Sp-5,6-dichloro-cBIMPS (sodium salt)
(Synonyms: Sp-5,6-DCI-cBIMPS) 目录号 : GC10428A selective PKA activator
Cas No.:142439-96-1
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ki: 30 nM
Sp-5,6-dichloro-cBIMPS is a PKA activator.
In cell biology, protein kinase A (PKA) is a family of enzymes whose activity is dependent on cellular levels of cyclic AMP. PKA is also known as cAMP-dependent protein kinase. PKA has several functions in the cell, such as regulation of sugar, glycogen, and lipid metabolism.
In vitro: Sp-5,6-dichloro-cBIMPS was found to be both a potent and specific activator of purified cAMP-PK and of cAMP-PK in platelet membranes, whereas 8-pCPT-cAMP proved to be a potent activator of cAMP-PK and cyclic-GMP-dependent protein kinase both as purified enzymes and in platelet membranes. Moreover, it was found that Sp-5,6-dichloro-cBIMPS was not significantly hydrolysed by three types of cyclic nucleotide phosphodiesterases, whereas 8-pCPT-cAMP was hydrolysed to a significant extent by the Ca2+/calmodulin-dependent phosphodiesterase and by the cGMP-inhibited phosphodiesterase. The apparent lipophilicity of Sp-5,6-dichloro-cBIMPS was higher than that of 8-pCPT-cAMP. Extracellular application of Sp-5,6-dichloro-cBIMPS to intact human platelets could reproduce the pattern of protein phosphorylation that was induced by prostaglandin E1. Additionally, in intact platelets, Sp-5,6-dichloro-cBIMPS was also more effective than 8-pCPT-cAMP in inducing quantitative phosphorylation of vasodilator-stimulated phosphoprotein, a major substrate of cAMP-PK in platelets. As demonstrated by prostaglandin E1, pretreatment of human platelets with Sp-5,6-DCl-cBiMPS Sp-5,6-dichloro-cBIMPS was able to prevent the aggregation induced by thrombin [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Sandberg, M. ,Butt, E.,Nolte, C., et al. Characterization of Sp-5,6-dichloro-1-β-D-ribofuranosylbenzimidazole-3',5'-monophosphorothioate (Sp-5,6-DCl-cBiMPS) as a potent and specific activator of cyclic-AMP-dependent protein kinase in cell extracts and intact cells. Biochemistry Journal 279, 521-527 (1991).
Cas No. | 142439-96-1 | SDF | |
别名 | Sp-5,6-DCI-cBIMPS | ||
化学名 | 5,6-dichloro-1-[3,5-O-[(S)-mercaptophosphinylidene]-β-D-ribofuranosyl]-1H-benzimidazole, monosodium salt | ||
Canonical SMILES | [S-][P@]1(OC[C@]2([H])[C@@]([C@@H](O)[C@H](N3C(C=C(Cl)C(Cl)=C4)=C4N=C3)O2)([H])O1)=O.[Na+] | ||
分子式 | C12H10Cl2N2O5PS • Na | 分子量 | 419.1 |
溶解度 | ≤167mg/ml in ethanol;167mg/ml in DMSO;167mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
General tips | 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°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.3861 mL | 11.9303 mL | 23.8607 mL |
5 mM | 0.4772 mL | 2.3861 mL | 4.7721 mL |
10 mM | 0.2386 mL | 1.193 mL | 2.3861 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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