[D-Trp11]-Neurotensin

发表于由

[D-Trp11]-Neurotensin;

[D-Trp11]-Neurotensin 是 Neurotensin (NT) 的类似物，在灌注的大鼠心脏中是 NT 的选择性拮抗剂，但在豚鼠心房和大鼠胃条中起完全激动剂的作用。[D-Trp11]-Neurotensin 可抑制 NT 引起的低血压。

[D-Trp11]-Neurotensinamp;;

[D-Trp11]-Neurotensin Chemical Structure

CAS No. : 73634-68-1

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生物活性

[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. [D-Trp11]-Neurotensin can inhibit NT-induced hypotension[1][2].

IC50 Target

Neurotensin Receptor[1]
体外研究
(In Vitro)

[D-Trp11]-Neurotensin (0.13-1.1 μM) markedly inhibits NT-induced coronary vessel constriction in perfused rat hearts[1].
[D-Trp11]-Neurotensin (2-110 μM) exhibits NT-like activity in perfused rat hearts[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

[D-Trp11]-Neurotensin (50-500 nmol/kg; i.v.) has hypotensive activity in pentobarbital-anesthetized rats, with an ED25 of 122 nmol/kg[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

1695.96

Formula

C80H122N22O19
CAS 号

73634-68-1
Sequence

{Pyr}-Leu-Tyr-Glu-Asn-Lys-Pro-Arg-Arg-Pro-{D-Trp}-Ile-Leu
Sequence Shortening

{Pyr}-LYENKPRRP-{D-Trp}-IL
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
Solvent Solubility
In Vitro:;

H2O

Peptide Solubility and Storage Guidelines:

1.;;Calculate the length of the peptide.

2.;;Calculate the overall charge of the entire peptide according to the following table:

; Contents Assign value
Acidic amino acid Asp (D), Glu (E), and the C-terminal -COOH. -1
Basic amino acid Arg (R), Lys (K), His (H), and the N-terminal -NH2 +1
Neutral amino acid Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) 0

3.;;Recommended solution:

Overall charge of peptide Details
Negative (lt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, add NH4OH (lt;50 μL).
3.;;If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide.
Positive (gt;0) 1.;;Try to dissolve the peptide in water first.
2.;;If water fails, try dissolving the peptide in a 10%-30% acetic acid solution.
3.;;If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO.
Zero (=0) 1.;;Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first.
2.;;For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration.
参考文献

  • [1]. Quirion R, et, al. Selective blockade of neurotensin-induced coronary vessel constriction in perfused rat hearts by a neurotensin analogue. Eur J Pharmacol. 1980 Feb 8;61(3):309-12.

    [2]. Quirion R, et, al. Hypotensive effects of centrally and peripherally administered neurotensin and neurotensin derivatives in rats. Neuropeptides. 1981 Jou. 1(4): 253-9.