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29

抑制剂 & 化合物

8

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T7144	BTS N-Tosylbenzylamine,N-苄基-对甲苯磺酸胺,N-Benzyl-p-toluenesulfonamide	ATPase; Myosin	Cytoskeletal Signaling; Membrane transporter/Ion channel
	BTS (N-Tosylbenzylamine) 是一种选择性骨骼肌肌球蛋白 II 亚片段 1 (S1) ATPase 活性抑制剂，可特异性抑制骨骼肌快速纤维的收缩。它对肌动蛋白和 Ca2+刺激的肌球蛋白 S1 ATPase 的 IC50值约为 5 µM。
T20386	Caprolactam	Others	Others
	Caprolactam 是一种用于制造聚酰胺类合成纤维的天然产物。
T23401	Strontium chloride	Others; CaSR	GPCR/G Protein; Others
	Strontium chloride 是钙敏感受体 (CaSR) 的激动剂，并可以直接影响 C 型神经纤维。
T0924	Benzocaine 苯唑卡因,苯佐卡因	Others; MRP; Sodium Channel	Immunology/Inflammation; Membrane transporter/Ion channel; Others
	Benzocaine 作用电压门控 Na+通道的共同受体，+30 mV 下的 IC50为0.8 mM。
T7218	Endomorphin 2 内吗啡肽 2	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	Endomorphin 2 是一种高亲和力和选择性的 μ-阿片受体激动剂，对 kappa3 结合位点具有合理的亲和力，Ki 为 20 到 30 nM 之间。
TD0098	Direct Red 80 Sirius Red,天狼猩红,Sirius Red F 3BA,C.I. direct red 80	Others	Others
	Direct Red 80 (Sirius Red) 是一种聚偶氮染料，在降解时不会释放联苯胺，比许多传统的直接染料更安全，主要用于胶原蛋白和淀粉样蛋白的染色方法。
TP1325L	Gastrin-Releasing Peptide, human(TFA)	Others	Others
	Gastrin-Releasing Peptide, human(TFA） (93755-85-2 free base) 是一种调节性人类肽，可引发胃泌素释放并调节胃酸分泌和肠道运动功能。支配胃G 细胞的迷走神经节后纤维释放GRP，刺激G 细胞释放胃泌素。
T1046	Mexiletine hydrochloride KOE-1173 (hydrochloride),Mexiletine HCl,KO1173,盐酸美西律	AhR; Sodium Channel	Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism
	Mexiletine hydrochloride (KOE-1173 hydrochloride) 是一种电压门控钠通道阻滞剂，是 IB 类抗心律失常药。 Mexiletine hydrochloride 通过抑制心肌细胞内钠电流，从而降低心脏动作电位（0相）上升速率，并且降低浦肯野纤维的自律性而发挥抗心律失常作用。
T30249	AZD 7009 AZD-7009,AZD7009	Sodium Channel	Membrane transporter/Ion channel
	AZD 7009是一种新型抗心律失常化合物，对CHO K1细胞中 hNav1.5的钠电流具有抑制作用，IC50为11 uM。AZD 7009 对离体兔心房和心室肌细胞的晚期钠电流具有抑制作用，对e -4031诱导的动作电位持续时间延长具有抑制作用，促使浦肯野纤维的早期后去极化(EADs)。
T0866	Propafenone Rythmol,普罗帕酮,Propafenonum	Potassium Channel; MRP; Sodium Channel	Immunology/Inflammation; Membrane transporter/Ion channel
	Propafenone (Propafenonum) 是钠通道阻滞剂，它对 β 受体具有高亲和力 (IC50=32 nM)。它能够阻断瞬时外向钾电流 (Ito) (IC50: 4.9 nM) 和持续延迟整流器K+电流 (Isus) (IC50: 8.6 nM) ，具有抗心律失常的作用。它能够诱导线粒体功能障碍及诱导细胞凋亡，从而抑制食管癌增殖。
T0210L	Tamsulosin LY253351 free base,HSDB7744,(R)-(-)-YM12617 free base,Harnal-D,Flowmax,HSDB 7744,HSDB-7744	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Tamsulosin ((R)-(-)-YM12617 free base) 是一种肾上腺素能受体α 1A 拮抗剂，用于良性前列腺增生(BPH)的治疗。Tansulosin 用于治疗排尿困难，这是前列腺肥大的一种常见症状。Tansulosin 和其他被称为α受体阻滞剂的药物通过放松膀胱颈部肌肉和前列腺本身的肌肉纤维来发挥作用，使其更容易排尿。
T77577	SLU-PP-332	Estrogen/progestogen Receptor	Endocrinology/Hormones
	SLU-PP-332 是一种泛雌激素受体相关受体 (ERR) 激动剂，其对 ERRα, ERRβ 以及 ERRγ 具有很高的亲和力，EC50 值分别为 98、230 以及 430 nM。SLUPP-332 可增强骨骼肌细胞系的线粒体功能和细胞呼吸，增加 IIa 型氧化骨骼肌纤维并增强了运动耐力。SLU-PP-332 具有研究代谢性疾病以及肌肉功能改善的潜力，可能用于改善代谢紊乱和衰老。
T20032	CI Direct Brown 2 Airedale Brown MD,Brown M,NSC 74701,Direct Brown 2,NSC-74701,NSC74701
	CI Direct Brown 2 is a direct dye. It is soluble in water and ionizable to form colored anions. It also can directly dye cellulose fibers or protein fibers.
T32724	LF 14 LF14,LF-14
	LF 14 affects mammalian non-myelinated nerve fibers.
T61215	Alinidine hydrobromide
	Alinidine hydrobromide, a specific bradycardic agent, diminishes the slope of the diastolic depolarization in sinoatrial tissue and Purkinje fibers [1].
T71531	Metamizil hydrochloride
	Metamizil hydrochloride is a cholinolytic agent -- an agent that blocks the transmission of excitation from cholinergic nerve fibers -- and an antagonist of the mediator acetylcholine.
TP1325	Gastrin-Releasing Peptide, human
	Gastrin-Releasing Peptide, human is a regulatory human peptide that elicits gastrin release and regulates gastric acid secretion and enteric motor function. The post-ganglionic fibers of the vagus nerve that innervate the G cells of the stomach release GRP, which stimulates the G cells to release gastrin.
T6782	Benzocaine hydrochloride Benzocaine HCl,Ethyl p-aminobenzoate hydrochloride,Ethyl 4-aminobenzoate hydrochloride	Sodium Channel	Membrane transporter/Ion channel
	Benzocaine hydrochloride (Ethyl 4-aminobenzoate hydrochloride) 是一种表面麻醉剂，通过阻止脉冲沿神经纤维和神经末梢传递而起作用。
T35755	Avermectin B1a aglycone
	Avermectin B1a aglycone is an aglycone form of the anthelmintic and insecticide avermectin B1a . It hyperpolarizes P. crassipes muscle fibers with a minimum active concentration (MAC) value of 0.1 μM. Avermectin B1a aglycone decreases survival of C. elegans (MAC = 0.1 μM). In vivo, avermectin B1a aglycone prevents seizures induced by pentylenetetrazole in mice (ED50 = 43.9 mg/kg) without inducing deficits in rotarod performance.
T70282	Drofenine
	Drofenin is an anticonvulsant. It is an anticholinergic that acts both at the level of the nerves and the muscle fibers (neurotropic musculotropic effect). Drofenin also acts as FIASMA (functional inhibitor of acid sphingomyelinase )
T26821	BIPM
	BIPM is a potent inhibitor of Rho-associated protein kinase 2 (ROCK2). Exposure of SH-SY5Y cells to BIPM led to significant changes in cell migration, actin stress fibers and neurite length. BIPM significantly inhibits phosphorylation of cofilin, a regula
TP1668	CGGRGD TFA (1260223-44-6 free base) CGGRGD TFA
	CGGRGD TFA is synthesized via solid-phase peptide synthesis technique and the surface of PCL fibers is aminolysised by amino 2-cyanobenzothiazole followed by the addition of 2-cyanobenzothiazole (CBT)[1].
TP1609	Angiotensin II (1-4), human
	Angiotensin II is a potent direct vasoconstrictor, causing arteries and veins to constrict, so leading to an increase in blood pressure. Angiotensin also potentiates the release of norepinephrine by a direct action on postganglionic sympathetic fibers.
T36561	(3S)-hydroxy Quinidine
	(3S)-hydroxy Quinidine is an active quinidine metabolite. Quinidine, an antiarrhythmic agent, undergoes rapid first-pass metabolism by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2C9, CYP2E1, and CYP3A5, with CYP3A4 being the most active enzyme in the (3S)-hydroxy quinidine formation. (3S)-hydroxy Quinidine prolongs repolarization of canine Purkinje fibers in vitro and prevents ventricular fibrillation and ventricular tachycardia after coronary reperfusion in isolated rat hearts in a dose-depe...
T81787	MitTx-beta
	MitTx-beta为一多肽，源自得克萨斯珊瑚蛇(Micrurus tener tener)之毒液。与MitTx-α配对，组成复合物MitTx，此复合物激活ASIC1通道，存在于辣椒素敏感神经纤维上。
T71356	Lanperisone HCl
	Lanperisone, also known as NK433, is a muscle relaxant. NK433 inhibited the facilitation of the flexor reflex mediated by group II afferent fibers that was induced by intrathecal administration of noradrenaline-HCl. NK433 had effects more than three times stronger and tending to be longer-lasting than those of eperisone-HCl. These results suggest that NK433 exerts a non-selective inhibition on spinal reflexes and that inhibition of the descending noradrenergic tonic facilitation within the spina...
T76135	Hemicellulase
	Hemicellulase（半纤维素酶），糖苷水解酶家族成员，广泛应用于生化研究领域。该酶能够分解植物纤维中的葡萄糖及其与水分子的聚合物，是自然界植物生物量及碳流降解的关键酶类。
T71119	Netarsudil free base
	Netarsudil, also known as AR-11324, is a Rho-associated protein kinase inhibitor. Netarsudil is potential useful for treating glaucoma and/or reducing intraocular pressure. Netarsudil Increases Outflow Facility in Human Eyes Through Multiple Mechanisms. Netarsudil inhibited kinases ROCK1 and ROCK2 with a Ki of 1 nM each, disrupted actin stress fibers and focal adhesions in TM cells with IC50s of 79 and 16 nM, respectively, and blocked the profibrotic effects of TGF-β2 in HTM cells. Netarsudi...
T61475	Ropivacaine mesylate
	Ropivacaine mesylate 是一种高效的钠通道 (sodium channel) 阻断剂，通过可逆性抑制钠离子内流 (sodium ion influx)，引致神经纤维脉冲传导阻滞。此外，Ropivacaine 还能抑制 K2P(双孔钾通道)TREK-1，其在 COS-7 细胞膜上的 IC50 值为 402.7 μM。

化合物

Cat.No: T7144

Synonym: N-Tosylbenzylamine,N-苄基-对甲苯磺酸胺,N-Benzyl-p-toluenesulfonamide

Target: ATPase, Myosin

Cat.No: T20386

Target: Others

Strontium chloride

Cat.No: T23401

Target: Others, CaSR

Cat.No: T0924

Synonym: 苯唑卡因,苯佐卡因

Target: Others, MRP, Sodium Channel

Cat.No: T7218

Synonym: 内吗啡肽 2

Target: Opioid Receptor

Cat.No: TD0098

Synonym: Sirius Red,天狼猩红,Sirius Red F 3BA,C.I. direct red 80

Target: Others

Gastrin-Releasing Peptide, human(TFA)

Cat.No: TP1325L

Target: Others

Mexiletine hydrochloride

Cat.No: T1046

Synonym: KOE-1173 (hydrochloride),Mexiletine HCl,KO1173,盐酸美西律

Target: AhR, Sodium Channel

Cat.No: T30249

Synonym: AZD-7009,AZD7009

Target: Sodium Channel

Cat.No: T0866

Synonym: Rythmol,普罗帕酮,Propafenonum

Target: Potassium Channel, MRP, Sodium Channel

Cat.No: T0210L

Synonym: LY253351 free base,HSDB7744,(R)-(-)-YM12617 free base,Harnal-D,Flowmax,HSDB 7744,HSDB-7744

Target: Adrenergic Receptor

Cat.No: T77577

Target: Estrogen/progestogen Receptor

CI Direct Brown 2

Cat.No: T20032

Synonym: Airedale Brown MD,Brown M,NSC 74701,Direct Brown 2,NSC-74701,NSC74701

Cat.No: T32724

Synonym: LF14,LF-14

Alinidine hydrobromide

Cat.No: T61215

Metamizil hydrochloride

Cat.No: T71531

Gastrin-Releasing Peptide, human

Cat.No: TP1325

Benzocaine hydrochloride

Cat.No: T6782

Synonym: Benzocaine HCl,Ethyl p-aminobenzoate hydrochloride,Ethyl 4-aminobenzoate hydrochloride

Target: Sodium Channel

Avermectin B1a aglycone

Cat.No: T35755

Cat.No: T70282

Cat.No: T26821

CGGRGD TFA (1260223-44-6 free base)

Cat.No: TP1668

Synonym: CGGRGD TFA

Angiotensin II (1-4), human

Cat.No: TP1609

(3S)-hydroxy Quinidine

Cat.No: T36561

Cat.No: T81787

Lanperisone HCl

Cat.No: T71356

Cat.No: T76135

Netarsudil free base

Cat.No: T71119

Ropivacaine mesylate

Cat.No: T61475

Cat. No.	Product Name	Target	Signaling Pathways
T15716	Lasalocid sodium 拉沙洛西钠,拉沙里菌素,Ionophore X-537A sodium,Antibiotic X-537A sodium,Lasalocid-A sodium	Antibacterial; Antibiotic; Autophagy	Autophagy; Microbiology/Virology
	Lasalocid sodium (Lasalocid-A sodium) 是一种抗菌剂。
T8195	Lotusine	Others	Others
	Lotusine 是一种提取自Nelumbo nucifera Gaertn 的绿色种胚中的纯生物碱。它能够作用于心肌中动作电位及心脏浦肯野纤维缓慢内向电流。
T3229	Cytochalasin D	ATPase; p38 MAPK; Calcium Channel; Akt; PI3K	Cytoskeletal Signaling; MAPK; Membrane transporter/Ion channel; Metabolism; PI3K/Akt/mTOR signaling
	Cytochalasin D is an actin inhibitor, the removal of actin stress fibers is crucial for the chondrogenic differentiation. It may be an inhibitor of some fertilization processes such as sperm penetration or sperm head decondensation. Cytochalasin D inhibit
TN1216	2-O-Acetyl-20-hydroxyecdysone 20-Hydroxyeedysone 2-acetate	Beta Amyloid; Others	Neuroscience; Others
	2-O-Acetyl-20-hydroxyecdysone 是存在于昆虫和陆生植物中的一种蜕皮激素，2-O-Acetyl-20-hydroxyecdysone 对 amyloid-β42 诱导的细胞毒性有抑制作用，能够通过促进纤维发生减少 Aβ 寡聚物的形成，将 Aβ 寡聚物转变为低毒性纤维。
T2163	Dihydrocapsaicin CCRIS1589,二氢辣椒素,6,7-Dihydrocapsaicin,8-Methyl-N-vanillylnonanamide	Others; TRP/TRPV Channel	Membrane transporter/Ion channel; Others
	Dihydrocapsaicin (CCRIS1589) 是一种天然来源的辣椒素，是TRPV1的选择性激动剂，同时可以增加 p-Akt 水平。它可以增强低温诱导的神经保护。
T3S0626	Denudatine 光翠雀碱；裸翠雀亭,光翠雀碱	Others	Others
	Denudatine 是分离自乌头属和翠雀属植物中，能够影响心室纤维的动作电位，并抑制乌头碱的致心律失常作用。
T20173	Noradrenaline tartrate NSC 169106,NSC-169106,l-Noradrenaline d-bitartrate,NSC169106,Norepinephrine bitartrate
	Norepinephrine bitartrate is a precursor of epinephrine. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus.
T78489	Lotusine hydroxide
	Lotusine (hydroxide)为纯生物碱，源自Nelumbo nucifera Gaertn绿色种胚提取。该化合物能够影响心肌动作电位和心脏浦肯野纤维的缓慢内向电流。

天然产物

Lasalocid sodium

Cat.No: T15716

Synonym: 拉沙洛西钠,拉沙里菌素,Ionophore X-537A sodium,Antibiotic X-537A sodium,Lasalocid-A sodium

Target: Antibacterial, Antibiotic, Autophagy

Cat.No: T8195

Target: Others

Cat.No: T3229

Target: ATPase, p38 MAPK, Calcium Channel, Akt, PI3K

2-O-Acetyl-20-hydroxyecdysone

Cat.No: TN1216

Synonym: 20-Hydroxyeedysone 2-acetate

Target: Beta Amyloid, Others

Dihydrocapsaicin

Cat.No: T2163

Synonym: CCRIS1589,二氢辣椒素,6,7-Dihydrocapsaicin,8-Methyl-N-vanillylnonanamide

Target: Others, TRP/TRPV Channel

Cat.No: T3S0626

Synonym: 光翠雀碱；裸翠雀亭,光翠雀碱

Target: Others

Noradrenaline tartrate

Cat.No: T20173

Synonym: NSC 169106,NSC-169106,l-Noradrenaline d-bitartrate,NSC169106,Norepinephrine bitartrate

Lotusine hydroxide

Cat.No: T78489

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