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33

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T16531	Picaridin 埃卡瑞丁,Lcaridin	Parasite	Microbiology/Virology
	Picaridin (Lcaridin) 是一种广谱节肢动物驱避剂，作用于蚊子和蜱的嗅觉感应，与其气味受体蛋白相互作用。
T9461	AZ194	Sodium Channel	Membrane transporter/Ion channel
	CRMP2-Ubc9-NaV1.7 inhibitor 194 是一流的CRMP2-Ubc9相互作用抑制剂及NaV1.7抑制剂 (IC50=1.2 μM)，口服有活性，具有抗伤害作用。AZ194 阻断 CRMP2 的 SUMOylation 以选择性地减少表面表达 NaV1.7 的量。
T9263	cim0216 N-(5-methyl-1,2-oxazol-3-yl)-2-phenyl-2-(1,2,3,4-tetrahydroquinolin-1-yl)acetamide	TRP/TRPV Channel	Membrane transporter/Ion channel
	CIM0216 是选择性的TRPM3激动剂，对 TRPM3 的选择性高于 TRPM1、TRPM2 和 TRPM4-8。它以TRPM3依赖性的方式引起疼痛并唤起感觉神经末梢的神经肽释放，可用于神经源性炎症的相关研究。
T1030	Triprolidine hydrochloride monohydrate 盐酸曲普利啶,盐酸曲普利啶一水合物,Triprolidine hydrochloride	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Triprolidine hydrochloride monohydrate 是一种组胺 H1 拮抗剂，用于过敏性鼻炎、哮喘。
T8333	Aurintricarboxylic acid ATA,NSC-4056,NSC4056,金精三羧酸,NSC 4056	Apoptosis; P2X Receptor; Influenza Virus; Topoisomerase	Apoptosis; DNA Damage/DNA Repair; Membrane transporter/Ion channel; Microbiology/Virology; Neuroscience
	Aurintricarboxylic acid (NSC-4056) 是高效的αβ-亚甲基-ATP 敏感选择性P2X1Rs 和P2X3Rs 变构拮抗剂。它是核糖核酸酶和拓扑异构酶 II 的有效抑制剂，可阻止核酸与酶结合。
T0217L	(+)-Dropropizine (+)-Dropropizine,左羟丙哌嗪	Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	(+)-Dropropizine 可以抑制组胺受体，抗过敏，并通过调节参与咳嗽反射的神经肽和干扰感觉神经末梢的刺激激活来减少咳嗽。
T15192	Eact	Chloride channel	Membrane transporter/Ion channel
	Eact 是一种选择性和有效的 TMEM16A 激活剂，可直接激活感觉伤害感受器中的 TRPV1 通道，还会产生瘙痒、急性伤害感受和热过敏。
T23002	ML-335	Opioid Receptor	Endocrinology/Hormones; GPCR/G Protein; Neuroscience
	ML-335 是μ-δ异构体靶向激动剂，是一种μOR-δOR 偏向配体，可以作为开发独特类型（异构体偏倚）药物的支架。ML-335是MOR（μ阿片受体）/DOR（δ阿片受体）异构体，具有抗伤害感受活性和抑制疼痛的活性。
T8776	FEMA 4774 S9632	Others	Others
	FEMA 4774 (S9632) 是 T1R2/T1R3 的正变构调节剂。 FEMA 4774 在感官评价测试中表现出明显增强蔗糖的甜度。
T10624	BT-13	c-RET	Apoptosis; Tyrosine Kinase/Adaptors
	BT-13 是一种胶质细胞源性神经营养因子 (GDNF) 受体 RET 的选择性激动剂，独立于 GDNF 配体发挥作用，能够促进体外感觉神经元神经突生长，减少大鼠神经病变的发生。
T12632	(R)-Mirtazapine (R)-Org3770,(R)-6-Azamianserin	5-HT Receptor	GPCR/G Protein; Neuroscience
	(R)-Mirtazapine ((R)-Org3770) 是 Mirtazapine 的 R(-)-对映体，在急性热痛觉动物模型中具有抗伤害感受的特性。(R)-Mirtazapine 是 5-HT3 受体的拮抗剂，是一种潜在的镇痛剂。
T21483	Tricaine methanesulfonate 3-氨基苯甲酸乙酯甲基磺酸盐,MS-222	Others	Others
	Tricaine methanesulfonate (MS-222) 常用于固定鱼的标记和运输，并能抑制入侵过程中的感觉系统。
T1092	Zolmitriptan 佐米曲普坦,311C90,BW-311C90	5-HT Receptor	GPCR/G Protein; Neuroscience
	Zolmitriptan (311C90) 是一种5-HT1B/1D 受体部分激动剂，可用于偏头痛的研究，对 5-HT1B、5-HT1D、5-HT1F 受体的Ki 分别为 5.01、0.63 和 63.09 nM。
T2525	Alosetron hydrochloride Lotronex,盐酸阿洛司琼,GR 68755C,GR 68755,GR 68755X	5-HT Receptor	GPCR/G Protein; Neuroscience
	Alosetron hydrochloride (GR 68755) 是一种高选择性的 5-HT3 受体拮抗剂，可减轻清醒或麻醉犬直肠扩张的内脏伤害性效应，具有抗炎活性，用于肠易激综合征的研究。它阻断 5HT3 介导的豚鼠肌间和粘膜下神经元的快速去极化，IC50约为 55 nM。
T12992	SPR741 acetate SPR741 acetate,NAB741 acetate,SPR741 acetate (1179330-52-9 free base)	Antibacterial	Microbiology/Virology
	SPR741 acetate 是衍生自多粘菌素 B 的阳离子肽，通过增加革兰氏阴性细菌外膜的通透性来抑制严重的革兰氏阴性细菌感从而展现出对革兰氏阴性菌的抗菌活性。SPR741 acetate 常与抗生素联合使用来治疗一些疾病。
T29968	AMG-0347 UNII-CD7L9290QR	TRP/TRPV Channel	Membrane transporter/Ion channel
	AMG-0347 (UNII-CD7L9290QR)是一种靶向TRPA1(瞬时受体电位锚蛋白1)离子通道的小分子抑制剂，是一种在感觉神经元中发现的受体，参与疼痛和环境刺激物的检测。AMG-0347通过阻断TRPA1的功能起作用，具有镇痛作用。
T24754	Hh-Ag1.5 SAG-1.5,SAG1.5,SAG 1.5	Hedgehog/Smoothened	GPCR/G Protein; Stem Cells
	Hh-Ag1.5 (SAG-1.5) 是一种高效的 Hedgehog (Hh) 激动剂(EC50： 1 nM)和Smoothened (Smo)受体激动剂，对Smo的 EC50 为 1 nM、 Ki值在 0.5 和 2.3 nM 之间。Hh-Ag1.5 介导的重编程打破了非损伤肝脏干细胞的静止状态，从而挽救了肝衰竭。Hh-Ag1.5 诱导 hiPSCs 分化为皮肤前体细胞、脊髓运动神经元和脊髓感觉神经元。
T10572L	BMT-124110 Formate BMT-124110 Formate（1679371-59-5 Free base）	Serine/threonin kinase; TGF-beta/Smad; AAK1 (AP2 associated kinase 1)	Cell Cycle/Checkpoint; Metabolism; Neuroscience; Stem Cells
	BMT-124110 Formate 是一种具有选择性的AAK1抑制剂(IC50: 0.9 nM)，具有抗伤害感受活性。BMT-124110 Formate 抑制BMP -2诱导蛋白激酶BIKE,其IC50为 17 nM。BMT-124110 Formate 抑制细胞周期蛋白 G 相关激酶GAK，其IC50:为99 nM。
T6602	Naratriptan hydrochloride Naratriptan HCl,Amerge,Naramig,盐酸那拉曲坦,GR-85548A hydrochloride	5-HT Receptor	GPCR/G Protein; Neuroscience
	Naratriptan hydrochloride (GR-85548A hydrochloride) 是一种5-HT1受体激动剂，有抗偏头疼特性。它还可以通过刺激三叉神经系统感觉神经末梢上的 5-HT1D/1B 受体来发挥其作用，从而减少促炎神经肽的释放。
T34535	Satratoxin G Satratoxin-G
	Satratoxin G is a trichothecene mycotoxin of Stachybotrys chartarum and has been shown to selectively induces apoptosis in olfactory sensory neurons (OSNs) of the nose and brain.
T71246	DD04107
	DD04107 is a novel inhibitor of α-calcitonin gene-related peptide (α-CGRP) exocytotic release from primary sensory neurons, selectively interacting with Synaptotagmin 1.
T28223	OB-1
	OB-1 is an inhibitor of stomatin-like protein-3 (STOML3) oligomerization. OB-1 reversibly reduces the sensitivity of mechanically gated currents in sensory neurons and silence mechanoreceptors in vivo.
T28224	OB-2
	OB-2 is an inhibitor of stomatin-like protein-3 (STOML3) oligomerization. OB-2 reversibly reduces the sensitivity of mechanically gated currents in sensory neurons and silence mechanoreceptors in vivo.
TP1631L	Competence-Stimulating Peptide-12261 acetate Competence-Stimulating Peptide-12261 acetate (1235882-91-3 free base)	Others	Others
	Competence-Stimulating Peptide-12261 acetate (1235882-91-3 free base) 是感觉刺激肽的片段，是一种抑制胚管 (GT) 形成的群体感应分子。
T60514	Triprolidine
	Triprolidine 是一种口服活性的组胺H1受体拮抗剂，可用于过敏性鼻炎的研究。Triprolidine 具有脊髓运动和知觉阻止的作用。
T81664	NMB-1
	NMB-1，一种锥肽类似物，选择性抑制感觉神经元的持续机械激活电流(IC50: 1 μM)，有效抑制机械性疼痛，并可用于研究听力和压力诱发疼痛。
T71559	Melanotan II acetate
	Melanotan II acetate is an agonist of melanocortin receptor 1 (MC1R), MC3R, MC4R, and MC5R. It has been shown to improve recovery of sciatic nerve function after mechanical injury and increase cisplatin-induced decreases in sensory nerve conduction velocity. Melanotan II acetate increases oxygen consumption and protein levels of uncoupling protein 1 (UCP1) in brown adipose tissue homogenates and decreases food intake, body weight, and serum levels of leptin, glucose, insulin, and cholesterol.
T76539	Insulin-like growth factor II
	Insulin-like growth factor II (IGF-2)为人血清中主要生长激素，对神经突生长具有许可性和直接作用，同时增强交感与感觉神经元的生存能力。
T62670	Cemdomespib
	Cemdomespib (KU-596) 是一种高效的二代 Hsp90 调节剂。Cemdomespib 能够诱导热休克反应，诱导 Hsp70 水平，具有神经保护作用。Cemdomespib 具有改善糖尿病周围神经病变模型感觉缺陷的疗效。
T60289	Pemirolast
	Pemirolast 是一种具有口服活性的抗过敏剂。Pemirolast 通过抑制感觉神经肽的释放来减轻紫杉醇超敏反应，可用于对支气管哮喘和结膜炎的研究。
T35461	δ14-Triamcinolone acetonide
	δ14-Triamcinolone acetonide is a potential impurity found in commercial preparations of triamcinolone acetonide. Triamcinolone acetonide is a synthetic corticosteroid. It decreases cytokine levels, the firing rate of sensory neurons, and mechanical hypersensitivity in a rat spinal nerve ligation model when used at a dose of 1.5 mg/kg prior to and following surgery for three days. Triamcinolone acetonide also decreases outflow facility in a mouse model of steroid-induced glaucoma when 20 μl of a ...
T37969	12(S)-HpETE
	12(S)-HpETE is a monohydroperoxy polyunsaturated fatty acid (PUFA) produced by the action of platelet or leukocyte 12-lipoxygenase (12-LO) on arachidonic acid. It activates human blood leukocyte 5-LO, resulting in the synthesis of 5(S)-HETE, leukotriene B4 (LTB4), and 5(S),12(S)-DiHETE. Rat lung metabolizes 12(S)-HpETE to 8,11,12- and 10,11,12-trihydroxyeicostrienoic acids. 12(S)-HpETE is the mediator of many biological functions, including induction of c-fos and c-jun, activation of AP-1, and e...
T76127	Urocortin II, mouse
	Urocortin II, mouse 是一种选择性的 2 型促肾上腺皮质激素释放因子 (CRF2) 受体内源性多肽激动剂，对CRFR2和CRFR1的Ki 值分别为 0.66 nM 和 ﹥100 nM。Urocortin II, mouse 通过以 cAMP/PKA 和 Ca2+/CaMKII 依赖性方式激活 CRF2 受体。Urocortin II, mouse 在中枢神经系统的离散区域表达，并激活参与内脏感觉信息处理和调节自主神经外流的中枢神经元。

化合物

Cat.No: T16531

Synonym: 埃卡瑞丁,Lcaridin

Target: Parasite

Cat.No: T9461

Target: Sodium Channel

Cat.No: T9263

Synonym: N-(5-methyl-1,2-oxazol-3-yl)-2-phenyl-2-(1,2,3,4-tetrahydroquinolin-1-yl)acetamide

Target: TRP/TRPV Channel

Triprolidine hydrochloride monohydrate

Cat.No: T1030

Synonym: 盐酸曲普利啶,盐酸曲普利啶一水合物,Triprolidine hydrochloride

Target: Histamine Receptor

Aurintricarboxylic acid

Cat.No: T8333

Synonym: ATA,NSC-4056,NSC4056,金精三羧酸,NSC 4056

Target: Apoptosis, P2X Receptor, Influenza Virus, Topoisomerase

(+)-Dropropizine

Cat.No: T0217L

Synonym: (+)-Dropropizine,左羟丙哌嗪

Target: Histamine Receptor

Cat.No: T15192

Target: Chloride channel

Cat.No: T23002

Target: Opioid Receptor

Cat.No: T8776

Synonym: S9632

Target: Others

Cat.No: T10624

Target: c-RET

(R)-Mirtazapine

Cat.No: T12632

Synonym: (R)-Org3770,(R)-6-Azamianserin

Target: 5-HT Receptor

Tricaine methanesulfonate

Cat.No: T21483

Synonym: 3-氨基苯甲酸乙酯甲基磺酸盐,MS-222

Target: Others

Cat.No: T1092

Synonym: 佐米曲普坦,311C90,BW-311C90

Target: 5-HT Receptor

Alosetron hydrochloride

Cat.No: T2525

Synonym: Lotronex,盐酸阿洛司琼,GR 68755C,GR 68755,GR 68755X

Target: 5-HT Receptor

Cat.No: T12992

Synonym: SPR741 acetate,NAB741 acetate,SPR741 acetate (1179330-52-9 free base)

Target: Antibacterial

Cat.No: T29968

Synonym: UNII-CD7L9290QR

Target: TRP/TRPV Channel

Cat.No: T24754

Synonym: SAG-1.5,SAG1.5,SAG 1.5

Target: Hedgehog/Smoothened

BMT-124110 Formate

Cat.No: T10572L

Synonym: BMT-124110 Formate（1679371-59-5 Free base）

Target: Serine/threonin kinase, TGF-beta/Smad, AAK1 (AP2 associated kinase 1)

Naratriptan hydrochloride

Cat.No: T6602

Synonym: Naratriptan HCl,Amerge,Naramig,盐酸那拉曲坦,GR-85548A hydrochloride

Target: 5-HT Receptor

Cat.No: T34535

Synonym: Satratoxin-G

Cat.No: T71246

Cat.No: T28223

Cat.No: T28224

Competence-Stimulating Peptide-12261 acetate

Cat.No: TP1631L

Synonym: Competence-Stimulating Peptide-12261 acetate (1235882-91-3 free base)

Target: Others

Cat.No: T60514

Cat.No: T81664

Melanotan II acetate

Cat.No: T71559

Insulin-like growth factor II

Cat.No: T76539

Cat.No: T62670

Cat.No: T60289

δ14-Triamcinolone acetonide

Cat.No: T35461

Cat.No: T37969

Urocortin II, mouse

Cat.No: T76127

Cat. No.	Product Name	Target	Signaling Pathways
TN1308	6-Hydroxyflavanone	Others; Lipoxygenase; COX; GABA Receptor	Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience; Others
	6-Hydroxyflavanone 是从菖蒲叶中提取分离，通过靶向环氧合酶-2（COX-2），5-脂氧合酶（5-LOX）以及阿片类药物和 GABA-A 受体从而具有抗炎和抗神经性疼痛活性。6-Hydroxyflavanone 在链脲佐菌素诱导的糖尿病神经病变模型中具有抗伤害感受特性。
T5S1389	Escin IB 七叶皂苷B,七叶皂苷 IB	5-HT Receptor; NO Synthase	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Escin IB 是一种皂苷，分离自马栗子种子的皮和胚乳中，能够抑制 pancreatic lipase 的活性。
TN1641	(-)-Fenchone	Others; Antioxidant; Antifungal	Microbiology/Virology; Others; oxidation-reduction
	(-)-Fenchone 是一种双环单萜类化合物，广泛分布于植物中，可从Foeniculum vulgare 和Peumus boldus 中提取。(-)-Fenchone 具有广泛的生物活性，包括抗氧化，伤口愈合，止泻，抗真菌，抗伤害感受和支气管扩张剂活性。(-)-Fenchone 是一种潜在的抗肿瘤化合物。
T4513	Vanillyl butyl ether 4-(Butoxymethyl)-2-methoxyphenol,香兰醇丁醚,Butyl vanillyl ether,香草醇丁醚	Others	Others
	Vanillyl butyl ether (Butyl vanillyl ether) 是香草特有风味和香气的来源。它是辣椒素类似物，对人体有感官刺激作用。它是环保且无毒的物质。它是烷氧基取代的苄基衍生物，主要用作调味剂。
T19317	Ethyl phenylacetate	Others	Others
	Ethyl phenylacetate 是天然香料，其感官阈值接近 73 µg/L。它可使葡萄酒具有强烈的蜂蜜样特性。它是一种毒性较小且对环境更友好的溶剂，是非诱变性的，并且是犹太食品添加剂。
T34885	Tinyatoxin TNX,TTN,TTX
	Tinyatoxin is a neurotoxin that works through vanillin receptors on sensory nerves.
T40543	3-Furanmethanol
	3-Furanmethanol is a furan compound exhibiting diverse sensory properties. Efficient and highly regioselective photocycloaddition reactions occur between 3-Furanmethanol and 2-cyanonaphthalenes.

天然产物

6-Hydroxyflavanone

Cat.No: TN1308

Target: Others, Lipoxygenase, COX, GABA Receptor

Cat.No: T5S1389

Synonym: 七叶皂苷B,七叶皂苷 IB

Target: 5-HT Receptor, NO Synthase

Cat.No: TN1641

Target: Others, Antioxidant, Antifungal

Vanillyl butyl ether

Cat.No: T4513

Synonym: 4-(Butoxymethyl)-2-methoxyphenol,香兰醇丁醚,Butyl vanillyl ether,香草醇丁醚

Target: Others

Ethyl phenylacetate

Cat.No: T19317

Target: Others

Cat.No: T34885

Synonym: TNX,TTN,TTX

3-Furanmethanol

Cat.No: T40543

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