Product Details
| Product Name:
Nelivaptan |
CAS No.:
439687-69-1 |
| Purity:
98.39% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | Nelivaptan |
| 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] |
| 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)
|
| Keywords | Nelivaptan | SSR 149415 | SR149415 | SSR-149415 |
| Inhibitors Related | Atosiban acetate | Desmopressin acetate (16679-58-6 free base) | OPC-51803 | Felypressin acetate | Balovaptan | d[Cha4]-AVP acetate(500170-27-4 free base) | TASP0390325 | d[Leu4,Lys8]-VP acetate | L-371,257 | Fuscoside | Conopressin S acetate(111317-90-9 free base) | Tolvaptan |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$0.00/50g |
VIP3Y
|
HangZhou RunYan Pharma Technology Co.,LTD.
|
2024-09-19 |
United States