KT5720

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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。

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 I_hin 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°C	3 years
In solvent	-80°C	6 months
	-20°C	1 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 mg

5 mg

10 mg

1 mM	1.8601 mL	9.3004 mL	18.6008 mL
5 mM	0.3720 mL	1.8601 mL	3.7202 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。