[Trp11]-Neurotensin
[Trp11]-Neurotensin is a neurotensin analog and neurotensin receptor agonist. The Tyr11 residue of neurotensin is replaced by L-Trp. [Trp11]-Neurotensin competes for neurotensin receptor binding sites, with an IC50 of 4.3 nM in rat brain synaptic membranes, and activates neurotensin receptor-mediated smooth muscle responses, with an EC50 of 1.7 nM in rat ileum, exhibiting significant species-dependent differences in receptor recognition. [Trp11]-Neurotensin can be used in studies related to neurotensin receptor pharmacology, gastrointestinal smooth muscle, and species-dependent receptor recognition.
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- CAS No.: 75644-95-0
- Formula: C80H122N22O19
- Molecular Weight:1695.99
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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Rat brain Neurotensin receptors 4.3 nM (IC50) |
Rat ileum 1.7 nM (EC50) |
Guinea-pig brain Neurotensin receptors 40 nM (IC50) |
Guinea-pig ileum 30 nM (EC50) |
[Trp11]-Neurotensin activates neurotensin receptor-mediated responses in isolated tissues. Its agonistic activity is slightly higher than that of neurotensin in rat gastric smooth muscle and perfused rat coronary vessels, but weaker in guinea pig atria[1].
[Trp11]-Neurotensin competitively inhibits the binding of [3H]Neurotensin to brain synaptic membranes of rats and guinea pigs, with IC50 values of 4.3 nM and 40 nM, respectively, and exhibits full agonist activity in the ileum of rats and guinea pigs, with EC50 values of 1.7 nM and 30 nM[2].
[Trp11]-Neurotensin relaxes rat ileum pre-contracted by acetylcholine, with an EC50 of 1.7 nM, and achieves a maximum relaxation effect similar to that of Neurotensin at approximately 30 nM[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 75644-95-0
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Molecular Weight 1695.99
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Formula C80H122N22O19
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Sequence
{Pyr}-Leu-Tyr-Glu-Asn-Lys-Pro-Arg-Arg-Pro-Trp-Ile-Leu
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Sequence Shortening
{Pyr}-LYENKPRRPWIL
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)