Lixivaptan

Alias: VPA-985; VPA985; VPA 985; WAY-VPA-985; WAY VPA-985; WAY-VPA 985; WAY VPA 985; CRTX-080; CRTX080; CRTX 080; Lixivaptan
Cat No.:V4748 Purity: ≥98%
Lixivaptan (formerly known as VPA-985, WAY-VPA 985) is a novel, potent, selective and orally bioactive non-peptide antagonist of vasopressin receptor V2 with IC50 values of 1.2 and 2.3 nM for human and rat V2, respectively.
Lixivaptan Chemical Structure CAS No.: 168079-32-1
Product category: Vasopressin Receptor
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Lixivaptan (formerly known as VPA-985, WAY-VPA 985) is a novel, potent, selective and orally bioactive non-peptide antagonist of vasopressin receptor V2 with IC50 values of 1.2 and 2.3 nM for human and rat V2, respectively. Lixivaptan functions by inhibiting the function of the vasopressin hormone, which prevents the excretion of fluid. Vasopressin is an anti-diuretic hormone that causes the kidneys to retain water, and lixivaptan works by blocking it. Vasopressin can provide protective effects when the body needs to stay hydrated under specific circumstances.

Biological Activity I Assay Protocols (From Reference)
Targets
human V2 receptor ( IC50 = 1.2 nM ); rat V2 receptor ( IC50 = 2.3 nM )
ln Vitro
Lixivaptan exhibits competitive antagonist activity on V2 absorption [1].
ln Vivo
In conscious dogs, lixivaptan (1, 3, and 10 mg/kg po) was administered with 30 mL/kg (po) and arginine vasopressin (AVP)-treated water (0.4 μg/kg in oil, subcutaneously) ) ) relative to the AVP-treated vehicle group increased Uvol by 438, 1018, and 1133%, respectively, while Uosm decreased from 1222 mOsm/kg (water-loaded and AVP-treated vehicle) to 307, 221, and 175 mOsm/kg, respectively. In AVP-deficient homozygous Brattleboro, lixivaptan at 10 mg/kg po (i.e., 10 times the dose that produced V2 multiantagonist activity) bid for 5 days showed sustained multiantagonist effects without evidence of agonist effects. In a randomized, double-blind, gradient-controlled ascending single-dose study, patients (fasted overnight before formulation) and mice received 30, 75, or 150 mg of lixivaptan. All of these increased doses increase urine flow and serum sodium concentrations and produce significant dose-related decreases in urine osmolality [1]. Phase II clinical trials in patients with congestive heart failure, liver tumor ascites, or inappropriate antidiuretic metabolic syndrome showed that lixivaptan increased water clearance rather than affecting renal sodium excretion or activating the neurohormonal system [2].
References

[1]. 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]. Lixivaptan, a non-peptide vasopressin V2 receptor antagonist for the potential oral treatment of hyponatremia. IDrugs. 2010 Nov;13(11):782-92.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C27H21CLFN3O2
Molecular Weight
473.92594
Exact Mass
473.13
Elemental Analysis
C, 68.43; H, 4.47; Cl, 7.48; F, 4.01; N, 8.87; O, 6.75
CAS #
168079-32-1
Appearance
Solid powder
SMILES
CC1=C(C=C(C=C1)F)C(=O)NC2=CC(=C(C=C2)C(=O)N3CC4=CC=CN4CC5=CC=CC=C53)Cl
InChi Key
PPHTXRNHTVLQED-UHFFFAOYSA-N
InChi Code
InChI=1S/C27H21ClFN3O2/c1-17-8-9-19(29)13-23(17)26(33)30-20-10-11-22(24(28)14-20)27(34)32-16-21-6-4-12-31(21)15-18-5-2-3-7-25(18)32/h2-14H,15-16H2,1H3,(H,30,33)
Chemical Name
N-[3-chloro-4-(6,11-dihydropyrrolo[2,1-c][1,4]benzodiazepine-5-carbonyl)phenyl]-5-fluoro-2-methylbenzamide
Synonyms
VPA-985; VPA985; VPA 985; WAY-VPA-985; WAY VPA-985; WAY-VPA 985; WAY VPA 985; CRTX-080; CRTX080; CRTX 080; Lixivaptan
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~95 mg/mL (~200.5 mM)
Ethanol: ~7 mg/mL
Preparing Stock Solutions 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

*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.

Calculator

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g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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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.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01055912 Completed Drug: Lixivaptan
Drug: Placebo
Congestive Heart Failure CardioKine Inc. January 2010 Phase 2
NCT00876798 Completed Drug: Lixivaptan
Drug: Placebo
Euvolemic Hyponatremia CardioKine Inc. June 2009 Phase 3
NCT00578695 Completed Drug: lixivaptan
Drug: Placebo
Hyponatremia CardioKine Inc. January 2007 Phase 3
NCT00675701 Completed Drug: placebo
Drug: lixivaptan
Drug: moxifloxacin
Healthy CardioKine Inc. May 2008 Phase 1
NCT03487913 Completed Drug: Lixivaptan Autosomal Dominant Polycystic
Kidney Disease
Palladio Biosciences September 14, 2018 Phase 2
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