Meclinertant (SR 48692) is an effective, selective, non-peptide and oral antagonist of active neurotensin receptor (NTS1). Meclinertant competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization in human colon cancer cells, with a pA2 value of 8.13. Meclinertant has anti-anxiety, anti-addiction and memory disorder effects.
Molecular Weight | 587.07 |
Formula | C32H31ClN4O5 |
CAS Number | 146362-70-1 |
Solubility (25°C) | DMSO 11.74 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
Related Neurotensin Receptor Products |
---|
Kinetensin
Kinetensin is a neurotensin-like peptide isolated from pepsin-treated human plasma. |
[Lys8, Lys9]-Neurotensin (8-13)
[Lys8, Lys9]-Neurotensin (8-13) (JMV438), a Neurotensin analog, exerts its analgesic effects through activation of the G protein-coupled receptors NTS1 and NTS2. |
[D-Trp11]-Neurotensin
[D-Trp11]-Neurotensin, an analogue of Neurotensin (NT), is a selective antagonist of NT in perfused rat hearts but behaves as a full agonist in guinea pig atria and rat stomach strips. |
Contulakin G
Contulakin G is an O-glycosylated invertebrate neurotensin. |
Acetyl neurotensin (8-13)
Acetyl neurotensin (8-13) is the shortest analog of neurotensin with full binding and pharmacological activities. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.