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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T0957	Isradipine PN 200-110,伊拉地平	Calcium Channel; Autophagy	Autophagy; Membrane transporter/Ion channel; Metabolism
	Isradipine (PN 200-110) 是一种二氢吡啶类钙通道阻滞剂，具有抗高血压和血管扩张活性。它是一种具有口服活性的 L 型钙通道阻滞剂，也是一种潜在可行的帕金森病神经保护剂。
T21447	Tolazoline Priscol,妥拉苏林,Priscoline,Pridazole,Divascol,Vasimid,Benzalolin	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Tolazoline (Benzalolin) 是一种竞争性的α-肾上腺素受体拮抗剂。
T16411	Otenzepad AF-DX 116	AChR	Neuroscience
	Otenzepad (AF-DX 116) 是 M2 mAChR 的特异性拮抗剂，对大鼠心脏和兔外周肺的 IC50 分别为 386 nM 和 640 nM。
T10244	ACY-1083	HDAC	Chromatin/Epigenetic; DNA Damage/DNA Repair
	ACY-1083 是一种选择性和脑穿透性 HDAC6 抑制剂 (IC50：3 nM)，可有效逆转化疗引起的周围神经病变。
T0806	Flunarizine dihydrochloride Flunarizine 2HCl,KW-3149,R14950,盐酸氟桂利嗪	Calcium Channel; Dopamine Receptor; Sodium Channel	GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Neuroscience
	Flunarizine dihydrochloride (R14950) 是 Na+/Ca2+(T 型) 通道双重阻滞剂。它也是 D2多巴胺受体拮抗剂。它具有用于扩张外周血管和预防偏头痛的潜力。
T5385	Radiprodil RGH-896	NMDAR; iGluR	Membrane transporter/Ion channel; Neuroscience
	Radiprodil (RGH-896) 是一种具有口服活性的、NMDA 受体 NR2B 亚类的选择性拮抗剂。它有用于神经性疼痛和其它慢性疼痛的相关研究潜力。
T2371	Emapunil AC-5216,XBD-173	Others	Others
	Emapunil (XBD-173) 是一种选择性的、口服有效的TSPO(一种线粒体苯二氮受体) 的配体。在多种动物模型中，它显示出抗焦虑和抗抑郁特性。
T10998	Deriglidole SL 86-0715	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Deriglidole (SL 86-0715) 是一种外周肾上腺素能受体拮抗剂，是一种具有选择性的α2受体抑制剂。 Deriglidole 对可乐定和 Idazoxan 有抑制作用而对哌唑嗪与大鼠皮质和人血小板α2-肾上腺素能受体不显示活性。
T10073	2-Iodomelatonin	Melatonin Receptor	GPCR/G Protein
	2-Iodomelatonin 是褪黑激素受体 1 (MT1) 的强效激动剂，Ki 为 28 pM，对 MT1的选择性是 MT2 的 5 倍以上。2-Iodomelatonin 可用于鉴定，表征和定位脑和周围组织的褪黑激素结合位点。
TP1918L1	Lys-[Des-Arg9]Bradykinin acetate Lys-[Des-Arg9]Bradykinin acetate (71800-36-7 free base)	Bradykinin Receptor	GPCR/G Protein
	Lys-[Des-Arg9]Bradykinin acetate (71800-36-7 free base) 是一种内源性强效和高选择性的缓激肽 B1 受体激动剂（对人 B1 和 B2 受体的 Ki 值分别为 0.12 和 > 30000 nM）。降低体内外周血管阻力的降压药。比 [Des-Arg9]-缓激肽强 16 倍。
TP1918L	Lys-[Des-Arg9]Bradykinin,TFA Lys-[Des-Arg9]Bradykinin,TFA 71800-36-7(fb-tfa)	Bradykinin Receptor	GPCR/G Protein
	Lys-[Des-Arg9]Bradykinin,TFA (71800-36-7 free base) 是内源性强效和高选择性的缓激肽 B1 受体激动剂（对人 B1 和 B2 受体的 Ki 值分别为 0.12 和 > 30000 nM）。降低体内外周血管阻力的降压药。比 [Des-Arg9]-缓激肽强 16 倍。
T13664	DSP-4 hydrochloride Neurotoxin DSP 4 (hydrochloride)	Others	Others
	DSP-4 hydrochloride (Neurotoxin DSP 4 (hydrochloride)) 是一种高选择性的神经毒素，主要是来自蓝斑 (LC) 的神经元，容易通过血脑屏障。它对成年和发育中大鼠去甲肾上腺素能神经元具有神经毒性作用，可用于中枢和外周去甲肾上腺素能神经元的暂时选择性降解。
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。
T1050	Prazosin hydrochloride Prazosin hydrochloride,哌唑嗪盐酸盐,Prazosin HCl,cp-12299-1,Peripress,Vasoflex,盐酸哌唑嗪,Minipress	Potassium Channel; MRP; Adrenergic Receptor; ABC; Autophagy	Autophagy; GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Neuroscience
	Prazosin hydrochloride (Vasoflex) 是一种选择性肾上腺素能 α-1 拮抗剂，可降低外周阻力并放松血管平滑肌。它可用于研究高血压和酒精使用障碍。它是一种合成哌嗪衍生物，具有降压抗肾上腺素能特性。它抑制有机阳离子转运蛋白 OCT-1 和 OCT-3，IC50分别为 1.8 和 13 μM 。
TP1992L	M40 acetate(143896-17-7 free base)	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	M40 acetate(143896-17-7 free base) 是一种有效的、非选择性的甘丙肽受体拮抗剂（GAL1 和 GAL2 的 Ki 值分别为 1.82 和 5.1 nM），在体外抑制大鼠脑中甘丙肽 (1-29) 的结合 (IC50 = 3 - 15 nM)。减弱氟西汀的抗抑郁作用并阻止甘丙肽诱导的体内食物摄入。在剂量 > 100 nM 时，对外周 GAL2 受体也表现出较弱的部分激动剂活性。
T3173	DAA-1106 DAA1106	Others; GABA Receptor	Membrane transporter/Ion channel; Neuroscience; Others
	DAA-1106是外周苯二氮受体激动剂。
T25102	Aprikalim RP52891,RP-52891,RP 52891
	Aprikalim is a specific and selective ATP-sensitive K+ (KATP) channel opener. Aprikalim affords cardioprotection and at higher doses also cause peripheral or coronary vasodilatation.
T21392	Flunarizine Flunarizinum,Flunarizin,Sibelium,Flunarizina,R-14950
	Flunarizine is a non-selective calcium entry blocker and a histamine H1 receptor blocker. It is effective in the prophylaxis of migraine, occlusive peripheral vascular disease, vertigo of central and peripheral origin, and as an adjuvant in the therapy of
T27324	FK614 FK 614,ATx-08-001,ATx-08001,FK-614
	FK-614 is a selective agonist of peroxisome proliferator-activated receptor gamma. FK-614 improves peripheral glucose utilization while decreases hepatic insulin extraction in alloxan-induced diabetic dogs.
T11323L	Frakefamide	Others	Others
	Frakefamide is a potent analgesic. It acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system.
T29933	AM-1714 UNII-E3OY6PCU04,AM1714
	AM-1714 is a reasonable selective agonist for the peripheral cannabinoid receptor CB2. In animal studies, it has been shown to have analgesic and anti-abnormal pain effects.
T11482	GSK2245035	Others	Others
	GSK2245035 is a highly selective intranasal TLR7 agonist with preferential Type-1 interferon (IFN)-stimulating properties (pEC50s: 9.3 and 6.5 for IFNα and TFNα). It effectively suppresses allergen-induced Th2 cytokine production in human peripheral blood
T28335	PD 140376 PD-140376,PD140376
	PD 140376 is a highly selective antagonist radioligand for the cholecystokinin(B)-gastrin receptor in guinea pig gastric mucosa & cerebral cortex in the peripheral and central nervous systems.
T14570	BI 99179 BI99179	Fatty Acid Synthase	Metabolism
	BI99179 is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC50 of 79 nM and it exhibits significant exposure (both peripheral and central) upon oral administration in rats[1].
T14938	CGP 36742 SGS-742	GABA Receptor	Membrane transporter/Ion channel; Neuroscience
	CGP 36742 is a selective antagonist of the GABAB receptor that can penetrate the blood-brain barrier after peripheral administration (IC50: 32 μM). It is useful in the treatment of depression.
TQ0002L	A-317491 sodium A-317491,A 317491,A317491
	A-317491 is an effective selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, which reverses inflammatory mechanical hyperalgesia and relieves chronic inflammation and neuropathic pain in rats by acting on peripheral receptors.
T33583	Naldemedine S-297995,S297995,Naldemedine,S 297995,S297,995,S 297,995,S297,995;Naldemedine,S-297,995
	Naldemedine (S 297995) is a peripheral selective μ-opioid receptor antagonist being developed by Shionogi for the treatment of opioid-induced adverse reactions, including constipation, nausea, and vomiting. They are usually well tolerated, mainly with mil
T11323	Frakefamide TFA (188196-22-7 free base) Frakefamide TFA	Others	Others
	Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system. Frakefamide TFA is a potent analgesic that acts as a peripheral active μ-selective receptor agonist.
T28850	SR57227A SR 57227A,SR-57227A
	SR 57227A is a highly selective of peripheral and central 5-HT3 receptors and an inhibitor of NMDA receptor-mediated responses in rat cortical pyramidal cells. It exhibits anti-depressant like effects in rats and decreased isolation-induced aggressive beh
T14374	AZD2906
	AZD2906, a selective glucocorticoid receptor (GR) agonist, demonstrates inhibitory concentrations (IC50s) of 2.2 nM in human GR, 0.3 nM in rat peripheral blood mononuclear cells (PBMC), 41.6 nM in human whole blood, and 7.5 nM in rat whole blood, respectively[1]. Additionally, it induces an increase in micronucleated immature erythrocytes within rat bone marrow.
T41183	Helianorphin-19
	Helianorphin-19 is a high affinity, potent and selective κ-opioid receptor (KOR) agonist (Ki = 25 nM; EC50= 45 nM). Helianorphin-19 exhibits approximately 200-fold selectivity for KOR over μ and δ-opioid receptors.In vivoHelianorphin-19 shows potent peripheral analgesic efficacy in a mouse model of visceral pain without affecting motor coordination/sedation.
TP1918	Lys-[Des-Arg9]Bradykinin
	Endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. 16-fold more potent than [Des-Arg9]
T79303	IACS-52825
	IACS-52825是一种选择性DLK抑制剂，具有1.3 nM的Kd值，适用于研究化疗引起的周围神经病变。
T73655	Frakefamide TFA
	Frakefamide TFA 是一种有效的止痛药物，作为μ 受体的选择性外围激动剂。该化合物不能穿透血脑屏障，因此不进入中枢神经系统。
T61850	Adenosine receptor inhibitor 1
	Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR). It exhibits exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties. Therefore, Adenosine receptor inhibitor 1 holds great promise for investigating cancer and neurodegenerative diseases [1].
TP1992	M40
	Potent, non-selective galanin receptor antagonist (Ki values are 1.82 and 5.1 nM at GAL1 and GAL2 respectively) that inhibits galanin (1-29) binding in rat brain in vitro (IC50 = 3 - 15 nM). Attenuates the antidepressant effects of fluoxetine and blocks galanin-induced food intake in vivo. Also exhibits weak partial agonist activity at peripheral GAL2 receptors at doses > 100 nM.
T79195	Cav 3.2 inhibitor 4	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Cav 3.2 inhibitor 4 (compound 21) 是高效的选择性 T 型钙通道 (Cav3.2) 抑制剂，具有外周限制性，其 IC50 值为 0.6 μM，适用于心房颤动研究。
T36109	L Moses dihydrochloride
	High affinity and selective cell-permeable p300/CBP-associated factor (PCAF) inhibitor (Ki = 47 nM). Exhibits no significant activity against a panel of 48 other bromodomains except GCN5 (Kd = 600 nM). Exhibits >4500-fold selectivity for PCAF over BRD4. Also exhibits metabolic stability in mouse and human liver microsomes and no observable cytotoxicity in peripheral blood mononuclear cells (PBMC). Moustakim et al (2017) Discovery of a PCAF bromodomain chemical probe. Angew.Chem.Int.Ed. 56 827 P...
T21411	Isoproterenol Norisodrine,Isoprenaline,Novodrin,Isuprel,Medihaler-Iso	Endogenous Metabolite; Adrenergic Receptor	GPCR/G Protein; Metabolism; Neuroscience
	Isoproterenol (Norisodrine) 是一种非选择性且具有口服活性的 β-肾上腺素受体激动剂。Isoproterenol 是有效的外周血管扩张剂和支气管扩张剂。Isoproterenol 可用于研究心动过缓和支气管哮喘，用于治疗心脏传导阻滞、心动过缓。
T62541	AChE-IN-22
	AChE-IN-22 (compound 10q) 是一种乙酰胆碱酯酶 (AChE) 的选择性抑制剂，能够作用于 AChE (IC50: 0.88 μM) 和 BuChE (IC50: 10 μM)。AChE-IN-22 能够同时与 AChE 的 CAS (catalytic active site) 和 PAS (peripheral anionic site) 位点结合，可用于研究阿尔茨海默病。
T73522	CR 665 FE 200665,JNJ 38488502 ; FE 200665,JNJ 38488502
	CR 665 (JNJ 38488502) 是一种外周选择性κ-阿片类激动剂。CR 665可以激活 kappa 阿片受体 EC50值为10.9 nM。CR 665 可用于外周疼痛的研究。
T82515	E104
	E104（compound 1）为一种高效且选择性的TLR7激动剂，适用于ADC合成，以激发显著的抗癌活性。该化合物能够诱导小鼠巨噬细胞与hPBMC的活化。
T63173	BTK-IN-8
	BTK-IN-8 是一种有效的、选择性的、外周共价 BTK 抑制剂，其 IC50 值为 0.22 nM，Kd 值为 0.91 nM。BTK-IN-8 表现出良好的全血 CD69 细胞效力，其 IC50 值为 0.029 μM。
T40572	Lesogaberan napadisylate AZD-3355 napadisylate
	Lesogaberan (AZD-3355) napadisylate is a potent and selective agonist of GABA B receptors, with an EC 50 of 8.6 nM for human recombinant GABA B receptors. It demonstrates an affinity (Ki) of 5.1 nM for rat GABA B receptors and 1.4 μM for GABA A receptors, as determined by its displacement of [3H]GABA binding in brain membranes. Notably, Lesogaberan napadisylate exerts a peripheral mode of action, inhibiting transient lower esophageal sphincter relaxation.
T62732	S1P1 agonist 5
	S1P1 agonist 5 是一种选择性的、口服具有活力的 S1P1 激动剂。S1P1 agonist 5 可以抑制淋巴细胞从淋巴组织排出到外周血。S1P1 agonist 5 具有潜力进行多发性硬化症 (MS) 的研究。
T63287	HPK1-IN-3
	HPK1-IN-3 是一种选择性的、有效的、ATP 竞争性的造血祖细胞激酶 1 (HPK1; MAP4K1) 抑制剂 (IC50: 0.25 nM)。HPK1-IN-3 具有 IL-2 细胞效力，能够作用于人外周血单核细胞 (PBMC)，EC50 值为 108 nM。
T71955	C3001a
	C3001a is a selective activator for TREK, against other two-pore domain K+(K2P) channels. C3001a binds to the cryptic binding site formed by P1 and TM4 in TREK-1. C3001a targets TREK channels in the peripheral nervous system to reduce the excitability of nociceptive neurons. In neuropathic pain, C3001a alleviated spontaneous pain and cold hyperalgesia. In a mouse model of acute pancreatitis, C3001a alleviated mechanical allodynia and inflammation. C3001a represents a lead compound which could a...
T69081	KRH-1636
	KRH-1636 is an orally active, selective and extremely potent CXC chemokine receptor 4 antagonist. KRH-1636 exhibits a potent and selective anti-HIV-1 activity. KRH-1636 efficiently blocked replication of various T cell line-tropic (X4) HIV type 1 (HIV-1) in MT-4 cells and peripheral blood mononuclear cells through the inhibition of viral entry and membrane fusion via the CXC chemokine receptor (CXCR)4 coreceptor but not via CC chemokine receptor 5. KRH-1636 also inhibits binding of the CXC chem...
T37273	BLX3887
	BLX3887 is an inhibitor of 15-lipoxygenase type 1 (15-LO-1; IC50 = 32 nM in a cell-free enzyme assay).1 It is selective for 15-LO-1 over 15-LO-2, which it does not inhibit, 5-LO (IC50 = 472 nM), and 12-LO (IC50 = 3,310 nM). BLX3887 inhibits the production of 15-LO metabolites selectively in eosinophils over neutrophils when used at a concentration of 10 μM. It also inhibits endocytosis in, and the migration of, isolated human peripheral blood mononuclear cell-derived dendritic cells in vitro. \|1...
T37523	Tenofovir diphosphate (sodium salt)
	Tenofovir diphosphate is an inhibitor of HIV reverse transcriptase (Kis = 0.022 and 1.55 μM for RNA and DNA, respectively) and hepatitis B virus (HBV) polymerase (Ki = 0.18 μM). It is selective for these enzymes over DNA polymerase α and β, as well as mitochondrial DNA polymerase γ (Kis = 5.2, 81.7, and 59.5 μM, respectively). Tenofovir diphosphate is formed intracellularly through phosphorylation of the prodrugs tenofovir and tenofovir disoproxil by nucleotide kinases. Increased levels of tenof...

化合物

Cat.No: T0957

Synonym: PN 200-110,伊拉地平

Target: Calcium Channel, Autophagy

Cat.No: T21447

Synonym: Priscol,妥拉苏林,Priscoline,Pridazole,Divascol,Vasimid,Benzalolin

Target: Adrenergic Receptor

Cat.No: T16411

Synonym: AF-DX 116

Target: AChR

Cat.No: T10244

Target: HDAC

Flunarizine dihydrochloride

Cat.No: T0806

Synonym: Flunarizine 2HCl,KW-3149,R14950,盐酸氟桂利嗪

Target: Calcium Channel, Dopamine Receptor, Sodium Channel

Cat.No: T5385

Synonym: RGH-896

Target: NMDAR, iGluR

Cat.No: T2371

Synonym: AC-5216,XBD-173

Target: Others

Cat.No: T10998

Synonym: SL 86-0715

Target: Adrenergic Receptor

2-Iodomelatonin

Cat.No: T10073

Target: Melatonin Receptor

Lys-[Des-Arg9]Bradykinin acetate

Cat.No: TP1918L1

Synonym: Lys-[Des-Arg9]Bradykinin acetate (71800-36-7 free base)

Target: Bradykinin Receptor

Lys-[Des-Arg9]Bradykinin,TFA

Cat.No: TP1918L

Synonym: Lys-[Des-Arg9]Bradykinin,TFA 71800-36-7(fb-tfa)

Target: Bradykinin Receptor

DSP-4 hydrochloride

Cat.No: T13664

Synonym: Neurotoxin DSP 4 (hydrochloride)

Target: Others

Alosetron hydrochloride

Cat.No: T2525

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

Target: 5-HT Receptor

Prazosin hydrochloride

Cat.No: T1050

Synonym: Prazosin hydrochloride,哌唑嗪盐酸盐,Prazosin HCl,cp-12299-1,Peripress,Vasoflex,盐酸哌唑嗪,Minipress

Target: Potassium Channel, MRP, Adrenergic Receptor, ABC, Autophagy

M40 acetate(143896-17-7 free base)

Cat.No: TP1992L

Target: Neuropeptide Y Receptor

Cat.No: T3173

Synonym: DAA1106

Target: Others, GABA Receptor

Cat.No: T25102

Synonym: RP52891,RP-52891,RP 52891

Cat.No: T21392

Synonym: Flunarizinum,Flunarizin,Sibelium,Flunarizina,R-14950

Cat.No: T27324

Synonym: FK 614,ATx-08-001,ATx-08001,FK-614

Cat.No: T11323L

Target: Others

Cat.No: T29933

Synonym: UNII-E3OY6PCU04,AM1714

Cat.No: T11482

Target: Others

Cat.No: T28335

Synonym: PD-140376,PD140376

Cat.No: T14570

Synonym: BI99179

Target: Fatty Acid Synthase

Cat.No: T14938

Synonym: SGS-742

Target: GABA Receptor

A-317491 sodium

Cat.No: TQ0002L

Synonym: A-317491,A 317491,A317491

Cat.No: T33583

Synonym: S-297995,S297995,Naldemedine,S 297995,S297,995,S 297,995,S297,995;Naldemedine,S-297,995

Frakefamide TFA (188196-22-7 free base)

Cat.No: T11323

Synonym: Frakefamide TFA

Target: Others

Cat.No: T28850

Synonym: SR 57227A,SR-57227A

Cat.No: T14374

Helianorphin-19

Cat.No: T41183

Lys-[Des-Arg9]Bradykinin

Cat.No: TP1918

Cat.No: T79303

Frakefamide TFA

Cat.No: T73655

Adenosine receptor inhibitor 1

Cat.No: T61850

Cat.No: TP1992

Cav 3.2 inhibitor 4

Cat.No: T79195

Target: Calcium Channel

L Moses dihydrochloride

Cat.No: T36109

Cat.No: T21411

Synonym: Norisodrine,Isoprenaline,Novodrin,Isuprel,Medihaler-Iso

Target: Endogenous Metabolite, Adrenergic Receptor

Cat.No: T62541

Cat.No: T73522

Synonym: FE 200665,JNJ 38488502 ; FE 200665,JNJ 38488502

Cat.No: T82515

Cat.No: T63173

Lesogaberan napadisylate

Cat.No: T40572

Synonym: AZD-3355 napadisylate

Cat.No: T62732

Cat.No: T63287

Cat.No: T71955

Cat.No: T69081

Cat.No: T37273

Tenofovir diphosphate (sodium salt)

Cat.No: T37523

Cat. No.	Product Name	Target	Signaling Pathways
TN2322	Yangambin	Calcium Channel; PAFR	GPCR/G Protein; Membrane transporter/Ion channel; Metabolism
	Yangambin 是从诸如番荔枝科植物中分离出来的呋喃木脂素，是选择性PAF 受体拮抗剂，通过调控Ca2+通道抑制 Ca2+流入，导致 [Ca2+]i 在血管平滑肌细胞和随后的外周血管舒张中减少，具有降压作用。

天然产物

Cat.No: TN2322

Target: Calcium Channel, PAFR

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