(D-ARG1,D-TRP7·9,LEU11)-SUBSTANCE P

生物活性靶点体内研究 (D-ARG1,D-TRP7·9,LEU11)-SUBSTANCE P 试剂级价格

CAS号:91224-37-2
英文名:D-ARG-PRO-LYS-PRO-GLN-GLN-D-TRP-PHE-D-TRP-LEU-LEU-NH2 HYDROCHLORIDE
中文名:(D-ARG1,D-TRP7·9,LEU11)-SUBSTANCE P
CBNumber:CB2230566
分子式:C75H108N20O13
分子量:1497.79
MOL File:91224-37-2.mol

(D-ARG1,D-TRP7·9,LEU11)-SUBSTANCE P化学性质

密度 :1.43±0.1 g/cm3(Predicted)
储存条件 :−20°C
形态 :Powder
酸度系数(pKa) :13.31±0.20(Predicted)
颜色 :White to off-white
水溶解性 :Soluble to 1 mg/ml in water

安全信息

WGK Germany :3

(D-ARG1,D-TRP7·9,LEU11)-SUBSTANCE P性质、用途与生产工艺

生物活性 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。
靶点

NK1

230 nM (Ki)

NK2

8150 nM (Ki)

体内研究

Spantide I (50 and 100 nM perfused through the cerebral ventricles) causes a complete respiratory arrest in all of the examined animals.
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.

Animal Model:	Female, 8-week-old C57BL/6 (B6) and BALB/c mice.
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.