Spantide I 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, 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]. |
| 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].
| 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 | |
| 性状 | |
| 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 | Sealed storage, away from moisture | Powder | -80°C | 2 years | | -20°C | 1 year |
*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 100 mg/mL(66.77 mM;Need ultrasonic) 配制储备液 | 1 mM | 0.6677 mL | 3.3383 mL | 6.6765 mL | | 5 mM | 0.1335 mL | 0.6677 mL | 1.3353 mL | | 10 mM | 0.0668 mL | 0.3338 mL | 0.6677 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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