Basic information Safety Supplier Related

LIXIVAPTAN

Basic information Safety Supplier Related

LIXIVAPTAN Basic information

Product Name:
LIXIVAPTAN
Synonyms:
  • LIXIVAPTAN
  • N-[3-Chloro-4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)-ylcarbonyl)phenyl]-5-fluoro-2-methylbenzamide
  • VPA 985
  • BenzaMide,N-[3-chloro-4-(5H-pyrrolo[2,1-c][1,4]benzodiazepin-10(11H)-ylcarbonyl)phenyl]-5-fluoro-2-Methyl-
  • N-[3-Chloro-4-(5H-pyrrolo[2,1-c][1,4]benzodiazepine-10(11H)-ylcarbonyl)phenyl]-5-fluoro-2-methylbenzamide
  • N-[3-chloro-4-(6,11-dihydropyrrolo[2,1-c][1,4]benzodiazepine-5-carbonyl)phenyl]-5-fluoro-2-methyl-benzamide
  • Lixivaptan (VPA-985)
  • VPA985;LIXIVAPTAN (VPA 985)
CAS:
168079-32-1
MF:
C27H21ClFN3O2
MW:
473.93
Product Categories:
  • Aromatics
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
Mol File:
168079-32-1.mol
More
Less

LIXIVAPTAN Chemical Properties

Melting point:
>114°C (dec.)
Boiling point:
626.5±55.0 °C(Predicted)
Density 
1.32
storage temp. 
Sealed in dry,Room Temperature
solubility 
DMSO: soluble20mg/mL, clear
pka
11.86±0.70(Predicted)
form 
powder
color 
white to beige
InChI
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)
InChIKey
PPHTXRNHTVLQED-UHFFFAOYSA-N
SMILES
C(NC1=CC=C(C(N2C3=CC=CC=C3CN3C=CC=C3C2)=O)C(Cl)=C1)(=O)C1=CC(F)=CC=C1C
More
Less

Safety Information

WGK Germany 
3
More
Less

LIXIVAPTAN Usage And Synthesis

Uses

Lixivaptan is a drug used in the treatment and prevention of cardiovascular diseases.

Biological Activity

Arginine vasopressin (AVP) plays an important part in circulatory and water homoeostasis and is important in renal hemodynamic alterations, water retention, and cardiac remodeling in congestive heart failure (CHF). Lixivaptan is an AVP V2-receptor selective antagonist th at increases water excretion and normalizes serum sodium levels. Lixivaptan has been in clinical trials for hyponatremia associated with heart failure.

in vivo

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].

IC 50

V2 Receptor

LIXIVAPTANSupplier

Dezhou LonWel Pharmaceutical Technology Co., Ltd. Gold
Tel
13761310616
Email
39324283@qq.com
Shanghai Boyle Chemical Co., Ltd.
Tel
021-50182298 021-50180596
Email
sales@boylechem.com
J & K SCIENTIFIC LTD.
Tel
18210857532; 18210857532
Email
jkinfo@jkchemical.com
NOTA Chemical (Shanghai) Co.,Ltd
Tel
021-50189163
Email
sales@notachem.com
Chemsky（shanghai）International Co.,Ltd.
Tel
021-50135380
Email
shchemsky@sina.com
More
Less

LIXIVAPTAN(168079-32-1)Related Product Information