您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > KT5720
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
KT5720
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。
KT5720图片
CAS NO:108068-98-0
包装与价格:
包装价格(元)
50 μg电议
100 μg电议

产品介绍
KT5720 是一种能透过细胞的、强效的、特异性的、可逆的以及 ATP 竞争性的PKA抑制剂 (IC50=3.3 μM)。KT5720 能有效逆转 MDR1 介导的多药耐药性。KT5720 还可通过减弱超极化激活环核苷酸门控阳离子 (HCN) 通道活性和减少细胞内 Ca2+浓度来降低背根神经节 (DRG) 神经元的兴奋性。KT5720 可用于血液恶性肿瘤以及 HCN 和 DRG 神经元相关疾病的研究。
生物活性

KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitivePKAinhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2+concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases[1][2][3].

IC50& Target

IC50: 11 nM (PHK); 300 nM (PDK1); 3.3 μM (PKA)[3].

体外研究
(In Vitro)

KT5720 (0-8 μM; 72 h) reverses multidrug resistance in an MDR1 lymphoma cell model[1].
KT5720 (3 μM) attenuates Ihin freshly isolated rat DRG neurons and slows down HCN channel activation kinetics[2].
KT5720 (3 μM) reduces DRG neurons excitability and reduces DRG neuron intracellular Ca2+level[2].

Cell Viability Assay[1]

Cell Line:LM1/MDR cells (carrying and expressing a human MDR1 transgene)
Concentration:0-8 μM
Incubation Time:72 h
Result:Increased sensitivity of LM1/MDR cells to colchicine in a dose-dependent manner.
体内研究
(In Vivo)

KT5720 (5 mg/kg; i.p.; single daily for 8 days) reverses completely DNR resistance in MDR1 transgenic mice model[1].

Animal Model:MDR1 transgenic mice model[1].
Dosage:5 mg/kg
Administration:Intraperitoneal injection; single daily for 8 days
Result:Exhibited the leukopenia induced by daunorubicin in the MDR mice was equivalent to that measured in non-MDR mice treated with daunorubicin alone.
分子量

537.61

性状

Solid

Formula

C32H31N3O5

CAS 号

108068-98-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

Methanol : 5 mg/mL(9.30 mM;Need ultrasonic and warming)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8601 mL9.3004 mL18.6008 mL
5 mM0.3720 mL1.8601 mL3.7202 mL
10 mM---------
*

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。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。