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PLpro inhibitor

NMR下載 COA and HPLC MSDS下載
names：
PLpro inhibitor
CAS號：
1093070-14-4
MDL Number： No data available
MF(分子式)： C22H22N2O2 MW(分子量)： 346.42
EINECS:No data available Reaxys Number:No data available
Pubchem ID:312811351 Brand:BIOFOUNT

PLpro inhibitor(1093070-14-4)是一種有效的木瓜蛋白酶樣蛋白酶（PLpro）抑制劑，PLpro抑制劑具有顯著的抗病毒活性。

貨品編碼	規(guī)格	純度	價格 (￥)	現(xiàn)價(￥)	特價(￥)	庫存描述	數(shù)量	總計 (￥)
YZM000881-5mg	5mg	99.7%	￥ 3295.00	￥ 3295.00		2-3天	- +	￥ 0.00
YZM000881-2mg	2mg	99.7%	￥ 2116.00	￥ 2116.00		2-3天	- +	￥ 0.00

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中文別名	PLpro inhibitor(1093070-14-4),5-(乙酰氨基)-2-甲基-N-[(1R)-1-(1-萘基)乙基]苯甲酰胺,PLpro抑制劑
英文別名	PLpro inhibitor,1093070-14-4
CAS號	1093070-14-4
Inchi	InChI=1S/C22H22N2O2/c1-14-11-12-18(24-16(3)25)13-21(14)22(26)23-15(2)19-10-6-8-17-7-4-5-9-20(17)19/h4-13,15H,1-3H3,(H,23,26)(H,24,25)/t15-/m1/s1
InchiKey	KGPYBLOBHQLIET-OAHLLOKOSA-N
分子式 Formula	C22H22N2O2
分子量 Molecular Weight	346.42
溶解度Solubility	生物體外In Vitro:DMSO溶解度≥ 42 mg/mL(121.24 mM)*"≥" means soluble可溶, but saturation unknown溶解度未知.
性狀	白色至灰白色固體粉末
儲藏條件 Storage conditions	在-20°C條件下保存3年,在4°C條件下保存2年

PLpro inhibitor(1093070-14-4)實驗注意事項：
1.實驗前需戴好防護眼鏡，穿戴防護服和口罩，佩戴手套，避免與皮膚接觸。
2.實驗過程中如遇到有毒或者刺激性物質(zhì)及有害物質(zhì)產(chǎn)生，必要時實驗操作需要手套箱內(nèi)完成以免對實驗人員造成傷害
3.實驗后產(chǎn)生的廢棄物需分類存儲，并交于專業(yè)生物廢氣物處理公司處理，以免造成環(huán)境污染

PLpro inhibitor(1093070-14-4) Experimental considerations:
1. Wear protective glasses, protective clothing and masks, gloves, and avoid contact with the skin during the experiment.
2. The waste generated after the experiment needs to be stored separately, and handed over to a professional biological waste gas treatment company to avoid environmental pollution.

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產(chǎn)品說明	PLpro inhibitor(1093070-14-4)是一種有效的木瓜蛋白酶樣蛋白酶（PLpro）抑制劑，PLpro抑制劑具有顯著的抗病毒活性。
Introduction	PLpro inhibitor (1093070-14-4) is a potent papain-like protease (PLpro) inhibitor, PLpro inhibitor has significant antiviral activity.
Application1
Application2
Application3

PLpro inhibitor is a potent inhibitor against the papain-like protease (PLpro) from the coronavirus that causes severe acute respiratory syndrome (SARS-CoV). PLpro inhibitor was found to have IC50 value of 2.6 μM. PLpro inhibitor display significant antiviral activity with EC50 values of 13.1 μM, without toxicity up to the highest concentration tested. Notably, the increasing antiviral potency correlates with the in vitro inhibition of PLpro, suggesting that the compounds work directly on the enzyme in cells.

警示圖
危險性	warning
危險性警示	Not available
安全聲明	H303吞入可能有害+H313皮膚接觸可能有害+H2413吸入可能對身體有害
安全防護	P264處理后徹底清洗+P280戴防護手套/穿防護服/戴防護眼罩/戴防護面具+P305如果進入眼睛+P351用水小心沖洗幾分鐘+P338取出隱形眼鏡（如果有）并且易于操作,繼續(xù)沖洗+P337如果眼睛刺激持續(xù)+P2393獲得醫(yī)療建議/護理
備注	實驗過程中防止吸入、食入，做好安全防護

Inhibitor recognition specificity of MERS-CoV papain-like protease may differ from that of SARS-CoV.
Lee H1, Lei H1, Santarsiero BD1, Gatuz JL1, Cao S1, Rice AJ1, Patel K1, Szypulinski MZ1, Ojeda I, Ghosh AK2, Johnson ME1. ACS Chem Biol. 2015 Jun 19;10(6):1456-65. doi: 10.1021/cb500917m. Epub 2015 Mar 16.
The Middle East Respiratory Syndrome coronavirus (MERS-CoV) papain-like protease (PLpro) blocking loop 2 (BL2) structure differs significantly from that of SARS-CoV PLpro, where it has been proven to play a crucial role in SARS-CoV PLpro inhibitor binding. Four SARS-CoV PLpro lead inhibitors were tested against MERS-CoV PLpro, none of which were effective against MERS-CoV PLpro. Structure and sequence alignments revealed that two residues, Y269 and Q270, responsible for inhibitor binding to SARS-CoV PLpro, were replaced by T274 and A275 in MERS-CoV PLpro, making critical binding interactions difficult to form for similar types of inhibitors. High-throughput screening (HTS) of 25?000 compounds against both PLpro enzymes identified a small fragment-like noncovalent dual inhibitor. Mode of inhibition studies by enzyme kinetics and competition surface plasmon resonance (SPR) analyses suggested that this compound acts as a competitive inhibitor with an IC50 of 6 μM against MERS-CoV PLpro, indicating that it binds to the active site, whereas it acts as an allosteric inhibitor against SARS-CoV PLpro with an IC50 of 11 μM.

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MSDS

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SDS 1.0 英文

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