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LSKL,Inhibitor of Thrombospondin(TSP-1)(TFA)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LSKL,Inhibitor of Thrombospondin(TSP-1)(TFA)图片
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品名称
LSKL, 血小板反应蛋白抑制剂 (TSP-1) 三氟醋酸盐
产品介绍
LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 是一种衍生自 LAP-TGFβ 的四肽,是一种竞争性的TGF-β1拮抗剂。LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 抑制TSP-1与 LAP 的结合并减轻肾间质纤维化和肝纤维化。LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 通过抑制TSP-1介导的TGF-β1活性来抑制蛛网膜下纤维化,防止慢性脑积水的发生并改善蛛网膜下腔出血后的长期神经认知缺陷。LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 可以轻松穿越血脑屏障。
生物活性

LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitiveTGF-β1antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding ofTSP-1to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition ofTSP-1-mediatedTGF-β1activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier[1][2].

IC50& Target

TGF-β1[1]

体外研究
(In Vitro)

The KTFR sequence from ADAMTS1 is responsible for the interaction with the LSKL, Inhibitor of Thrombospondin (TSP-1) (LSKL peptide) from the latent form of TGF-β, leading to its activation. There is a stable binding mode between LSKL, Inhibitor of Thrombospondin (TSP-1) and ADAMTS1 KTFR sequence, characterized by 3 salt bridges and 2 hydrogen bonds[2].

体内研究
(In Vivo)

LSKL, Inhibitor of Thrombospondin (TSP-1) (1 mg/kg; intraperitoneal injection; male Sprague-Dawley rats) is protective against subarachnoid fibrosis, attenuates ventriculomegaly and effectively suppresses hydrocephalus. LSKL, Inhibitor of Thrombospondin (TSP-1) treatment inhibits TGF-β1 activity and subsequent Smad2/3 signaling[1].
LSKL, Inhibitor of Thrombospondin (TSP-1) (30 mg/kg, i.p.) successfully inhibits transforming growth factor (TGF) β-Smad signal activation induced by partial hepatectomy. LSKL, Inhibitor of Thrombospondin (TSP-1) successfully attenuates TGF-β-Smad signal activation by antagonizing TSP-1, but not by reducing TSP-1 protein expression. LSKL, Inhibitor of Thrombospondin (TSP-1) accelerates hepatocyte proliferation after hepatectomy[3].

Animal Model:103 male Sprague-Dawley rats (6 weeks of age; 160-180 g) with subarachnoid hemorrhage (SAH)[1]
Dosage:1 mg/kg
Administration:Intraperitoneal injection
Result:Was protective against subarachnoid fibrosis, attenuated ventriculomegaly and effectively suppressed hydrocephalus.
分子量

572.62

性状

Solid

Formula

C23H43F3N6O7

Sequence

Leu-Ser-Lys-Leu

Sequence Shortening

LSKL

中文名称

LSKL, 血小板反应蛋白抑制剂 (TSP-1) 三氟醋酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder-80°C2 years
-20°C1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : 250 mg/mL(436.59 mM;Need ultrasonic)

H2O : 100 mg/mL(174.64 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.7464 mL8.7318 mL17.4636 mL
5 mM0.3493 mL1.7464 mL3.4927 mL
10 mM0.1746 mL0.8732 mL1.7464 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (174.64 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.63 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (3.63 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.63 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。