PL-017

发表于由

PL-017;

PL-017 是一种有效的，选择性 μ 阿片受体 (μ opioid receptor) 激动剂，对 125I-FK 33,824 与 μ 位点结合的 IC50 为 5.5 nM。PL-017 在大鼠中产生持久的可逆性缓解疼痛作用。

PL-017amp;;

PL-017 Chemical Structure

CAS No. : 83397-56-2

规格 是否有货
100 mg ; 询价 ;
250 mg ; 询价 ;
500 mg ; 询价 ;

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生物活性

PL-017 is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats[1].

IC50 Target

IC50: 5.5 nM (125I-FK 33,824 binding to μ site)[1]
体外研究
(In Vitro)

PL-017 has an IC50 of 10000 nM for 125I-DADLE binding to δ site[1].

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

PL-017 (0.22, 0.45, 0.9 nmol/rat; i.c.v.) has the time of maximum effect of approximately 15 to 30 mm after injection at lower doses and produces analgesia lasting as long as 4 hours with larger doses in male Sprague-Dawley rats weighing 250 to 375 g[1].

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

535.63

Formula

C29H37N5O5
CAS 号

83397-56-2
Sequence Shortening

YP-{N(Me)Phe}-P-NH2
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]. K J Chang, et al. Potent morphiceptin analogs: structure activity relationships and morphine-like activities. J Pharmacol Exp Ther. 1983 Nov;227(2):403-8.