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首页 / 抑制剂/激动剂 / G蛋白偶联受体/G蛋白 / cAMP / KH7

KH7 {[allProObj[0].p_purity_real_show]}

货号：A957502 同义名： KH 7 free

KH7是可溶性腺苷酸环化酶（sAC）的特异性抑制剂，在细胞中对重组sACt蛋白（人类和其他物种）的IC50为3-10 μM。KH7也是cAMP的抑制剂。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
KH7 化学结构 CAS号：330676-02-3
KH7 化学结构
CAS号：330676-02-3
KH7 3D分子结构
CAS号：330676-02-3
KH7 化学结构 CAS号：330676-02-3
KH7 3D分子结构 CAS号：330676-02-3
规格 价格 会员价 库存 数量
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KH7 纯度/质量文件 产品仅供科研

货号：A957502 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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产品名称 AC ↓ EPAC1 ↓ EPAC2 ↓ PACAP receptor ↓ 其他靶点 纯度
Bithionol +

sAC, IC50: 4.0 μM

 		98%
SQ22536 ✔ 99%+
ESI-09 ++

EPAC1, IC50: 3.2 μM

 		+++

EPAC2, IC50: 1.4 μM

 		98%
HJC0350 +++

EPAC2, IC50: 0.3 μM

 		99%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

KH7 生物活性

描述 Soluble adenylate cyclase (sAC) is a non-plasma membrane bound form of adenylate cyclase (AC) that produces the second messenger adenosine 3’,5’-cyclic AMP (cAMP) from ATP. It has been suggested to be involved in various cellular and physiological processes. KH 7, working as a classical uncoupler, is a sAC-specific inhibitor with an IC50 of 2.7 μM. KH 7 at 25 μM inhibited ATP production by reducing respiration at lower concentrations and by perturbing membrane potential at higher concentrations in isolated mouse liver mitochondria[2]. Application of the KH 7 showed almost complete inhibition of ATP-induced [Ca2+]i elevation in pretreated EA.hy926 cells indicating it reduces intracellular Ca2+ response[3]. In vivo, KH 7 (1.25 mM dissolved in 4 mL/kg DMSO) treatment caused an increased IOP (intraocular pressure) in avertin- and KXA(ketamine/xylazine/acepromazine)-anesthetized C57BL/6J mice compared with DMSO controls. In mice, KH 7 (5 μM) decreased outflow facility by 85.1% in nonanesthetized, enucleated eyes[4].

KH7 细胞实验

Cell Line
Concentration Treated Time Description References
NHBE cells 50 μM To test the inhibitory effect of KH7 on sAC activity Am J Respir Cell Mol Biol. 2014 Dec;51(6):750-60.
Islet β-cells 30 μmol/L KH7 inhibited glucose-induced [cAMP]pm oscillations Diabetes. 2011 May;60(5):1535-43.
MIN6 β-cells 30 μmol/L KH7 inhibited glucose-induced [cAMP]pm oscillations Diabetes. 2011 May;60(5):1535-43.
PBMCs 25 μM 30 minutes Minimal effect on basal cAMP levels J Nutr Biochem. 2011 Jul;22(7):681-90.
HEK293T cells 50 μM 48 hours To test the inhibitory effect of KH7 on sAC activity Am J Respir Cell Mol Biol. 2014 Dec;51(6):750-60.
Primary mouse cholangiocytes 100 μM 3 hours KH7 treatment also prevented NaGCDC-induced apoptosis in primary mouse cholangiocytes. Hepatology. 2016 Aug;64(2):522-34.
H69 human cholangiocytes 50-100 μM 1 hour KH7 dose-dependently inhibited BSIA in both control and AE2 knockdown cholangiocytes and at higher concentrations also prevented NaCDC-induced apoptosis altogether. Hepatology. 2016 Aug;64(2):522-34.
HEK293 cells 50 μM KH7 inhibited the pH recovery rate in sAC-overexpressing HEK293 cells Invest Ophthalmol Vis Sci. 2014 Jan 9;55(1):187-97.
Nonpigmented ciliary epithelial cells (NPE) 50 μM 2 minutes KH7 significantly reduced the acetazolamide-induced increase in cAMP Invest Ophthalmol Vis Sci. 2014 Jan 9;55(1):187-97.
MLTC-1 cells 6.25, 12.5, 50, 100 µM 1 hour KH7 dose-dependently inhibited LH-stimulated cAMP accumulation, with 100 µM concentration almost completely abolishing cAMP accumulation Int J Mol Sci. 2021 Apr 28;22(9):4641.
Cardiac fibers 5 μM 30 minutes KH7, a soluble adenylyl cyclase inhibitor, reduced ADP-stimulated respiratory rates Int J Mol Sci. 2016 Dec 10;17(12):2075.
PBMCs 10 or 25 μM 30 minutes Inhibition of sAC activity, reduction in cAMP levels J Nutr Biochem. 2011 Jul;22(7):681-90.
Ciona intestinalis sperm 10 μM 3 min Investigate the effect of KH-7 on sperm motility and trajectory, results showed KH-7 significantly reduced swimming velocity and decreased the diameter of sperm trajectory. Int J Mol Sci. 2014 Jul 28;15(8):13192-208.
Human endometrial epithelial cell line (ISK) 10 µM 24 hours KH-7, a selective inhibitor of soluble adenylyl cyclase (sAC), was used to investigate the effect of ENaC knockdown or Ca2+ chelation on CFTR upregulation. Results showed that KH-7 completely reversed the CFTR mRNA increase induced by low-degree ENaC knockdown or BAPTA-AM, suggesting the involvement of sAC-driven cAMP production in the regulation of CFTR. Front Cell Dev Biol. 2022 Aug 30;10:781762.

KH7 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice SAC C2KO mice Perfusion 25 μM To test the regulatory effect of KH7 on CBF Am J Respir Cell Mol Biol. 2014 Dec;51(6):750-60.
Male DBA/1 J mice Collagen-induced arthritis (CIA) mouse model Intraperitoneal injection 6 mg/kg Three times a week for 6 weeks To evaluate the inhibitory effect of KH7-33 mAb on arthritic symptoms. Results showed that KH7-33 mAb significantly ameliorated the arthritis index, squeaking index, and paw volume. Arthritis Res Ther. 2018 Oct 30;20(1):245

KH7 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00035490 Arrhythmia Phase 3 Completed - -
NCT03127059 Dysfunctional Breathing in Ast... 展开 >>hma 收起 << Not Applicable Recruiting November 2020 Denmark ... 展开 >> Dep. of Physiotherapy and Dep. of Pulmonology Recruiting Silkeborg, Central Denmark Region, Denmark, 8600 Contact: Karen H Andreasson       khad@regionsjaelland.dk    Dep. of Physiotherapy and Dep. of Pulmonology Recruiting Bispebjerg, Danish Capital Region, Denmark Contact: Karen H Andreasson       khad@regionsjaelland.dk    Allergi og Lungeklinikken Helsingør Recruiting Helsingør, Danish Capital Region, Denmark, 3000 Contact: Karen H Andreasson       khad@regionsjaelland.dk    Dep. of Physiotherapy and Dep. of Pulmonology Recruiting Hvidovre, Danish Capital Region, Denmark Contact: Karen H Andreasson       khad@regionsjaelland.dk    Dep. of Physiotherapy and Dep. of Pulmonology Recruiting Aalborg, Region North, Denmark Contact: Karen H Andreasson       khad@regionsjaelland.dk    Dep. of Physiotherapy and Dep. of Pulmonology Recruiting Naestved, Region Zealand, Denmark Contact: Karen H Andreasson, PT MSc    +45 24 25 49 26    khad@regionsjaelland.dk    Contact: Uffe Bødtger, MD PhD    +45 56 51 45 92    ubt@regionsjaelland.dk    Dep. of Physiotherapy and Dep. of Pulmonology Recruiting Roskilde, Region Zealand, Denmark Contact: Karen H Andreasson       khad@regionsjaelland.dk 收起 <<
NCT03616912 Systemic Lupus Erythematosus Phase 3 Recruiting February 16, 2021 -

KH7 参考文献

[2]Jakobsen E, et al. The inhibitors of soluble adenylate cyclase 2-OHE, KH7, and bithionol compromise mitochondrial ATP production by distinct mechanisms. Biochem Pharmacol. 2018 Sep;155:92-101

[3]Mewes M, et al. Soluble adenylyl cyclase (sAC) regulates calcium signaling in the vascular endothelium. FASEB J. 2019 Dec;33(12):13762-13774

[4]Gandhi JK, et al. Differential Intraocular Pressure Measurements by Tonometry and Direct Cannulation After Treatment with Soluble Adenylyl Cyclase Inhibitors. J Ocul Pharmacol Ther. 2017 Oct;33(8):574-581

KH7 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.38mL

0.48mL

0.24mL

11.92mL

2.38mL

1.19mL

23.85mL

4.77mL

2.38mL

KH7 技术信息

CAS号330676-02-3
分子式C17H15BrN4O2S
分子量 419.3
SMILES Code OC(C=CC(Br)=C2)=C2/C=N/NC(C(C)SC1=NC(C=CC=C3)=C3N1)=O
MDL No. MFCD01230899
别名 KH 7 free
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C
溶解方案

DMSO: 250 mg/mL(596.24 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: KH7 | 330676-02-3 | KH 7 | KH-7 | Soluble Adenylyl Cyclase Inhibitor | GPCR/G Protein | Adenylate Cyclase | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | KH7 纯度/质量文件 | KH7 亚型比较 | KH7 生物活性 | KH7 临床数据 | KH7 参考文献 | KH7 实验方案 | KH7 技术信息

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