(R)?-?CR8

CAS号

294646-77-8

分子式

C24H29N7O

主要靶点

CDK|Apoptosis

仅限科研使用

Cat No : CM03353

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Synonyms

Isomer|lesion|caspases|cell|cdk2/cyclin A|CDK2/cyclinE|CDK7/cyclin H|Cdk5/p25|CDK9/Cyclin T|CK1δ/ε|Cdk1/cyclin B|CDK|Apoptosis|(R)-Isomer|(R)?-?CR8|(R)??CR8|(R)?-?CR-8|(R)? ?CR8|CR 8|CR8, (R)-Isomer|CR-8|CR8|death|Hippocampus



产品信息

CAS号 294646-77-8
分子式 C24H29N7O
主要靶点 CDK|Apoptosis
主要通路 细胞周期|凋亡
分子量 431.53
纯度 98.41%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Isomer|lesion|caspases|cell|cdk2/cyclin A|CDK2/cyclinE|CDK7/cyclin H|Cdk5/p25|CDK9/Cyclin T|CK1δ/ε|Cdk1/cyclin B|CDK|Apoptosis|(R)-Isomer|(R)?-?CR8|(R)??CR8|(R)?-?CR-8|(R)? ?CR8|CR 8|CR8, (R)-Isomer|CR-8|CR8|death|Hippocampus

靶点活性

CK1δ/ε:0.4 μM|CDK1-CyclinB:0.09 μM|CDK7-CyclinH:1.1 μM|CDK9-CyclinT:0.18 μM|CDK5-p25:0.11 μM|CDK2-CyclinA:0.072 μM|CDK2-CyclinE:0.041 μM

体内活性

在系统性后LFP 3小时给药的条件下,强效的第二代细胞周期依赖性激酶(CDK)抑制剂CR8能够减少CCA以及皮层、海马和丘脑的神经元损失,并且减轻了皮层微胶质和星形胶质细胞的激活。此外,CR8治疗减轻了感觉运动和认知障碍,缓解了类似抑郁的症状,并且减小了病变体积[1]。

溶解度

DMSO:11 mg/mL (25.49 mM)

参考文献

1.Kabadi SV, et al. CR8, a novel inhibitor of CDK, limits microglial activation, astrocytosis, neuronal loss, and neurologic dysfunction after experimental traumatic brain injury. J Cereb Blood Flow Metab. 2014 Mar;34(3):502-13.
2.Bettayeb K, et al. CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases. Oncogene. 2008 Oct 2;27(44):5797-807.

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