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SQ 22536 Sale

(Synonyms: 9-(四氢-2-呋喃)腺膘呤) 目录号 : GC13867

An adenylyl cyclase inhibitor

SQ 22536 Chemical Structure

Cas No.:17318-31-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥368.00
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10mg
¥630.00
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50mg
¥2,436.00
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Sample solution is provided at 25 µL, 10mM.

Description

SQ22536 is an effective adenylate cyclase (AC) inhibitor.
SQ22536 (SQ22,536) effectively inhibits the effect of forskolin with respective IC50 values of 5 μM.Preincubation with graded concentrations of SQ22536 reveals that both SQ22536 effectively inhibits PACAP-induced reporter gene activation with approximate IC50 value of 5 μM. SQ22536 more potently inhibits forskolin-induced Elk activation (IC50=10 μM) than 8-Br-cAMP-induced Elk activation (IC50=170 μM). Most notably, there are substantial differences in the reported potencies of SQ22536 to inhibit the activities of recombinant AC5 and AC6, with respective IC50 values of 2 μM and 360 μM. At a greater concentration (500 μM), SQ22536 significantly inhibits neurite elongation due to either forskolin or 8-Br-cAMP[1].
Reference:
[1]. Emery AC, et al. A new site and mechanism of action for the widely used adenylate cyclase inhibitor SQ22,536. Mol Pharmacol. 2013 Jan;83(1):95-105.

实验参考方法

Cell experiment:

HEK293 CRE-luc2P GloResponse luciferase reporter cells are transduced with retroviral vectors expressing rat PAC1hop receptors. Individual cell lines are obtained by limiting dilution cloning, and a clonal PAC1-expressing line is propagated and used for CRE luciferase assays. In brief, HEK293 CRE-luc2P cells are plated in 96-well plates (10,000 cells in 80 μL media per well) in assay media (DMEM supplemented with 1% fetal bovine serum). One day after plating, cells are treated with AC inhibitors (10 μL in assay media/well) for 30 minutes, followed by agonists (10 μL in assay media/well), and are incubated for 4 hours. Luciferase activity is determined after the addition of 100 μL/well Bright-Glo Luciferase Assay Reagent. Luminescence (RLU) is measured in a Victor3 microtiter plate reader after 2 minutes of agitation at room temperature. Cyclic AMP is measured in NS-1 cells. In brief, NS-1 cells are seeded and grown overnight in 96-well plates. The next day, cells are pretreated for 20 minutes in media containing the phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine (0.5 mM) with or without SQ22536. After pretreatment with inhibitors, cells are stimulated with agonists, added as 10× solutions, for an additional 20 minutes. Intracellular cAMP is then assayed using the cAMP Biotrak enzyme immunoassay kit for measurement of nonacetylated cAMP[1].

References:

[1]. Emery AC, et al. A new site and mechanism of action for the widely used adenylate cyclase inhibitor SQ22,536. Mol Pharmacol. 2013 Jan;83(1):95-105.

化学性质

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
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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。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 4.8728 mL 24.3641 mL 48.7282 mL
5 mM 0.9746 mL 4.8728 mL 9.7456 mL
10 mM 0.4873 mL 2.4364 mL 4.8728 mL
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