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KH7

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Chemical Structure| 330676-02-3 同义名 : KH 7 free
CAS号 : 330676-02-3
货号 : A957502
分子式 : C17H15BrN4O2S
纯度 : 99%+
分子量 : 419.296
MDL号 : MFCD01230899
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

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

动物实验配方:
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].
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 -
实验方案
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

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