Spantide I TFA 是substance P 的类似物，是选择性的神经激肽-1 受体 (NK1receptor) 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 TFA, a substance P analog, is a selectiveNK1receptorantagonist, withKivalues of 230 nM and 8150 nM for NK1and NK2receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokineIL-10in the infected cornea, leading to a significant reduction in corneal perforation[1][2][3]. |
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].
| 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 | |
| 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 | 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 (<0) | 1. Try to dissolve the peptide in water first.
2. If water fails, add NH4OH (<50 μL).
3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. | | Positive (>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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