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12

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8452	Dantrolene	Others	Others
	Dantrolene 是一种肌肉松弛剂，是人红细胞谷胱甘肽还原酶的非竞争性抑制剂，其Ki 和IC50值分别为 111.6 μM 和 52.3 μM。它是兰尼碱受体拮抗剂及Ca2+信号稳定剂。它可用于研究恶性高热、亨廷顿病、肌肉痉挛和其他神经阻滞剂恶性综合征。
T8815	Azumolene 阿珠莫林,EU4093 free base	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Azumolene (EU4093 free base) 是一种 Dantrolene 的类似物，是一种肌肉松弛剂，可用于恶性高热研究。它是一种 ryanodine 受体调节剂，并通过 ryanodine 受体抑制钙释放。
T60127	Chlorantraniliprole Rynaxypyr,Chlorantranilipole,Rynaxpyr	Others	Others
	Chlorantraniliprole (Rynaxypyr) 是一种杀虫剂，能够有效地、选择性地激活鱼尼丁受体 (ryanodine receptor)，对黑腹果蝇和烟芽夜蛾的 ryanodine 受体 EC50 值分别为 40 nM 和 50 nM，对其选择性是对小鼠骨骼肌 2C12 细胞 ryanodine 受体 (EC50，14 μM) 的 300 多倍。
T37807	JTV 519 fumarate
	Ryanodine receptor (RyR) inhibitor; stabilizes RyR2 in a closed conformation. Exhibits antiarrhythmic and cardioprotective properties in vivo. Hunt et al (2007) K201 (JTV519) suppresses spontaneous Ca2+ release and [3H]ryanodine binding to RyR2 irrespective of FKBP12.6 association. Biochem.J. 404 431 PMID:17313373 \|Chen et al (2008) Effect of K201, a novel antiarrhythmic drug on calcium handling and arrhythmogenic activity of pulmonary vein cardiomyocytes. Br.J.Pharmacol. 153 915 PMID:17994112 \|...
T4054	Dantrolene sodium hemiheptahydrate Dantrolene sodium hydrate,Dantrolene sodium salt,Dantrium,丹曲林钠五水合物,Sodium dantrolene	Calcium Channel; Autophagy	Autophagy; Membrane transporter/Ion channel; Metabolism
	Dantrolene sodium hemiheptahydrate (Sodium dantrolene) 是一种钙通道蛋白抑制剂, 抑制钙离子从肌浆释放, 它是一种乙内酰脲衍生物和直接作用的骨骼肌松弛剂。
T32855	Lomifylline Cervilane
	Lomifylline is an inducer that induces the release of Ca2+ stored in cells, specifically through the ryanodine receptor.
T72004	Azumolene sodium anhydrous
	Azumolene sodium anhydrous is a muscle relaxant that inhibits the release of calcium from skeletal muscle sarcoplasmic reticulum. Azumolene inhibits a component of store-operated calcium entry coupled to the skeletal muscle ryanodine receptor. Azumolene, an equipotent dantrolene analog, inhibits a component of SOCE coupled to activation of RyR1 by caffeine and ryanodine, whereas the SOCE component induced by thapsigargin is not affected.
T68366	Azumolene sodium dihydrate
	Azumolene sodium dihydrate is a muscle relaxant that inhibits the release of calcium from skeletal muscle sarcoplasmic reticulum. Azumolene inhibits a component of store-operated calcium entry coupled to the skeletal muscle ryanodine receptor.
T80153	Maurocalcine	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Maurocalcine是一种能穿透细胞膜的激动剂，对ryanodine receptor (RyR)通道1、2、3型具有活性。在与RyR1的结合实验中，Maurocalcine诱导[3H]ryanodine的结合，表现出EC50值为2558 nM。此外，Maurocalcine对RyR2也展示出较高的表观亲和力，达14 nM。该化合物可用于体内细胞追踪及其他细胞成像技术。
T81237	RyRs activator 4
	RyRs activator 4为一款昆虫兰尼碱受体激活剂，对粘虫幼虫显示出显著的杀灭活性，其半致死浓度(LC50)为1.32 mg/L。
T79703	RyRs activator 3	Parasite	Microbiology/Virology
	RyRs activator 3 (compound A4) 作为有效杀虫剂，针对斑小菜蛾 (M. separata) 及小菜蛾 (P. xylostella) 显示出较高效力，其对斑小菜蛾的 LC50 值达到 3.27 mg/L。通过与兰尼碱受体 (ryanodine receptor) 结合，RyRs activator 3 能增加细胞质中 Ca2+ 的浓度，从而产生生物毒性。
T80975	TMDJ-035	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	TMDJ-035为选择性RyR2抑制剂。该化合物能够抑制携带ryr2突变的小鼠心肌细胞中异常的Ca2+波动和瞬态现象。作为研究RyR2通道开闭机制及其动力学的实验工具，TMDJ-035的应用十分关键。

化合物

Cat.No: T8452

Target: Others

Cat.No: T8815

Synonym: 阿珠莫林,EU4093 free base

Target: Calcium Channel

Chlorantraniliprole

Cat.No: T60127

Synonym: Rynaxypyr,Chlorantranilipole,Rynaxpyr

Target: Others

JTV 519 fumarate

Cat.No: T37807

Dantrolene sodium hemiheptahydrate

Cat.No: T4054

Synonym: Dantrolene sodium hydrate,Dantrolene sodium salt,Dantrium,丹曲林钠五水合物,Sodium dantrolene

Target: Calcium Channel, Autophagy

Cat.No: T32855

Synonym: Cervilane

Azumolene sodium anhydrous

Cat.No: T72004

Azumolene sodium dihydrate

Cat.No: T68366

Cat.No: T80153

Target: Calcium Channel

RyRs activator 4

Cat.No: T81237

RyRs activator 3

Cat.No: T79703

Target: Parasite

Cat.No: T80975

Target: Calcium Channel

Cat. No.	Product Name	Target	Signaling Pathways
T4973	Paraxanthine 1,7-二甲基黄嘌呤,1,7-DIMETHYLXANTHINE	Endogenous Metabolite	Metabolism
	Paraxanthine (1,7-dimethylxanthine) 是一种 caffeine 的代谢物，能够刺激Ryanodine 受体通道来抑制多巴胺能细胞的死亡。
T12787	Ryanodine	Others	Others
	Ryanodine, a diterpenoid poison derived from Ryania speciosa, acts as a modulator of the ryanodine receptor, which is permeable to cells. Depending on its concentration, ryanodine can either stimulate or inhibit Ca2+ release mediated by these receptors.
T19253	Cyclic ADP-ribose cADPR	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Cyclic ADP-ribose (cADPR) is an effective calcium mobilization second messenger, which is synthesized from NAD + by ADP-ribosyl cyclase. Cyclic ADP-ribose mainly increases cytosolic calcium through Ryanodine receptor-mediated endoplasmic reticulum release
T37687	Cyclic ADP-ribose ammonium
	Cyclic ADP-ribose ammonium (cADPR ammonium) is a powerful calcium mobilization second messenger synthesized from NAD+ by an ADP-ribosyl cyclase. It primarily raises cytosolic calcium levels through Ryanodine receptor-mediated release from the endoplasmic reticulum, while also facilitating extracellular influx through the opening of TRPM2 channels [1][2][3].

天然产物

Cat.No: T4973

Synonym: 1,7-二甲基黄嘌呤,1,7-DIMETHYLXANTHINE

Target: Endogenous Metabolite

Cat.No: T12787

Target: Others

Cyclic ADP-ribose

Cat.No: T19253

Synonym: cADPR

Target: Calcium Channel

Cyclic ADP-ribose ammonium

Cat.No: T37687

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