SQ 22536
(Synonyms: 9-(四氢-2-呋喃)腺膘呤) 目录号 : GC13867
SQ 22536是一种有效的腺苷酸环化酶（AC）抑制剂。
Cas No.:17318-31-9
Sample solution is provided at 25 µL, 10mM.
SQ 22536 is a potent adenylate cyclase (AC) inhibitor[1]. SQ 22536 can be widely used in various studies to elucidate the role of cAMP signaling pathways in many physiological and pathological processes[2, 3]. SQ 22536 can block dopamine-induced decreases in cyclin E, cyclin-dependent protein kinase-2 (CDK-2), cyclin D1, and CDK-4[4].
In vitro, treatment of human acute myeloid leukemia (AML) KG-1 cells with SQ 22536 (100µM) for 24h reversed the inhibitory effects of polydatin on KG-1 cell proliferation, migration, and invasion[5]. Pretreatment of Schwann cells with SQ 22536 (100µM) for 1h abolished the calcitonin gene-related peptide (CGRP)-mediated increase in IL-1β[6].
In vivo, SQ 22536 (1nmol/kg) was injected intraperitoneally to treat epilepsy model mice. The use of SQ 22536 alone or in combination with dipyridamole or BRL50481 significantly improved the anticonvulsant activity, with the protection rates increasing by 83.3%, 66.7% and 50%, respectively[7].
References:
[1] Emery A C, Eiden M V, Eiden L E. A new site and mechanism of action for the widely used adenylate cyclase inhibitor SQ22,536[J]. Molecular pharmacology, 2013, 83(1): 95-105.
[2] Alasbahi R H, Melzig M F. Forskolin and derivatives as tools for studying the role of cAMP[J]. Die Pharmazie-An International Journal of Pharmaceutical Sciences, 2012, 67(1): 5-13.
[3] Khan H, Tiwari C, Grewal A K, et al. Pharmacological modulation of phosphodiesterase-7 as a novel strategy for neurodegenerative disorders[J]. Inflammopharmacology, 2022, 30(6): 2051-2061.
[4] Lee M Y, Heo J S, Han H J. Dopamine regulates cell cycle regulatory proteins via cAMP, Ca2+/PKC, MAPKs, and NF‐κB in mouse embryonic stem cells[J]. Journal of cellular physiology, 2006, 208(2): 399-406.
[5] Min H U A, Weili Z. Effects of polydatin on the cell proliferation, migration, invasion and tumor growth of AML[J]. China Pharmacy, 2024, 35(6): 701-706.
[6] Permpoonputtana K, Porter J E, Govitrapong P. Calcitonin gene-related peptide mediates an inflammatory response in Schwann cells via cAMP-dependent ERK signaling cascade[J]. Life sciences, 2016, 144: 19-25.
[7] Nandhakumar J, Tyagi M G. Evaluation of seizure activity after phospho-diesterase and adenylate cyclase inhibition (SQ22536) in animal models of epilepsy[J]. Indian J Sci Technol, 2010, 3(7): 710-717.
SQ 22536是一种有效的腺苷酸环化酶（AC）抑制剂[1]。SQ 22536能够广泛用于各种研究，以阐明cAMP信号通路在许多生理和病理过程中的作用[2, 3]。SQ 22536能够阻断多巴胺诱导的细胞周期蛋白E、细胞周期蛋白依赖性蛋白激酶-2（CDK-2）和细胞周期蛋白D1、CDK-4的降低[4]。
在体外，SQ 22536（100µM）处理人急性髓系白血病（AML）KG-1细胞24h，逆转了虎杖苷（polydatin）对KG-1细胞增殖、迁移、侵袭的抑制作用[5]。SQ 22536（100µM）预处理Schwann细胞1h，消除了降钙素基因相关肽（CGRP）介导的IL-1β增加[6]。
在体内，SQ 22536（1nmol/kg）通过腹腔注射治疗癫痫模型小鼠，单独使用SQ 22536、SQ 22536与dipyridamole或BRL50481联合使用均大大提高了抗惊厥活性，保护率分别提高了83.3%、66.7%和50%[7]。
| Cell experiment [1]: | |
Cell lines | Human acute myeloid leukemia (AML) cell KG-1 |
Preparation Method | Human acute myeloid leukemia (AML) cell KG-1 were divided into normal group, polydatin (PD) low-, medium- and high-concentration groups (10, 30, 60μM PD), SQ 22536 group (100μM), high concentration of PD+SQ 22536 group (60μM PD+100μM SQ 22536). The cells were cultured for 24h. The effects of PD on cell activity, apoptotic rate, invasion and migration ability, cAMP level, the expression of epithelial-mesenchymal transition (EMT) related proteins and protein kinase A (PKA) were investigated. |
Reaction Conditions | 100µM; 24h |
Applications | SQ 22536 has the opposite effect on cells as PD and can significantly reverse the anti-tumor activity of PD. |
| Animal experiment [2]: | |
Animal models | Swice Albino mice |
Preparation Method | Pentylenetetrazole (PTZ) or metrazol (MTZ) induced seizure model in mice. Swice Albino mice were divided into 7 groups with six animals (n=6) in each. Treatment protocol and group description is mentioned as follows: Group - I : Mice served as solvent control, received 10% w/v of DMSO (5ml/kg, i.p). Group - II : Mice received gabapentin (2.5mg/kg, i.p) treated as positive control. Group- III : Mice received SQ 22536 (1nmol/kg, i.p) an adenylate cyclase inhibitor. Group -IV : Mice received dipyridamole (2mg/kg, i.p) a PDE-5/6/8/10/11 Inhibitor. Group -V : Mice received BRL50481 (2mg/kg, i.p) a PDE-7 inhibitor. Group-VI : Mice received SQ 22536 (1nmol/kg, i.p) along with dipyridamole (2mg/kg, i.p) combination of adenylate cyclase inhibitor and PDE-5/6/8/10/11 inhibitor. Group-VII: Mice received SQ 22536 (1nmol/kg, i.p) along with BRL50481 (2mg/kg, i.p) combination of adenylate cyclase inhibitor and PDE-7 inhibitor. All the drugs were administered intraperitoneally 30min prior to the administration of pentylenetetrazole (60mg/kg, i.p). The animals were observed for 1h by placing in a separate cage. The onset time of various phases of convulsions like action, jerky movement, convulsions and recovery/mortality. |
Dosage form | 1nmol/kg; i.p. |
Applications | SQ 22536 alone, SQ 22536 followed by dipyridamole and SQ 22536 with BRL50481 greatly increased the anticonvulsant activity (P<0.01, P<0.05 and P<0.01) along with higher protection 83.3%, 66.7% and 50% range respectively. |
References: | |
| Cas No. | 17318-31-9 | SDF | |
| 别名 | 9-(四氢-2-呋喃)腺膘呤 | ||
| 化学名 | (R)-9-(tetrahydrofuran-2-yl)-9H-purin-6-amine | ||
| Canonical SMILES | NC(N=CN=C12)=C2N=CN1[C@@H]3OCCC3 | ||
| 分子式 | C9H11N5O | 分子量 | 205.22 |
| 溶解度 | ≥ 20.5mg/mL in DMSO | 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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.8728 mL | 24.3641 mL | 48.7282 mL |
| 5 mM | 974.6 μL | 4.8728 mL | 9.7456 mL |
| 10 mM | 487.3 μL | 2.4364 mL | 4.8728 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
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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- Purity: >98.00%
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