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作靶點(diǎn): TGF- Receptor作通路: TGF-beta/Smad儲(chǔ)存式: Powder -80C 2 years-20C 1 yearIn solvent -8

2、0C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (218.05 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)

3、請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.45 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE2. 請(qǐng)依序添加每種溶劑： 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)種四肽，源于潛在聯(lián)系多肽，能夠抑制 TSP-1 的活性，來(lái)降低 TGF- 的活性，能夠阻肝損傷和肝纖維化。體外研究 LSKL peptide is able to reduce liver fibrosis by inhibiting TGF- activation 2.體內(nèi)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