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Mozavaptan

CAS No.
137975-06-5
Chemical Name:
Mozavaptan
Synonyms
CS-134;OPC31260l;OPC 31260;MOZAVAPTAN;Mozavaptan USP/EP/BP;Mozavaptan (OPC-31260);N-(4-(5-(Dimethylamino);OPC-31260; OPC31260L; OPC 31260;-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl);5-(Dimethylamino)-1-[4-(2-methylbenzamido)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine
CBNumber:
CB51388577
Molecular Formula:
C27H29N3O2
Molecular Weight:
427.54
MDL Number:
MFCD00908918
MOL File:
137975-06-5.mol
MSDS File:
SDS
Last updated:2024-11-06 18:33:45

Mozavaptan Properties

Melting point 213 - 217°C
Boiling point 543.0±50.0 °C(Predicted)
Density 1.21±0.1 g/cm3(Predicted)
storage temp. Sealed in dry,Room Temperature
solubility Chloroform (Slightly), DMSO (Slightly), Methanol (Slightly)
form Solid
pka 13.04±0.70(Predicted)
color White to Off-White
FDA UNII 17OJ42922Y

Mozavaptan price More Price(23)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
TRC M732720 Mozavaptan 137975-06-5 5mg $130 2021-12-16 Buy
ApexBio Technology B2299 Mozavaptan 137975-06-5 10mg $95 2021-12-16 Buy
Biosynth Carbosynth FD71413 5-(Dimethylamino)-1-[4-(2-methylbenzamido)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine 137975-06-5 100mg $120 2021-12-16 Buy
ChemScene CS-6286 Mozavaptan 99.89% 137975-06-5 10mg $60 2021-12-16 Buy
ChemScene CS-6286 Mozavaptan 99.89% 137975-06-5 50mg $180 2021-12-16 Buy
Product number Packaging Price Buy
M732720 5mg $130 Buy
B2299 10mg $95 Buy
FD71413 100mg $120 Buy
CS-6286 10mg $60 Buy
CS-6286 50mg $180 Buy

Mozavaptan Chemical Properties,Uses,Production

Description

Mozavaptan is an oral vasopressin V2 antagonist that has been launched in Japan for inappropriate antidiuretic hormone secretion syndrome (IADHS), an affliction manifesting as hyponatremia. It joins another nonpeptidic benzazepine, conivaptan, which corrects sodium and water imbalance by blocking the renal V2 receptor resulting in enhanced diuresis, thereby effectively increasing serum sodium concentration. While conivaptan inhibits both V1 and V2 receptors, mozavaptan is significantly more selective for V2 (IC50 of 14nM vs. 1.2 mM for V1).

Originator

Otsuka (Japan)

Uses

Mozavaptan is a vasopressin-receptor antagonist. It is used in the treatment of congestive heart failure and hyponatremia.

Uses

vasopressin V2 receptor antagonist

Definition

ChEBI: Mozavaptan is a member of benzamides.

brand name

Physuline

Synthesis

The reported synthesis of mozavaptan is shown in the scheme. Readily available benzazepin-5-one 39 was refluxed with 40% methyl amine methanol solution in the presence of molecular sieves for 5h followed by the reduction of the resulting imine with sodium borohydride to give the monomethyl amine. Reductive alkylation of the monomethyl amine with formaldehyde in the presence of sodium cyanoborohydride gave the dimethyl amino benzazepine 40. Removal of the tosyl group was facilitated by heating 40 in polyphosphoric acid at 150oC for 2 h to give 41 in 97% yield. Reaction of the resulting benzazepine 41 with p-nitrobenzoyl chloride (42) in the presence of triethylamine provided amide 43 which was hydrogenated in the presence of 10% Pd/C in ethanol at room temperature to give aniline 44. Acylation of aniline 44 with 2-methylbenzoylchloride (45) in the presence of triethylamine gave mozavaptan (VI) in 54% yield.

Synthesis_137975-06-5

Mozavaptan Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 135)Suppliers
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Hebei Weibang Biotechnology Co., Ltd
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View Lastest Price from Mozavaptan manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Mozavaptan pictures 2024-11-06 Mozavaptan
137975-06-5
US $10.00 / KG 1KG 99% 10 mt Hebei Weibang Biotechnology Co., Ltd
Mozavaptan pictures 2023-09-05 Mozavaptan
137975-06-5
US $0.00 / KG 1KG 99% 50000KG/month Hebei Mojin Biotechnology Co., Ltd
Mozavaptan pictures 2021-07-13 Mozavaptan
137975-06-5
US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd
  • Mozavaptan pictures
  • Mozavaptan
    137975-06-5
  • US $10.00 / KG
  • 99%
  • Hebei Weibang Biotechnology Co., Ltd
  • Mozavaptan pictures
  • Mozavaptan
    137975-06-5
  • US $0.00 / KG
  • 99%
  • Hebei Mojin Biotechnology Co., Ltd
  • Mozavaptan pictures
  • Mozavaptan
    137975-06-5
  • US $15.00-10.00 / KG
  • 99%+ HPLC
  • Zhuozhou Wenxi import and Export Co., Ltd
OPC 31260 MOZAVAPTAN 5-(Dimethylamino)-1-[4-(2-methylbenzamido)benzoyl]-2,3,4,5-tetrahydro-1H-benzazepine Benzamide, N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methyl- -2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl) N-(4-(5-(Dimethylamino) CS-134 OPC-31260; OPC31260L; OPC 31260 OPC31260l N-[4-[[5-(dimethylamino)-2,3,4,5-tetrahydro-1H-1-benzazepin-1-yl]carbonyl]phenyl]-2-methyl- Mozavaptan USP/EP/BP N-[4-[5-(dimethylamino)-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide N-(4-(5-(Dimethylamino)-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)phenyl)-2-methylbenzamide Mozavaptan (OPC-31260) 137975-06-5 Inhibitors Pharmaceutical intermediate