرئيسية>>Signaling Pathways>> GPCR/G protein>> Vasopressin Receptor>>Lixivaptan (VPA-985)

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

رقم الكتالوجGC32453

Lixivaptan (VPA-985) (VPA-985 ، WAY-VPA 985) هو مضاد V2 نشط وانتقائي لمستقبل الفازوبريسين ، بقيم IC50 تبلغ 1.2 و 2.3 نانومتر للإنسان والجرذان V2 ، على التوالي.

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Lixivaptan (VPA-985) التركيب الكيميائي

Cas No.: 168079-32-1

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
74٫00
متوفر
2mg
46٫00
متوفر
5mg
71٫00
متوفر
10mg
125٫00
متوفر
25mg
262٫00
متوفر
50mg
455٫00
متوفر
100mg
818٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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.

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

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].

[1]. Albright JD, et al. 5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors. J Med Chem. 1998 Jul 2;41(14):2442-4. [2]. Ghali JK, et al. Lixivaptan, a non-peptide vasopressin V2 receptor antagonist for the potential oral treatment of hyponatremia. IDrugs. 2010 Nov;13(11):782-92.

Chemical Properties

Cas No. 168079-32-1 SDF
المرادفات VPA-985, WAY-VPA-985
Canonical 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
Formula C27H21ClFN3O2 M.Wt 473.93
الذوبان DMSO : ≥ 150 mg/mL (316.50 mM) 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.11 mL 10.5501 mL 21.1002 mL
5 mM 0.422 mL 2.11 mL 4.22 mL
10 mM 0.211 mL 1.055 mL 2.11 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 37 reference(s) in Google Scholar.)

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