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Nelivaptan

🥰Excellent
Catalog No. T28153Cas No. 439687-69-1
Alias SSR149415, SR-149415, SR 149415

Nelivaptan (SR 149415) is a vasopressin V1b receptor antagonist that can eliminate CHS-induced GE damage and inhibit [3H]AVP binding in a competitive manner.

Nelivaptan

Nelivaptan

🥰Excellent
Purity: 98.39%
Catalog No. T28153Alias SSR149415, SR-149415, SR 149415Cas No. 439687-69-1
Nelivaptan (SR 149415) is a vasopressin V1b receptor antagonist that can eliminate CHS-induced GE damage and inhibit [3H]AVP binding in a competitive manner.
Pack SizePriceAvailabilityQuantity
1 mg$71In Stock
5 mg$153In Stock
10 mg$220In Stock
25 mg$367In Stock
50 mg$545In Stock
100 mg$785In Stock
500 mg$1,630In Stock
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Purity:98.39%
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Product Introduction

Bioactivity
Description
Nelivaptan (SR 149415) is a vasopressin V1b receptor antagonist that can eliminate CHS-induced GE damage and inhibit [3H]AVP binding in a competitive manner.
In vitro
METHODS: Nelivaptan (SR 149415) (1.25 nM, 2.5 nM and 5 nM) was used to treat In-R1-G9 pancreatic model cells, and the inhibitory effect of Nelivaptan on the specific binding of [3H]AVP (radiolabeled vasopressin) was detected.
RESULTS As the concentration of Nelivaptan5 increased, the Kd value (dissociation constant) under control conditions showed a dose-dependent decrease, which indicated that Nelivaptan inhibited the binding of [3H]AVP in a competitive manner, and the Ki value of Nelivaptan (inhibition constant) is 1.61 ± 0.17 nM. [1]
In vivo
METHODS: Animals in the male Wistar rat administration group and the Nelivaptan (SR 149415) group were intraperitoneally injected with drug (1ml/kg, 5% DMSO, 95% normal saline) or Nelivaptan dissolved in the drug (1ml/kg; stock solution concentration 5mg/kg) , the rats were placed in a high temperature environment of 38°C for 60 minutes, and the body weight and rectal temperature were measured before and immediately after treatment.
RESULTS Nelivaptan treatment reduced intracranial V1bR levels. [2]
METHODS: Nelivaptan was injected with DMSO as solvent at a dose of 1 nmol/rat (icv) with a volume of 5µl. The rats were monitored under basal non-stress (NS) conditions, acute stress (AS), CHS and CHeS. Changes in hypothalamic OXT and AVP release under conditions.
RESULTS Nelivaptan could eliminate CHS-induced GE damage. [3]
AliasSSR149415, SR-149415, SR 149415
Chemical Properties
Molecular Weight630.11
FormulaC30H32ClN3O8S
Cas No.439687-69-1
SmilesO=C1[C@](C=2C(N1S(=O)(=O)C3=C(OC)C=C(OC)C=C3)=CC=C(Cl)C2)(N4[C@H](C(N(C)C)=O)C[C@@H](O)C4)C5=C(OC)C=CC=C5
Relative Density.1.414 g/cm3 (Predicted)
Storage & Solubility Information
Storagekeep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (79.35 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.5870 mL7.9351 mL15.8702 mL79.3512 mL
5 mM0.3174 mL1.5870 mL3.1740 mL15.8702 mL
10 mM0.1587 mL0.7935 mL1.5870 mL7.9351 mL
20 mM0.0794 mL0.3968 mL0.7935 mL3.9676 mL
50 mM0.0317 mL0.1587 mL0.3174 mL1.5870 mL

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