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31

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T2562	Eltrombopag SB-497115,SB-497115-GR,艾曲波帕	Thrombin	Proteases/Proteasome
	Eltrombopag (SB-497115-GR) 是一种具有巨核细胞生成刺激活性的口服活性血小板生成素受体激动剂，可结合并刺激血小板血小板生成素受体，用于血小板减少的某些病症研究。
T0182L	Clopidogrel hydrogen sulfate 硫酸氢氯吡格雷,(S)-(+)-Clopidogrel hydrogen sulfate,(S)-(+)-Clopidogrel bisulfate,SR-25990C,Clopidogrel,硫酸氯吡格雷	P450; P2Y Receptor	GPCR/G Protein; Metabolism; Neuroscience
	Clopidogrel hydrogen sulfate ((S)-(+)-Clopidogrel bisulfate) 是一种抗血小板药物，可防止血栓形成。它抑制 CYP2B6和 CYP2C19，IC50分别为 18.2 和 524 nM。它是一种选择性的高亲和力 P2Y12 受体拮抗剂，可抑制纤维蛋白原与血小板的结合以及血小板的粘附和聚集。
T6825	Eltrombopag Olamine Promacta Olamine,Revolade,艾曲泊帕乙醇胺盐,Eltrombopag diethanolamine salt,SB497115,艾曲波帕乙醇胺盐,SB-497115GR	Thrombin	Proteases/Proteasome
	Eltrombopag Olamine (Eltrombopag diethanolamine salt) 是 Eltrombopag 的口服活性乙醇胺盐，是一种血小板生成素(TPO)受体激动剂，用于血小板减少的某些病症研究。
T1667	Tandutinib MLN518,CT53518,NSC726292,坦度替尼	Apoptosis; FLT; CSF-1R; PDGFR; Src; c-Kit	Angiogenesis; Apoptosis; Tyrosine Kinase/Adaptors
	Tandutinib (CT53518) 是一种选择性 FLT3抑制剂，其 IC50为 0.22 μM。它还抑制c-Kit 和PDGFR，其IC50分别为 0.17 μM 和 0.20 μM。它可穿透血脑屏障，用于急性骨髓性白血病。
T15108	DG-041	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	DG-041 是高亲和力，选择性的，有效的 EP3受体拮抗剂，在结合和 FLIPR 试验中，IC50分别为 4.6 nM 和 8.1 nM。DG-041通过抑制 PGE2促进血小板聚集。DG-041具有血脑屏障渗透性。
T3616	Carbazochrome AC-17,Adrenostazin,Cromadrenal,Adona,Adchnon,卡巴克络,Adedolon	Others; Phospholipase	Metabolism; Others
	Carbazochrome (Adchnon) 是毛细管稳定剂，是抗出血剂，用于研究出血。
T17039	Terbogrel BIBV 308SE	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Terbogrel 是一种可口服的、具有选择性 thromboxane A2 受体拮抗剂（IC50 约为 10 nM），是一种 thromboxane A2 synthase 抑制剂（IC50 约为 10 nM）。Terbogrel 是一种抗血小板化合物，可抑制血小板聚集，是预防血栓的潜在化合物。
T6040	Aloxistatin E64d,Loxistatin,阿洛司他丁,E64c ethyl ester	SARS-CoV; Cysteine Protease	Microbiology/Virology; Proteases/Proteasome
	Aloxistatin (E64d) 是一种不可逆的、可透过膜的溶酶体和细胞溶质半胱氨酸蛋白酶抑制剂，能够抑制完整血小板中的钙蛋白酶活性。它是一种半胱氨酸蛋白酶抑制剂，具有血小板聚集抑制活性。
T3536	AZD1283	P2Y Receptor	GPCR/G Protein; Neuroscience
	AZD1283是P2Y12受体拮抗剂，EC50为3.0 ug/kg/min，结合的IC50为11 nM。它剂量依赖性地诱导血流量增加和抑制 ADP 诱导的血小板聚集，抗血栓形成的 ED50 值分别为 3.0 和 10 μg/kg/min。
T70423	Imolamine hydrochloride
	Imolamine hydrochloride is a blood platelet aggregation antagonist.
T69457	Imolamine
	Imolamine is a blood platelet aggregation antagonist.
T68902	Talosalate
	Talosalate is an inhibitor of blood platelet aggregation.
T36213	16,16-dimethyl Prostaglandin D2 16,16-dimethyl Prostaglandin D2
	16,16-dimethyl PGD2 is a metabolically stable synthetic analog of PGD2. It enhances ADP-induced human platelet aggregation and increases systemic blood pressure in rats.
T35725	4-hydroxy Valsartan
	4-hydroxy Valsartan is a major metabolite of the angiotensin II type 1 (AT1) receptor antagonist valsartan . It reduces platelet aggregation induced by epinephrine and collagen but not ADP in human whole blood.
T33431	MK-287 L680573,L 680573,L-680573
	MK-287 (L-680573) is a platelet activator (PAF) antagonist that effectively inhibates the binding of [3H]C18-PAF to human platelets, polynucleated white blood cells (PMN), and pulmonary membranes. May be used to treat asthma,
T26932	BX 667 BX-667,BX667
	BX 667 is a P2Y12 receptor antagonist. BX 667 blocks ADP-induced platelet aggregation in human, dog and rat blood with IC50 value of 97, 317 and 3000 nM respectively.
T35417	α-Linolenic Acid (sodium salt)
	α-Linolenic acid (ALA) is an essential fatty acid found in leafy green vegetables. ALA, as part of a low saturated fat diet, helps prevent cardiovascular disease. ALA decreases blood pressure, serum cholesterol levels, and platelet aggregation.
T35867	TRAP-6 Peptide (trifluoroacetate salt)
	TRAP-6 peptide is a hexapeptide corresponding to residues 42-47 of protease-activated receptor 1 (PAR1). It acts as an agonist of PAR1, inducing platelet aggregation in human platelet-rich plasma ex vivo (EC50 = 0.8 μM). TRAP-6 (0.3 and 0.6 mg/kg) has a triphasic effect on mean arterial blood pressure (MAP) in anesthetized rats with a short decrease, an increase, and then a longer decrease in MAP following intravenous administration.
T81234	S-(1,2-Dicarboxyethyl)glutathione
	S-(1,2-Dicarboxyethyl)glutathione为多肽类化合物，具有抑制血液凝固与血小板聚集的功能。
T36153	15(S)-15-methyl Prostaglandin D2 15(S)-15-methyl Prostaglandin D2
	15(S)-15-methyl Prostaglandin D2 (15(S)-15-methyl PGD2) is a metabolically stable synthetic analog of PGD2 . In contrast to PGD2, 15(S)-15-methyl PGD2 induces vasoconstriction and increases systemic blood pressure with much reduced inhibitory activity on ADP-induced platelet aggregation. It also exhibits strong antifertility activity in hamsters (200-fold more potent than PGD2).
T36160	8-iso Prostaglandin E2 8-iso Prostaglandin E2
	8-iso PGE2 is one of several isoprostanes produced from arachidonic acid during lipid peroxidation. It is a potent renal vasoconstrictor in the rat. 8-iso PGE2 inhibits U-46619 or I-BOP-induced platelet aggregation with IC50 values of 0.5 and 5 μM, respectively. When infused into the renal artery of the rat at a concentration of 4 μg/kg/min, 8-iso PGE2 decreases the GFR and renal plasma flow by 80% without affecting blood pressure.
T35990	ent-8-iso-15(S)-Prostaglandin F2α ent-8-iso-15(S)-Prostaglandin F2α
	Isoprostanes are produced by the non-enzymatic, free radical peroxidation of phospholipid-esterified arachidonic acid. They have been used as biomarkers of oxidative stress, but they also have been found to have potent biological activity. ent-8-iso-15(S)-Prostaglandin F2α (ent-8-iso-15(S)-PGF2α) is a potent vasoconstrictor of porcine retinal and brain microvessels with EC50 values of 15 and 24 nM, respectively. This isoprostane is about ten-fold more potent than 8-iso-PGF2α in a whole blood pla...
T71300	Pentoxifylline-d6
	Pentoxifylline-d6 is intended for use as an internal standard for the quantification of pentoxifylline by GC- or LC-MS. Pentoxifylline is a hemorrheologic agent. It increases the deformability of washed isolated human erythrocytes when used at a concentration of 100 µM. Pentoxifylline (1, 2, and 3 mM) inhibits ADP-induced platelet aggregation in isolated human whole blood. It inhibits thrombus formation induced by ADP in a hamster cheek pouch model when administered at doses of 5, 10, and 20 mg/...
T15757	Limaprost 17α,20-dimethyl-δ2-PGE1,利马前列素,OP1206,ONO1206	PGE Synthase	Immunology/Inflammation
	Limaprost (17α,20-dimethyl-δ2-PGE1) 是PGE1类似物，也是口服具有活性的血管舒张剂。它能够增加血流量以及减少血小板聚集。它具有抗心绞痛的功能，可用于疼痛的缓解，以及用于研究缺血性症状。
T35600	NO-Losartan A
	Angiotensin II is a hormone that plays an important role in regulating blood pressure. Elevated levels of angiotensin II are implicated in inducing and maintaining hypertension, and also in the development of atherosclerosis. Both of these effects are mediated by the angiotensin II type 1 (AT1) receptor. Losartan is a mammalian AT1 receptor antagonist with a Ki value of 5-20 nM. In humans, losartan effectively controls hypertension while protecting renal function. Nitric oxide (NO) causes vasodi...
T17231	Vicagrel	Others	Others
	Vicagrel 是一种有效的、具有口服活性抗血小板化合物，通过不可逆地抑制 P2Y12 受体，降低代谢失活，增强了阿司匹林对啮齿类动物血小板聚集和血栓形成起抑制作用。Viagrel 可用于治疗冠状动脉疾病、外周血管疾病和脑血管疾病中血栓。
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...
T81609	omega-3 Arachidonic acid ethyl ester (all-Z)-8,11,14,17-Eicosatetraenoic acid ethyl ester,ω-3 Arachidonic acid ethyl ester
	omega-3 Arachidonic Acid ethyl ester 是一种少见的多不饱和脂肪酸，饮食来源稀少。ω-3脂肪酸对婴幼儿生长发育极为重要，能够帮助预防心脏病、血栓、高血压及炎症和自身免疫性疾病。该化合物在人血小板膜中通过抑制花生四烯酰辅酶A合成酶发挥作用，Ki值达到14 μM；同时在小牛脑提取物中也表现出抑制作用，IC50大约5 μM。omega-3 Arachidonic Acid ethyl ester 作为游离酸的亲脂性更强的形式，具备独特的生物活性。
T83785	2-Chloroadenosine-5'-O-diphosphate sodium 2-chloro ADP
	2-Chloroadenosine-5'-O-diphosphate是一种腺苷5'二磷酸（ADP）的衍生物。它在浓度依赖性的方式下，促进了人类富含血小板的血浆中的聚集，并抑制了由前列腺素E2（PGE2）诱导的环磷酸腺苷（cAMP）的产生。2-Chloroadenosine-5'-O-diphosphate引起预收缩的孤立的豚鼠taenia coli条带放松（pD2 = 6.74），降低大鼠的动脉血压。此外，它还抑制了热休克蛋白70（Hsp70）家族成员mortalin的ATP酶活性（人类酶的表观Ki = 45.05 µM）。
T38171	Ro 1138452 hydrochloride
	Selective prostacyclin IP receptor antagonist (pKi = 8.3). Exhibits no affinity at other prostanoid receptors (EP1-4, FP and TP) in a radioligand binding assay. Demonstrates analgesic activity in rats. Orally bioavailable. Clark et al (2004) Discovery and SAR development of 2-(phenylamino) imidazolines as prostacyclin receptor antagonists. Bioorg.Med.Chem.Lett. 14 1053 PMID:15013022 \|Jones et al (2006) Investigation of the prostacyclin (IP) receptor antagonist RO1138452 on isolated blood vessel ...
T67442	CGP-53716
	The growth factors, platelet-derived growth factor (PDGF) and basic fibroblast growth factor (bFGF) play major roles in enhanced smooth muscle cells growth in rodent blood vessels after vascular injury. Tyrosine kinase inhibition has been shown to be effective in blocking tyrosine phosphorylation at the PDGF and bFGF receptors in cultured fibroblast and vascular smooth muscle cells which in turn inhibits their proliferation[1]. CGP 53716 is a specific PDGFR tyrosine kinase inhibitor on SMC (smoo...

化合物

Cat.No: T2562

Synonym: SB-497115,SB-497115-GR,艾曲波帕

Target: Thrombin

Clopidogrel hydrogen sulfate

Cat.No: T0182L

Synonym: 硫酸氢氯吡格雷,(S)-(+)-Clopidogrel hydrogen sulfate,(S)-(+)-Clopidogrel bisulfate,SR-25990C,Clopidogrel,硫酸氯吡格雷

Target: P450, P2Y Receptor

Eltrombopag Olamine

Cat.No: T6825

Synonym: Promacta Olamine,Revolade,艾曲泊帕乙醇胺盐,Eltrombopag diethanolamine salt,SB497115,艾曲波帕乙醇胺盐,SB-497115GR

Target: Thrombin

Cat.No: T1667

Synonym: MLN518,CT53518,NSC726292,坦度替尼

Target: Apoptosis, FLT, CSF-1R, PDGFR, Src, c-Kit

Cat.No: T15108

Target: Prostaglandin Receptor

Cat.No: T3616

Synonym: AC-17,Adrenostazin,Cromadrenal,Adona,Adchnon,卡巴克络,Adedolon

Target: Others, Phospholipase

Cat.No: T17039

Synonym: BIBV 308SE

Target: Prostaglandin Receptor

Cat.No: T6040

Synonym: E64d,Loxistatin,阿洛司他丁,E64c ethyl ester

Target: SARS-CoV, Cysteine Protease

Cat.No: T3536

Target: P2Y Receptor

Imolamine hydrochloride

Cat.No: T70423

Cat.No: T69457

Cat.No: T68902

16,16-dimethyl Prostaglandin D2

Cat.No: T36213

Synonym: 16,16-dimethyl Prostaglandin D2

4-hydroxy Valsartan

Cat.No: T35725

Cat.No: T33431

Synonym: L680573,L 680573,L-680573

Cat.No: T26932

Synonym: BX-667,BX667

α-Linolenic Acid (sodium salt)

Cat.No: T35417

TRAP-6 Peptide (trifluoroacetate salt)

Cat.No: T35867

S-(1,2-Dicarboxyethyl)glutathione

Cat.No: T81234

15(S)-15-methyl Prostaglandin D2

Cat.No: T36153

Synonym: 15(S)-15-methyl Prostaglandin D2

8-iso Prostaglandin E2

Cat.No: T36160

Synonym: 8-iso Prostaglandin E2

ent-8-iso-15(S)-Prostaglandin F2α

Cat.No: T35990

Synonym: ent-8-iso-15(S)-Prostaglandin F2α

Pentoxifylline-d6

Cat.No: T71300

Cat.No: T15757

Synonym: 17α,20-dimethyl-δ2-PGE1,利马前列素,OP1206,ONO1206

Target: PGE Synthase

Cat.No: T35600

Cat.No: T17231

Target: Others

Cat.No: T37969

omega-3 Arachidonic acid ethyl ester

Cat.No: T81609

Synonym: (all-Z)-8,11,14,17-Eicosatetraenoic acid ethyl ester,ω-3 Arachidonic acid ethyl ester

2-Chloroadenosine-5'-O-diphosphate sodium

Cat.No: T83785

Synonym: 2-chloro ADP

Ro 1138452 hydrochloride

Cat.No: T38171

Cat.No: T67442

Cat. No.	Product Name	Target	Signaling Pathways
T0853	Adenosine 腺苷,D-Adenosine,Adenine riboside	Apoptosis; Nucleoside Antimetabolite/Analog; Endogenous Metabolite; Autophagy	Apoptosis; Autophagy; Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
	Adenosine (D-Adenosine) 是一种核糖核苷，由与核糖结合的腺嘌呤组成，具有血管扩张、抗心律失常和镇痛作用。
T4S1658	Benzoyloxypaeoniflorin 苯甲酰氧化芍药苷,Benzoyloxypeoniflorin,苯甲酰氧芍药苷	NF-κB; Tyrosinase	NF-κB; Proteases/Proteasome
	Benzoyloxypaeoniflorin (Benzoyloxypeoniflorin) 是一种酪氨酸酶抑制剂，分离于Paeonia suffruticosa 的根，对mushroom tyrosinase 的 IC50为 0.453 mM。它是一种NF-κB 抑制剂，它通过对血小板聚集和凝血的抑制作用，有助于改善血液循环。
T0070	Pentoxifylline Oxpentifylline,PTX,己酮可可碱,BL-191	HIV Protease; PDE; Adenosine Receptor; Autophagy	Autophagy; GPCR/G Protein; Metabolism; Microbiology/Virology; Neuroscience; Proteases/Proteasome
	Pentoxifylline (PTX) 是一种具有口服活性的磷酸二酯酶非选择性抑制剂，具有免疫调节、抗炎、抗纤溶、抗增殖和血液流变学改善作用。它可研究周围血管疾病、脑血管疾病和其他一些涉及局部微循环缺陷的疾病。
T3427	Polydatin Piceid,虎杖苷,Polydotin Peceid	Apoptosis; Mitophagy; NF-κB; Autophagy	Apoptosis; Autophagy; NF-κB
	Polydatin (Piceid) 是从传统中药虎杖根中提取的一种天然产物，在多个实验模型中具有抗炎作用。它可抑制 G6PD，并诱导氧化和内质网应激。
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。
TN5661	1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one
	1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one shows strong inhibition of collagen-induced, arachidonic acid-induced, and adenosine diphosphate-induced platelet aggregation of human whole blood.

天然产物

Cat.No: T0853

Synonym: 腺苷,D-Adenosine,Adenine riboside

Target: Apoptosis, Nucleoside Antimetabolite/Analog, Endogenous Metabolite, Autophagy

Benzoyloxypaeoniflorin

Cat.No: T4S1658

Synonym: 苯甲酰氧化芍药苷,Benzoyloxypeoniflorin,苯甲酰氧芍药苷

Target: NF-κB, Tyrosinase

Cat.No: T0070

Synonym: Oxpentifylline,PTX,己酮可可碱,BL-191

Target: HIV Protease, PDE, Adenosine Receptor, Autophagy

Cat.No: T3427

Synonym: Piceid,虎杖苷,Polydotin Peceid

Target: Apoptosis, Mitophagy, NF-κB, Autophagy

Prostaglandin E1

Cat.No: T1626

Synonym: 前列地尔,PGE1,列腺素E1,Alprostadil

Target: Endogenous Metabolite, Prostaglandin Receptor

1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one

Cat.No: TN5661

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