Spantide I 是substance P 的类似物，是选择性的神经激肽-1 受体 (NK1 receptor) 的拮抗剂，其对NK1 和 NK2 受体的 Ki 值分别为 230 nM 和 8150 nM。Spantide I 可减少感染角膜的1型细胞因子和增强2型细胞因子 IL-10，从而显著减少角膜穿孔。
| 生物活性 |
Spantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation[1][2][3].
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| IC50 Target[2] |
|
NK1
230 nM (Ki)
|
NK2
8150 nM (Ki)
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|
体内研究
(In Vivo) |
Spantide I (50 and 100 nM perfused through the cerebral ventricles) causes a complete respiratory arrest in all of the examined animals[2].
Spantide I (36 μg/mouse, ip daily) significantly decreases the number of perforated corneas, bacterial counts, and PMNs. Spantide I also downregulates the mRNA levels for type I cytokines (e.g., IFN-γ) as well as MIP-2, IL-6, TNF-α, and IL-1β[3].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: |
Female, 8-week-old C57BL/6 (B6) and BALB/c mice[3]. |
| Dosage: |
36 μg/mouse. |
| Administration: |
IP on days -1 and 0 (day of infection) and daily through 5 days pi (post infection). |
| Result: |
At 3 and 5 days pi, compound-treated mice had significantly less severe ocular disease than did the PBS-treated mice.
Contained significantly fewer PMNs than the corneas of PBS-treated mice at 3 and 5 days pi.
Significantly reduced levels of corneal TNF-α mRNA at 3 and 5 days pi.
Significantly reduced the level of IL-18 mRNA at 1 day pi. |
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| 分子量 |
|
| Formula |
|
| CAS 号 |
|
| Sequence Shortening |
{D-Arg}PKPQQ-{D-Trp}-F-{D-Trp}-LL-NH2
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere.
|
| 储存方式 |
| Powder |
-80deg;C |
2 years |
|
-20deg;C |
1 year |
| In solvent |
-80deg;C |
6 months |
|
-20deg;C |
1 month |
|
| 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. |
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| 参考文献 |
-
[1]. J C Beaujouan, et al. Higher potency of RP 67580, in the mouse and the rat compared with other nonpeptide and peptide tachykinin NK1 antagonists. Br J Pharmacol. 1993 Mar;108(3):793-800.
[2]. M Zubrzycka, et al. Comparison of antagonistic properties of substance P analogs, spantide I, II and III, on evoked tongue jerks in rats. Endocr Regul. 2000 Mar;34(1):13-8.
[3]. Linda D Hazlett, et al. Spantide I decreases type I cytokines, enhances IL-10, and reduces corneal perforation in susceptible mice after Pseudomonas aeruginosa infection. Invest Ophthalmol Vis Sci. 2007 Feb;48(2):797-807.
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