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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELSKL, Inhibitor of Thrombospondin TSP-1Cat. No.: HY-P0299CAS No.: 283609-79-0分式: CHNO分量: 458.6Sequence: Leu-Ser-Lys-LeuSequence Shortening: LSKL作靶点: TGF- Receptor作通路: TGF-beta/Smad储存式: Powder -80C 2 years-20C 1 yearIn solvent -8

2、0C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (218.05 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1805 mL 10.9027 mL 21.8055 mL5 mM 0.4361 mL 2.1805 mL 4.3611 mL10 mM 0.2181 mL 1.0903 mL 2.1805 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,并请注意储备液的保存式和期限。体内实验

3、请根据您的实验动物和给药式选择适当的溶解案,配制前请先配制澄清的储备液,再依次添加助溶剂(为保证实验结果的可靠性,体内实验的作液,建议您现现配,当天使;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占):1. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.45 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE2. 请依序添加每种溶剂: 10% DMSO 90% corn

4、oilSolubility: 2.5 mg/mL (5.45 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 LSKL, Inhibitor of Thrombospondin (TSP-1)种四肽,源于潜在联系多肽,能够抑制 TSP-1 的活性,来降低 TGF- 的活性,能够阻肝损伤和肝纤维化。体外研究 LSKL peptide is able to reduce liver fibrosis by inhibiting TGF- activation 2.体内研究 LSKL (1 mg/kg, i.p.) can easily traverse the

5、blood brain barrier. LSKL peptide also alleviates hydrocephalusand improves long-term cognitive function following SAH. Moreover, LSKL peptide inhibits subarachnoidfibrosis after SAH. LSKL treatment significantly decreases the activation of TGF-1 in the CSF in comparisonwith that in the SAH+PBS grou

6、p 1. LSKL peptide (30 mg/kg, i.p.) successfully inhibits transforming growthfactor (TGF) -Smad signal activation induced by partial hepatectomy. LSKL peptide successfully attenuatesTGF-Smad signal activation by antagonizing TSP-1, but not by reducing TSP-1 protein expression. LSKLpeptide accelerates

7、 hepatocyte proliferation after hepatectomy 3.PROTOCOLAnimal Wild-type 812-week-old male mice (C57BL/6) are used for all experiments. LSKL TSP-1 inhibitory peptide isAdministration 3 diluted to 5 mg/mL with normal saline. In the LSKL peptide group, LSKL peptide (30 mg/kg bodyweight in 6mL/kg) is adm

8、inistered intraperitoneally before abdominal wall closure and at 6 h after the 70 per centhepatectomy. In the normal saline group, saline (6 mL/kg) is given intraperitoneally at the same time points.In the sham-operated group, laparotomy is performed and the incision is sutured after normal saline (

9、6mL/kg) have been administered intraperitoneally.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Liao F, et al. LSKL peptide alleviates subarachnoid fibrosis and hydrocephalus by inhibiting TSP1-mediated TGF-1 signaling activityfollowing su

10、barachnoid hemorrhage in rats. Exp Ther Med. 2016 Oct;12(4):2537-2543. Epub 2016 Aug 31.2. Laurent MA, et al. In silico characterization of the interaction between LSKL peptide, a LAP-TGF-beta derived peptide, and ADAMTS1.Comput Biol Chem. 2016 Apr;61:155-61.3. Kuroki H, et al. Effect of LSKL peptide on thrombospondin 1-mediated transforming growth factor signal activation and liverregeneration after hepatectomy in an experimental model. Br J Surg. 2015 Jun;102(7):813-25.McePdfHeightCaution: Product has not been f

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