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26

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。
T24239	K201 K-201,JTV 519,JTV-519,K 201	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	K201 (JTV-519) 是一种 Ca2+ 依赖性阻滞剂，通过稳定兰尼碱受体来防止缺血性心脏和骨骼肌 (SkM) 中的肌质网异常 Ca(2+) 泄漏。
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.
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。
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.
T11732	JTV-519 hemifumarate K201 hemifumarate	MELK	PI3K/Akt/mTOR signaling
	JTV-519 hemifumarate,Antiarrhythmic and cardioprotective properties. is a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and a partial agonist of ryanodine receptors in striated muscle.
T34458	Ryanodol
	Ryanodol is a complex diterpenoid that modulates intracellular calcium-ion release at ryanodine receptors, ion channels critical for skeletal and cardiac muscle excitation-contraction coupling and synaptic transmission.
T68886	FLA-365
	FLA-365 is a biochemical that has been shown to inhibit ryanodine-enhanced calcium release from skeletal SR vesicles in a dose-dependent manner.
T81236	RyRs activator 5
	RyRs activator 5 (Compd A-1) 为针对Spodoptera frugiperda鸟苷酸受体的有效激动剂。
T80039	ATX-II	Sodium Channel	Membrane transporter/Ion channel
	ATX-II为特定Na+通道调节剂，源自海葵(Anemonia sulcata)毒液。该化合物会使细胞培养物对Na+Halothane、Caffeine及Ryanodine敏感，并可诱发肺静脉心律失常及心房颤动。
T11731	JTV-519 free base K201 free base	FLT	Angiogenesis; Tyrosine Kinase/Adaptors
	JTV-519 free base (K201 free base), recognized for its antiarrhythmic and cardioprotective properties, functions as a Ca2+-dependent blocker of sarcoplasmic reticulum Ca2+-stimulated ATPase (SERCA) and serves as a partial agonist of ryanodine receptors in striated muscle.
T80063	Imperatoxin A	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Imperatoxin A，源自非洲蝎Pandinus imperator毒液的一种肽毒素，作为Ca2+-释放通道/兰尼碱受体（RyRs）的激活剂，促进Ca2+从肌浆网流入细胞。
T82936	ATX-II TFA	Sodium Channel	Membrane transporter/Ion channel
	ATX-II TFA为源自海葵(Anemonia sulcata)毒素的特定Na+通道调节剂，能使细胞培养物对Na+、Halothane、Caffeine和Ryanodine敏感，并可诱发肺静脉心律失常和心房颤动。
T11731L	JTV-519 Formate JTV-519 Formate (145903-06-6 Free base)	Others; Calcium Channel	Membrane transporter/Ion channel; Metabolism; Others
	JTV-519 Formate 是一种 Ca2+ 依赖性的肌质网 Ca2+ 刺激的 ATP 酶 (SERCA) 阻断剂，同时也是横纹肌中兰尼碱受体 (ryanodine receptors) 的部分激动剂。JTV-519 Formate 显示出抗心律失常作用，是一种心脏保护剂。
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。
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。
T82064	Insecticidal agent 6	Parasite	Microbiology/Virology
	Insecticidal agent 6（化合物 Im）是昆虫兰尼碱受体（RyRs）的抑制剂，该化合物对 S. frugiperda RyRs 具有强效的抑制作用，其 EC50 值为0.6308 µM。该化合物在鳞翅目害虫中展现出卓越的杀虫效果，适用于病虫害研究。
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。
T37803	8-bromo-Cyclic ADP-Ribose (sodium salt)
	Cyclic ADP-ribose (cADP-ribose) is a calcium mobilizing nucleotide that is biosynthesized from NAD+ by cADP-ribose synthases, including CD38. cADP-Ribose appears to activate calcium channels in intracellular membranes, which in turn activate ryanodine receptors. 8-bromo-cADP-Ribose is a stable, cell-permeable analog that blocks calcium release evoked by cADP-ribose in sea urchin egg homogenates with an IC50 value of 1.7 μM. It is commonly used to investigate intracellular signaling through cADP-...
T37475	Cyclic ADP-Ribose (ammonium salt) cADP-Ribose,cADPR,Cyclic ADP-Ribose (ammonium salt)
	Cyclic ADP-ribose (cADP-ribose) is an endogenous metabolite of NAD+ that mobilizes the release of stored Ca2+ in the endoplasmic reticulum via ryanodine receptors in various cell types.[1],[2],[3],[4],[5] This second messenger is generated via the cADP-ribose synthases CD38 and CD157.[6],[5],[7] cADP-Ribose may also trigger the cell surface Ca2+ influx channel TRPM2 in a temperature-dependent manner.[8] In vitro, cADP-ribose modulates Ca2+ signaling in rat and mouse cardiomyocytes treated with i...
T35922	NAADP (sodium salt)
	Nicotinic acid adenine dinucleotide phosphate (NAADP) is a secondary messenger that induces calcium mobilization. It induces calcium release from endosomes and lysosomes via two-pore channel 2 (TPC2) and TPC1, which then stimulates large-scale calcium release from granules and the endoplasmic reticulum mediated by type 1 ryanodine receptors (RyR2s), RyR3s, and inositol-(1,4,5)-triphosphate receptors (IP3Rs). NAADP induces calcium mobilization in sea urchin and starfish eggs post fertilization to...

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: T24239

Synonym: K-201,JTV 519,JTV-519,K 201

Target: Calcium Channel

Cat.No: T32855

Synonym: Cervilane

Azumolene sodium anhydrous

Cat.No: T72004

Cat.No: T80153

Target: Calcium Channel

Azumolene sodium dihydrate

Cat.No: T68366

JTV-519 hemifumarate

Cat.No: T11732

Synonym: K201 hemifumarate

Target: MELK

Cat.No: T34458

Cat.No: T68886

RyRs activator 5

Cat.No: T81236

Cat.No: T80039

Target: Sodium Channel

JTV-519 free base

Cat.No: T11731

Synonym: K201 free base

Target: FLT

Cat.No: T80063

Target: Calcium Channel

Cat.No: T82936

Target: Sodium Channel

JTV-519 Formate

Cat.No: T11731L

Synonym: JTV-519 Formate (145903-06-6 Free base)

Target: Others, Calcium Channel

RyRs activator 3

Cat.No: T79703

Target: Parasite

RyRs activator 4

Cat.No: T81237

Insecticidal agent 6

Cat.No: T82064

Target: Parasite

Cat.No: T80975

Target: Calcium Channel

8-bromo-Cyclic ADP-Ribose (sodium salt)

Cat.No: T37803

Cyclic ADP-Ribose (ammonium salt)

Cat.No: T37475

Synonym: cADP-Ribose,cADPR,Cyclic ADP-Ribose (ammonium salt)

NAADP (sodium salt)

Cat.No: T35922

Cat. No.	Product Name	Target	Signaling Pathways
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.
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。
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: T12787

Target: Others

Cat.No: T4973

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

Target: Endogenous Metabolite

Cyclic ADP-ribose

Cat.No: T19253

Synonym: cADPR

Target: Calcium Channel

Cyclic ADP-ribose ammonium

Cat.No: T37687

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