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33

抑制剂 & 化合物

9

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6579	Medetomidine hydrochloride MPV785,Medetomidine HCl,Domitor	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Medetomidine hydrochloride (MPV785) 是一种 α2 肾上腺素受体激动剂，能够作用于α2和α1肾上腺素受体，其Ki 分别为1.08 nM 和1750 nM。
T1650	Chlorzoxazone Paraflex,Chlorzoxazon,氯唑沙宗	P450; Potassium Channel	Membrane transporter/Ion channel; Metabolism
	Chlorzoxazone (Chlorzoxazon) 是作用于中枢的肌肉松弛剂, 可用于肌肉痉挛的研究。
T0156	Rocuronium bromide ORG 9426,罗库溴铵,ORG 9426 (Bromide)	AChR	Neuroscience
	Rocuronium bromide (ORG 9426) 是一种氨基甾体类的、非去极化的神经肌肉受体抑制剂，也是一种肌肉松弛剂。
T6968	Riociguat 利奥西呱,BAY 632521	Guanylate cyclase	GPCR/G Protein
	Riociguat (BAY 632521) 是一种鸟苷酸环化酶的刺激剂，可导致血管平滑肌松弛，用于治疗严重的肺动脉高压。
T12481	Pipecuronium bromide RGH-1106	AChR	Neuroscience
	Pipecuronium bromide (RGH-1106)是一种具有选择性和有效性的 nAChR 拮抗剂，也可当作一种非去极化甾体神经肌肉阻滞剂，可使肌肉松弛，常与抗生素一起使用。
T78108	µ-Conotoxin-CnIIIC acetate	Sodium Channel	Membrane transporter/Ion channel
	µ-Conotoxin-CnIIIC acetate 是一种高效的 NaV1.4 钠通道拮抗剂，是由22个氨基酸组成的芋螺肽，可用于肌肉松弛和缓解疼痛。
T0324	Isoxsuprine hydrochloride Duvadilan,Isolait,盐酸异克舒令,盐酸苯氧丙酚胺	Adrenergic Receptor; iGluR	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	Isoxsuprine hydrochloride (Isolait) 是 β 肾上腺素受体激动剂和NMDA 受体拮抗剂，对子宫肌层和胎盘的 β 肾上腺素受体的Ki 值分别为 13.65 和 3.48 μM。
T0954	Halothane Narcotane,氟烷,Anestan	Potassium Channel; Chloride channel; GABA Receptor; NMDAR	Membrane transporter/Ion channel; Neuroscience
	Halothane (Anestan) 可以减弱内皮依赖性舒张作用。
T1398	Tadalafil Cialis,他达那非,IC-351,西力士	Apoptosis; PDE	Apoptosis; Metabolism
	Tadalafil (IC-351) 是一种PDE5抑制剂，IC50为 1.8 nM。
T0096	Vardenafil 伐地那非,Vivanza,Levitra,Vardenafil hydrochloride	PDE	Metabolism
	Vardenafil (Vivanza) 是选择性、高效的、具有口服活性的磷酸二酯酶5抑制剂，IC50=0.7 nM。它能够非竞争性地抑制环磷酸鸟苷水解，从而提高 cGMP 水平。它对 PDE1 (180 nM)，PDE6 (11 nM)，PDE2，PDE3，PDE4 (>1000 nM) 具有选择性。它可用于研究勃起功能障碍。
T0939	Phenytoin 苯妥英,Diphenylhydantoin,5,5-Diphenylhydantoin	Virus Protease; Sodium Channel	Membrane transporter/Ion channel; Microbiology/Virology
	Phenytoin (5,5-Diphenylhydantoin) 是一种有效的电压门控钠离子通道阻滞剂，可减少小鼠乳腺肿瘤的生长和转移，具有抗癫痫活性。
T22371	Mivacurium dichloride 米库氯铵,Mivacurium chloride,二氯美维库铵	AChR	Neuroscience
	Mivacurium dichloride (Mivacurium chloride) 是苄基异喹啉衍生物，可与 nAChR 偶联，以减少或抑制乙酰胆碱对肌肉细胞末端盘的去极化作用。它也是非去极化短效的神经肌肉阻滞剂和骨骼肌松弛剂。
T1179	Tiotropium bromide Tiopropium,噻托溴铵,BA679 BR	AChR	Neuroscience
	Tiotropium bromide (BA679 BR) 是一种毒蕈碱乙酰胆碱受体拮抗剂，可阻断乙酰胆碱配体的结合。
T67956L	Litoxetine HCl litoxetine HCL(86811-09-8 Free base)	5-HT Receptor	GPCR/G Protein; Neuroscience
	Litoxetine HCl 是一种选择性5-羟色胺（5-HT）再摄取抑制剂（SSRI）和混合5-羟色胺拮抗剂，可用于治疗尿失禁。Litoxetine HCl 在没有抗毒蕈碱特性的浓度下（10 nM-1 microM）引起大鼠离体食道肌肉粘膜的浓度依赖性松弛，使卡巴胆碱张力降低达37%,更高浓度的Litoxetine HCl（3微摩-300微摩）与明显的松弛有关，直至取消卡巴胆碱张力。以前在离体豚鼠肠道中证明的利托西汀的抗心律失常活性，在浓度大于1 microM 时在大鼠离体食道肌肉粘膜中发挥了作用。 Litoxetine HCl 的5-HT 释放作用可以解释利托西汀对未处理的大鼠组织中的5-HT 诱导的松弛的效力，这种效力被pCPA 处理所逆转。
T68129L1	Picumeterol FA Picumeterol FA(130641-36-0 Free base)	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	picumeterol FA 是一种有效的选择性β2肾上腺素能受体激动剂。在体外和体内试验中，picumeterol FA 可产生持久的气道平滑肌松弛作用。picumeterol FA 是一种纯 R 对映异构体，可用于改善哮喘患者的肺功能和降低气道高反应性。
T26666	ASM-024	AChR	Neuroscience
	ASM-024是一种有效的烟碱受体激动剂，是一种小分子合成哌嗪化合物，可促进β2-肾上腺素受体不同的靶点和信号通路介导平滑肌松弛，是治疗哮喘和慢性阻塞性支气管炎的潜在化合物，具有抗炎活性。
T32066	Hexafluronium Bromide Mylaxen,Hexafluorenium bromide,Milaxen,Hexafluorenium dibromide,Esafluronio bromuro
	Hexafluronium bromide is a neuromuscular blocker and nicotinic acetylcholine receptor antagonist used in anesthesiology to prolong and enhance the skeletal muscle relaxation of succinylcholine during surgery.
T30321	Bentazepam Tiadipone,CI-718,Knoll brand of bentazepam,Thiadipone
	Bentazepam is a thienodiazepine, which is a benzodiazepine analogue. It has anti-anxiety, anti-convulsion, sedative and skeletal muscle relaxation properties.
T25637	Laudexium methylsulfate Laudexium,Laudolissin methosulphate
	Laudexium methylsulfate is a neuromuscular blocking drug or skeletal muscle relaxant. It is used adjunctively in surgical anesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation.
T25636	Laudexium Laudexium ion,Laudexium cation
	Laudexium is a neuromuscular blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs. It is used adjunctively in surgical anesthesia to facilitate endotracheal intubation and to provide skeletal muscle re
T69303	Isoxsuprine Free Base
	Isoxsuprine Free Base is a beta-adrenergic agonist that causes direct relaxation of uterine and vascular smooth muscle. Its vasodilating actions are greater on the arteries supplying skeletal muscle than on those supplying skin. It is used in the treatment of peripheral vascular disease and in premature labor.
T73439	MPH-220
	MPH-220是一种口服活性的、选择性骨骼肌myosin-2抑制剂，能够促进肌肉松弛。作为一种抗痉挛药物，它用于研究痉挛和肌肉僵硬。
T36150	14,15-EE-5(Z)-E
	Epoxyeicosatrienoic acids (EETs), such as 11(12)-EET and 14(15)-EET, are cytochrome P450 metabolites of arachidonic acid that have been identified as endothelium-derived hyperpolarizing factors with vasodilator activity. 14,15-EE-5(Z)-E is a structural analog of 14,15-epoxyeicosatrienoic acids (14,15-EET) that antagonizes EET-induced relaxation of vascular smooth muscle. Relaxation of U46619-constricted bovine arteries by 14,15-EET could be inhibited approximately 80% by 14,15-EE-5(Z)-E at a con...
T40744	Eperisone
	Eperisone is a centrally acting muscle relaxant and antispastic agent utilized in the treatment of conditions distinguished by muscle stiffness and pain. Its mechanism of action involves the relaxation of skeletal muscles and vascular smooth muscles, resulting in a range of beneficial effects including reduction of myotonia, enhancement of circulation, and suppression of the pain reflex. Additionally, Eperisone exhibits inhibitory properties on the pain reflex pathway and exerts a vasodilator ef...
T36547	Quazinone
	Quazinone is a selective inhibitor of phosphodiesterase 3 (PDE3) with positive inotropic and vasodilating properties.1,2 It induces relaxation of precontracted isolated human cavernous smooth muscle (IC50 = 4.2 μM).1 Quazinone (10-300 μg/kg) increases myocardial contractile force in anesthetized open-chest dogs in a dose-dependent manner, as well as decreases systolic and diastolic blood pressure.2 It also inhibits DNA synthesis induced by the PDGF isoform PDGF-BB in bovine coronary artery smoot...
T73804	Botulinum toxin type B
	Botulinum toxin type B是用于颈部肌张力障碍研究的抗原特异性肉毒毒素。该毒素为厌氧细菌肉毒梭菌产生的外毒素，其机制是通过抑制乙酰胆碱在神经肌肉接头的释放，从而导致注射部位肌肉的松弛性麻痹或减弱。
T11240	Ethacrynic acid D5	Others	Others
	Ethacrynic acid, a diuretic, functions as an inhibitor of L-type voltage-dependent and store-operated calcium channels, facilitating the relaxation of airway smooth muscle (ASM) cells. It exhibits anti-inflammatory effects, notably reducing retinoid-induced ear edema in mice, and inhibits glutathione S-transferases (GSTs), making it a potent suppressor of the NF-kB signaling pathway. Additionally, ethacrynic acid modulates leukotriene formation. A variant, Ethacrynic acid D5, is distinguished by...
T37787	10-Nitrolinoleic acid
	10-Nitrolinoleate is the product of nitration of linoleate by NO-derived reactive species. Other nitrolinoleates detected in human plasma and urine include 9-, 12-, and 13-nitrolinoleate. Nitrolinoleates activate peroxisome proliferator-activated receptor γ (PPARγ; Ki = 133 nM), inducing CD36 expression in macrophages, adipocyte differentiation, and glucose uptake. Nitrolinoleates can also be metabolized by smooth muscle cells to produce nitrite derivatives which in turn form NO, leading to incr...
T71329	Theophylline-d6
	Theophylline-d6 is intended for use as an internal standard for the quantification of theophylline by GC- or LC-MS. Theophylline is an inhibitor of phosphodiesterase. It is also an adenosine A1 and A2 receptor antagonist. Theophylline induces relaxation of isolated cat bronchial smooth muscle segments precontracted with acetylcholine. It inhibits ovalbumin-induced increases in bronchoalveolar lavage fluid (BALF) eosinophil infiltration in an ovalbumin-sensitized mouse model of allergic asthma. F...
T68129	Picumeterol GR 114297A	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Picumeterol（GR 114297A）是一种有效的选择性β2肾上腺素能受体激动剂。在体外和体内试验中，Picumeterol 可产生持久的气道平滑肌松弛作用。Picumeterol 是一种纯 R 对映异构体，可用于改善哮喘患者的肺功能和降低气道高反应性。
T78540	α-CGRP (mouse, rat) TFA	CGRP Receptor	GPCR/G Protein; Neuroscience
	α-CGRP (mouse, rat) TFA 是神经系统中的一种活性神经肽，位于神经肌肉接合部，具有显著的血管舒张功能。适用于心血管疾病、炎症、偏头痛及代谢研究领域。
T38306	tetranor-PGDM
	Prostaglandin D2 is synthesized by hematopoietic-type PGD-synthase (H-PGDS) in mast cells and is released in large quantities during allergic and asthmatic anaphylaxis. PGD2 is also produced in the brain by lipocalin-PGD-synthase also known as β-trace. In the brain, PGD2 produces normal physiological sleep and lowering of body temperature. Further pharmacological actions include inhibition of platelet aggregation and relaxation of vascular smooth muscle. tetranor-PGDM is a major metabolite of PG...
T83905	Brain Natriuretic Peptide-32 (rat) acetate BNP (14-45),B-type Natriuretic Peptide-32,Brain Natriuretic Polypeptide-32,BNP-32
	BNP-32（Brain natriuretic peptide-32）是心血管激素前体proBNP的肽段，能够结合大鼠血管平滑肌上的利钠肽受体（IC50 = 7.3 nM），并在同样的细胞中促进cGMP积累（EC50 = 170 nM）。BNP-32还能使经去甲肾上腺素预收缩的孤立大鼠主动脉条带松弛（EC50 = 6.7 nM），当以3 µg/kg的剂量给药时，能增加大鼠的尿量和尿液电解质排泄，并诱导低血压。

化合物

Medetomidine hydrochloride

Cat.No: T6579

Synonym: MPV785,Medetomidine HCl,Domitor

Target: Adrenergic Receptor

Cat.No: T1650

Synonym: Paraflex,Chlorzoxazon,氯唑沙宗

Target: P450, Potassium Channel

Rocuronium bromide

Cat.No: T0156

Synonym: ORG 9426,罗库溴铵,ORG 9426 (Bromide)

Target: AChR

Cat.No: T6968

Synonym: 利奥西呱,BAY 632521

Target: Guanylate cyclase

Pipecuronium bromide

Cat.No: T12481

Synonym: RGH-1106

Target: AChR

µ-Conotoxin-CnIIIC acetate

Cat.No: T78108

Target: Sodium Channel

Isoxsuprine hydrochloride

Cat.No: T0324

Synonym: Duvadilan,Isolait,盐酸异克舒令,盐酸苯氧丙酚胺

Target: Adrenergic Receptor, iGluR

Cat.No: T0954

Synonym: Narcotane,氟烷,Anestan

Target: Potassium Channel, Chloride channel, GABA Receptor, NMDAR

Cat.No: T1398

Synonym: Cialis,他达那非,IC-351,西力士

Target: Apoptosis, PDE

Cat.No: T0096

Synonym: 伐地那非,Vivanza,Levitra,Vardenafil hydrochloride

Target: PDE

Cat.No: T0939

Synonym: 苯妥英,Diphenylhydantoin,5,5-Diphenylhydantoin

Target: Virus Protease, Sodium Channel

Mivacurium dichloride

Cat.No: T22371

Synonym: 米库氯铵,Mivacurium chloride,二氯美维库铵

Target: AChR

Tiotropium bromide

Cat.No: T1179

Synonym: Tiopropium,噻托溴铵,BA679 BR

Target: AChR

Cat.No: T67956L

Synonym: litoxetine HCL(86811-09-8 Free base)

Target: 5-HT Receptor

Cat.No: T68129L1

Synonym: Picumeterol FA(130641-36-0 Free base)

Target: Adrenergic Receptor

Cat.No: T26666

Target: AChR

Hexafluronium Bromide

Cat.No: T32066

Synonym: Mylaxen,Hexafluorenium bromide,Milaxen,Hexafluorenium dibromide,Esafluronio bromuro

Cat.No: T30321

Synonym: Tiadipone,CI-718,Knoll brand of bentazepam,Thiadipone

Laudexium methylsulfate

Cat.No: T25637

Synonym: Laudexium,Laudolissin methosulphate

Cat.No: T25636

Synonym: Laudexium ion,Laudexium cation

Isoxsuprine Free Base

Cat.No: T69303

Cat.No: T73439

14,15-EE-5(Z)-E

Cat.No: T36150

Cat.No: T40744

Cat.No: T36547

Botulinum toxin type B

Cat.No: T73804

Ethacrynic acid D5

Cat.No: T11240

Target: Others

10-Nitrolinoleic acid

Cat.No: T37787

Theophylline-d6

Cat.No: T71329

Cat.No: T68129

Synonym: GR 114297A

Target: Adrenergic Receptor

α-CGRP (mouse, rat) TFA

Cat.No: T78540

Target: CGRP Receptor

Cat.No: T38306

Brain Natriuretic Peptide-32 (rat) acetate

Cat.No: T83905

Synonym: BNP (14-45),B-type Natriuretic Peptide-32,Brain Natriuretic Polypeptide-32,BNP-32

Cat. No.	Product Name	Target	Signaling Pathways
T6060	(±) Anabasine 八角枫碱	Endogenous Metabolite	Metabolism
	(±) Anabasine 是肌肉松弛剂，能够用于外科手术时肌肉松驰。
T3A2467	Allocryptopine Thalictrimine,Fagarine I,别隐品碱	Potassium Channel	Membrane transporter/Ion channel
	Allocryptopine (Thalictrimine) 是一种延胡索乙素的衍生物，提取自Corydalis decumbens。Allocryptopine 具有抗心律失常作用，能有效阻断hERG 电流。
T5014	Prostaglandin E2 地诺前列酮,前列腺素 E2,PGE2,Dinoprostone,Prostaglandin E2 (PGE2)	Endogenous Metabolite; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Metabolism
	Prostaglandin E2 (PGE2) 是一种天然激素，参与人体内的各种生理过程，包括平滑肌收缩和放松、调节血管扩张和收缩、调节血压和炎症调节。
T4S1102	Liensinine diperchlorate 莲心碱高氯酸盐,莲心碱二高氯酸盐,Liensinine-Perchlorate	Mitophagy; Others; Autophagy	Autophagy; Others
	Liensinine Diperchlorate 是从芙蕖种子胚中提取的一种异喹啉生物碱。它通过阻断自噬小体-溶酶体融合来抑制晚期自噬，具有抗心律不齐、抗高血压、抗肺纤维化和血管平滑肌松弛等生物学活性。
T0892	Diphylline 二羟丙茶碱,Dyphylline,Diprophylline	PDE; Adenosine Receptor	GPCR/G Protein; Metabolism; Neuroscience
	Diphylline (Diprophylline) 是一种A1/A2腺苷受体拮抗剂，也是环状核苷酸磷酸二酯酶抑制剂。它是一种黄嘌呤衍生物，具有支气管扩张和血管扩张作用，有用于治疗慢性支气管炎和肺气肿的潜力。
T1626	Prostaglandin E1 前列地尔,PGE1,列腺素E1,Alprostadil	Endogenous Metabolite; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Metabolism
	Prostaglandin E1 (Alprostadil) 是一种前列腺素受体配体，对小鼠 EP1、EP2、EP3、EP4和 IP 的 Ki 值分别为 36、10、1.1、2.1 和 33 nM。它诱导血管舒张并抑制血小板聚集，可作为血管扩张剂用于外周血管疾病的研究。
T5065	GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SOD Monosodium-GMP,cGMP sodium salt,鸟苷-3',5'-环磷酸一钠盐,Cyclic GMP	PKA	Tyrosine Kinase/Adaptors
	GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SOD (cGMP sodium salt) 也称为 cGMP，是一种细胞调节剂，被描述为第二信使。它的水平随着各种激素的增加而增加，包括乙酰胆碱、胰岛素和催产素。 cGMP 激活蛋白激酶 G(PKG) 并调节离子通道电导，信号传导影响多种过程，包括平滑肌松弛和增殖、光转导和能量稳态。
TN1985	Neoprzewaquinone A	ROCK; Pim; STAT	Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; JAK/STAT signaling; Stem Cells
	Neoprzewaquinone A (NEO) 是 S. miltiorrhiza 的活性成分，通过靶向 PIM1 阻断 ROCK2/STAT3 通路来抑制乳腺癌细胞迁移并促进平滑肌松弛。
T72152	Eicosapentaenoic Acid sodium 二十碳五烯酸钠盐,Timnodonic acid sodium,EPA sodium
	Eicosapentaenoic Acid (EPA) sodium 为口服活性 ω-3 长链多不饱和脂肪酸 (ω-3 LC-PUFAs)。其通过DNA去甲基化，促进肿瘤抑制基因CCAAT/增强子结合蛋白δ (C/EBPδ)的重新表达，并通过H-RAS内含子1 CpG岛的去甲基化，激活U937白血病细胞中RAS/ERK/C/EBPβ途径。此外，该化合物能够促进血管平滑肌细胞松弛和血管舒张。

天然产物

Cat.No: T6060

Synonym: 八角枫碱

Target: Endogenous Metabolite

Cat.No: T3A2467

Synonym: Thalictrimine,Fagarine I,别隐品碱

Target: Potassium Channel

Prostaglandin E2

Cat.No: T5014

Synonym: 地诺前列酮,前列腺素 E2,PGE2,Dinoprostone,Prostaglandin E2 (PGE2)

Target: Endogenous Metabolite, Prostaglandin Receptor

Liensinine diperchlorate

Cat.No: T4S1102

Synonym: 莲心碱高氯酸盐,莲心碱二高氯酸盐,Liensinine-Perchlorate

Target: Mitophagy, Others, Autophagy

Cat.No: T0892

Synonym: 二羟丙茶碱,Dyphylline,Diprophylline

Target: PDE, Adenosine Receptor

Prostaglandin E1

Cat.No: T1626

Synonym: 前列地尔,PGE1,列腺素E1,Alprostadil

Target: Endogenous Metabolite, Prostaglandin Receptor

GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SOD

Cat.No: T5065

Synonym: Monosodium-GMP,cGMP sodium salt,鸟苷-3',5'-环磷酸一钠盐,Cyclic GMP

Target: PKA

Neoprzewaquinone A

Cat.No: TN1985

Target: ROCK, Pim, STAT

Eicosapentaenoic Acid sodium

Cat.No: T72152

Synonym: 二十碳五烯酸钠盐,Timnodonic acid sodium,EPA sodium

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