计算溶液所需的质量、体积或浓度。
PK68
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
PK68 is a potent orally active and specifical type II inhibitor of receptor-interacting kinase 1 (RIPK1) with an IC 50 of ~90 nM, displays inhibition of RIPK1-dependent necroptosis . PK68 powerfully ameliorates TNF-induced systemic inflammatory response syndrome, and can be used for the research of inflammatory disorders and cancer metastasis
In Vitro
PK68 has highly potent inhibition of TNF-induced necroptosis with EC 50 values of 23 nM and 13 nM in human and mouse cells, respectively. PK68 is a highly selective inhibitor of RIPK1 kinase activity with IC 50 value of 90 nM. PK68 (100 nM, 1 h) blocks necroptosis through the suppression of RIPK3 function or signaling upstream of RIPK3 activation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Bone marrow-derived macrophages, NIH3T3-RIPK3 cells Concentration: 100 nM Incubation Time: 1 h Result: PK68 block cellular activation of RIPK1, RIPK3, and MLKL upon necroptotic stimuli. PK68 inhibit TNF-induced necroptosis but not RIPK3 dimerization-induced cell death in NIH3T3-RIPK3 cells. Western Blot AnalysisCell Line: HT-29 cells Concentration: 100 nM Incubation Time: 1 h Result: Completely abolished phosphorylation of RIPK1, RIPK3, and MLKL. ImmunofluorescenceCell Line: HT-29 cells Concentration: 100 nM Incubation Time: 1 h Result: Prevented generation of RIPK3 puncta.
In Vivo
PK68 (5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days) or (2 mg/kg, i.v.; 10 mg/kg, p.o.; for 14 days) exhibits a favorable pharmacokinetic profile and no obvious toxicity in mice . PK68 (1 mg/kg, i.p.) ameliorates TNF-induced systemic inflammatory response syndrome . PK68 (5 mg/kg, i.v.) inhibits RIPK1 that results in attenuated tumor cell transmigration across the endothelial barrier and preventive suppression of tumor metastasis . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6 mice Dosage: 5 mg/kg, 25 mg/kg Administration: 5 mg/kg, 25 mg/kg; oral gavage; daily; for 7 days Result: Exhibited favorable pharmacokinetic profiles and no obvious toxicity in mice treated with a 14-day course at a dose of 25 mg/kg. Animal Model: C57BL/6 mice Dosage: 2 mg/kg, 10 mg/kg Administration: 2 mg/kg, i.v.; 10 mg/kg, p.o; for 14 days Result: PO (Gavage) IV (Bolus) T max (hr) 0.5 C max (ng/mL) 2423 AUC 0-24 (ng/mL•hr) 4821 1588 AUCINF (ng/mL•hr) 4897 1590 t 1/2 (hr) 1.3 1.0 MRT (hr) 1.8 0.8 CL (mL/hr/kg) 1258 CL (mL/min/kg) 21 Vss (mL/kg) 1009 Vss (L/kg) 1.0 F(%) 61 Animal Model: C57BL/6 mice Dosage: 1 mg/kg Administration: 1 mg/kg, i.p. Result: Provided effective protection against TNFα-induced lethal shock. Animal Model: C57BL/6 mice Dosage: 5 mg/kg Administration: 5 mg/kg, i.v. Result: Significantly reduced the number of pulmonary metastasis nodules, decreased lung metastasis, decreased number of RFP-LL/2 cells, attenuated transmigration of RFP-LL/2 cells through the endothelial cell monolayer and had no obvious influence on the proliferation rate and invasion ability of B16-F10 or RFP-LL/2 cells without the endothelial cell monolayer in vitro.
IC50& Target:RIPK1 90 nM (IC 50 ) RIPK1 23 nM (EC 50 )
规格
规格或纯度
Moligand™,10mM in DMSO
英文名称
PK68
生化机理
PK68 是受体相互作用激酶 1（RIPK1）的一种强效口服活性特异性 II 型抑制剂，IC50 为 90u2009nM 左右，具有抑制 RIPK1 依赖性坏死的作用。PK68 能有效改善 TNF 诱导的全身炎症反应。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC1=C(C=C(C=N1)C2=CC3=C(C=C2)N=C(S3)NC(=O)C)NC(=O)OC4CCCCC4
PubChem CID
MeSH Entry Terms
N-(6-(2-bromoacetyl)benzo(d)thiazol-2-yl)acetamide;PK68
分子量
424.52
技术文档
高级数据
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
「Moligand?」是什么？
「Moligand?」是阿拉丁科学的高端产品线之一，专为多个工作流程中的高纯度应用而设计。与同类工作流程中的标准级别相比，「Moligand?」产品通常具有更严格的规格、更严谨的 QC 以及更强的批间一致性。
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 2173556-69-7，分子式为 C22H24N4O3S，分子量为 424.52 g/mol。
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每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
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