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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 Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $71 | In Stock | |
5 mg | $153 | In Stock | |
10 mg | $220 | In Stock | |
25 mg | $367 | In Stock | |
50 mg | $545 | In Stock | |
100 mg | $785 | In Stock | |
500 mg | $1,630 | In Stock |
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] |
Alias | SSR149415, SR-149415, SR 149415 |
Molecular Weight | 630.11 |
Formula | C30H32ClN3O8S |
Cas No. | 439687-69-1 |
Smiles | O=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 | keep 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
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