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18

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T0160	Anagrelide Anagrelida,Xagrid,Anagrelidum,阿那格雷	PDE	Metabolism
	Anagrelide (Xagrid) 是III 型磷酸二酯酶(PDEIII)抑制剂 (IC50=36 nM)，是咪唑喹唑啉衍生物。它能够抑制血小板生成，以及抗血栓形成作用，可用作血小板聚集抑制剂。
T2386	Pirfenidone S-7701,AMR-69,S-7701,AMR69,吡非尼酮	CCR; TGF-beta/Smad	Immunology/Inflammation; Microbiology/Virology; Stem Cells
	Pirfenidone (AMR69) 是一种抗纤维化剂，可减弱纤维细胞中CCL2和CCL12的产生。它可抑制细胞生长，并能降低人胶质瘤细胞系中的TGF-β2蛋白水平，具有抗炎活性。
T7417	Avatrombopag YM477,AKR-501,1-[3-氯-5-[[[4-(4-氯-2-噻吩基)-5-(4-环己基-1-哌嗪基)-2-噻唑基]氨基]羰基]-2-吡啶基]-4-哌啶羧酸,E5501	Thrombin; Thrombopoietin Receptor	Immunology/Inflammation; Proteases/Proteasome
	Avatrombopag (YM477) 是一种新型口服血小板生成素 (TPO) 受体激动剂，可激活 TPO 受体并增加巨核细胞增殖/分化和血小板生成。
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。
T77638	BIRM 271	Phospholipase; LTR	Immunology/Inflammation; Metabolism
	BIRM 271 是一种新型花生四烯酸释放抑制剂，可阻断白三烯B4和人中性粒细胞中的血小板活化因子生物合成。BIRM 271 和 BIRM 270 属于对映异构体，对白三烯B4 的产生有抑制作用，IC50 为40 nM。
T4092	AG126 Tyrphostin AG126,AG 126	ERK; COX	Immunology/Inflammation; MAPK; Neuroscience
	AG126 (Tyrphostin AG126) 是一种酪氨酸激酶抑制剂，可阻止丝裂原活化蛋白激酶 p42MAPK(ERK2) 的激活。
T27408	Gea 3162 Gea3162,Gea-3162
	Gea 3162 is a potent inhibitor of ADP-induced platelet aggregation in platelet rich plasma (PRP). GEA 3162 stimulates cGMP production in granulocytes, platelets, and polymorphonuclear leukocytes.
T28243	Ono 6240 Ono-6240,Ono6240
	Ono 6240 is an antagonist of platelet-activating factor. Ono 6240 prevents airway eosinophilia by inhibiting production of IL-2 and IL-5.
TP1298	Z-Gly-Gly-Arg-AMC acetate
	Z-Gly-Gly-Arg-AMC acetate is a thrombase-specific fluorescent matrix for the detection of thrombin production in PRP and poor platelet plasma (PPP).
T38257	PGDM
	Prostaglandin D2 (PGD2) plays a pharmacological role in allergic and asthmatic anaphylaxis, normal physiological sleep and lowering of body temperature, as well as inhibits platelet aggregation and relaxes vascular smooth muscle. PGDM is a major urinary metabolite of PGD2 with a unique lower sidechain that readily undergoes reversible cyclization. It is used as a biomarker to assess endogenous production of PGD2.
T72265	Eltrombopag methyl ester
	Eltrombopag methyl ester，一种Eltrombopag衍生物，为促血小板生成素(Tpo)受体激动剂，旨在促进血小板生成，用于研究特定类型的血小板减少症。
T40654	Avatrombopag hydrochloride AKR-501 hydrochloride,YM477hydrochloride,E5501hydrochloride
	Avatrombopag hydrochloride (AKR-501) is an orally active, nonpeptide agonist of the thrombopoietin (TPO) receptor with an EC 50 of 3.3 nM. It effectively mimics the biological activities of TPO, stimulating platelet production by activating the intracellular signaling system and facilitating the generation of platelets and megakaryocytes from hemopoietic precursor cells. Additionally, Avatrombopag hydrochloride serves as a substrate for cytochrome P450 (CYP) 2C9 and CYP3A.
T37382	1,2,3-Trieicosapentaenoyl-rac-glycerol
	1,2,3-Trieicosapentaenoyl-rac-glycerol (EPA-TG) is a glycerol ester of eicosapentaenoic acid , which is an ω-3 fatty acid. An EPA-TG emulsion, administered i.v., lowers leukotriene B4 production by 40% in polymorphonuclear leukocytes from rabbits and reduces platelet aggregation. It suppresses natural killer cell activity both in vitro and in vivo, in human lymphocytes and murine spleens, respectively, with the in vivo effects lasting up to seven days.
T37331	Pyrrophenone
	The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid (AA) from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins (PGs) and leukotrienes (LTs). Pyrrophenone inhibits cPLA2α with an IC50 of 4.2 nM in enzyme assays and potently blocks the release of AA and the production of PGE2 and LTC4 in cells (IC50 = 24, 25, and 14 nM, respectively). Its action is reversible and selective, as py...
T36221	2-chloro Palmitic Acid
	2-chloro Palmitic acid is a monochlorinated form of palmitic acid . It is produced in a myeloperoxidase (MPO) and time-dependent manner in neutrophils stimulated by phorbol 12-myristate 13-acetate . 2-chloro Palmitic acid (10 μM) induces neutrophil extracellular trap (NET) formation (NETosis) in human neutrophils, increasing DNA release from neutrophils, colocalization of MPO with extracellular DNA (ecDNA), and trapping of E. coli. It increases COX-2 protein levels in human coronary artery endot...
T70882	Orlistat-d3
	Orlistat-d3 is intended for use as an internal standard for the quantification of orlistat by GC- or LC-MS. Orlistat is a digestive lipase inhibitor. It inhibits diacylglycerol lipase α (DAGLα), DAGLβ, α/β-hydrolase domain-containing protein 12 (ABHD12), ABHD16A, and platelet-activating factor acetylhydrolase (PAF-AH; IC50s = 0.06, 0.1, 0.08, 0.03, and 0.05 µM, respectively), as well as pancreatic lipase and hormone-sensitive lipase (IC50s = 0.65 and 2.1 µg/ml, respectively) but does not inhibit...
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）。
T83807	Rp-Adenosine-5'-O-(1-thiotriphosphate) sodium Rp-ATP-α-S
	Rp-Adenosine-5'-O-(1-thiotriphosphate)（Rp-ATP-α-S）是一种含硫核苷酸衍生物ATP-α-S的异构体，同时也是嘌呤P2Y1受体的激动剂。在表达人类P2Y1受体的HEK293细胞中，Rp-ATP-α-S能增加钙的动员（EC50 = 75 nM）。该化合物与洗涤的人类孤立血小板结合（Ki = 156 nM），抑制由ADP引发的人类富血小板血浆（PRP）的聚集（pA2 = 4.74），并且能够抑制前列腺素E1（PGE1）在人类孤立PRP中引发的cAMP产生（pA2 = 5.26）。同时，Rp-ATP-α-S还能引起用氨基甲酰胆碱预先缩紧的豚鼠结肠条带的松弛（EC50 = 56 nM）。此外，Rp-ATP-α-S已经被用于合成被细菌核糖开关识别的环状二核苷酸。

化合物

Cat.No: T0160

Synonym: Anagrelida,Xagrid,Anagrelidum,阿那格雷

Target: PDE

Cat.No: T2386

Synonym: S-7701,AMR-69,S-7701,AMR69,吡非尼酮

Target: CCR, TGF-beta/Smad

Cat.No: T7417

Synonym: YM477,AKR-501,1-[3-氯-5-[[[4-(4-氯-2-噻吩基)-5-(4-环己基-1-哌嗪基)-2-噻唑基]氨基]羰基]-2-吡啶基]-4-哌啶羧酸,E5501

Target: Thrombin, Thrombopoietin 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: T77638

Target: Phospholipase, LTR

Cat.No: T4092

Synonym: Tyrphostin AG126,AG 126

Target: ERK, COX

Cat.No: T27408

Synonym: Gea3162,Gea-3162

Cat.No: T28243

Synonym: Ono-6240,Ono6240

Z-Gly-Gly-Arg-AMC acetate

Cat.No: TP1298

Cat.No: T38257

Eltrombopag methyl ester

Cat.No: T72265

Avatrombopag hydrochloride

Cat.No: T40654

Synonym: AKR-501 hydrochloride,YM477hydrochloride,E5501hydrochloride

1,2,3-Trieicosapentaenoyl-rac-glycerol

Cat.No: T37382

Cat.No: T37331

2-chloro Palmitic Acid

Cat.No: T36221

Cat.No: T70882

2-Chloroadenosine-5'-O-diphosphate sodium

Cat.No: T83785

Synonym: 2-chloro ADP

Rp-Adenosine-5'-O-(1-thiotriphosphate) sodium

Cat.No: T83807

Synonym: Rp-ATP-α-S

Cat. No.	Product Name	Target	Signaling Pathways
T7053	p-Hydroxycinnamic acid p-Coumaric acid,p-Cumaric acid,p-Hydroxy-cinnamic acid,对羟基肉桂酸,NSC 59260	Thrombin; Endogenous Metabolite; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Metabolism; Proteases/Proteasome
	p-Hydroxycinnamic acid (NSC-59260) 是常见的食用酚，可抑制血小板活性，对血栓素 B2 和前列腺素 E2 的 IC50值分别为 371 和 126 μM。
T0131	Cepharanthine NSC-623442,千金藤碱,千金藤素	Apoptosis; TNF; HIV Protease; Autophagy	Apoptosis; Autophagy; Microbiology/Virology; Proteases/Proteasome
	Cepharanthine (NSC-623442) 是从Stephania cepharanthaHayata 中提取的一种生物碱，具有抗炎、抗氧化作用。它可抑制肿瘤坏死因子 (TNF)-α 介导的 NFκB 刺激、质膜脂质过氧化和血小板聚集，并抑制细胞因子的产生。
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。
TN6056	Zanthobungeanine 8-Methoxy-N-methylflindersine
	Zanthobungeanine has anti-inflammatory activity, it shows moderate NO production inhibitory activity with an IC50 value of 37.26 mg /L.It shows obviously inhibitoryactivity to platelet aggregation caused by platelet-activating factor (PAF). Zanthobungeani
T3P2855	Chamigrenal	EGFR; NOS; PAFR; COX; Prostaglandin Receptor	Angiogenesis; GPCR/G Protein; Immunology/Inflammation; JAK/STAT signaling; Neuroscience; Tyrosine Kinase/Adaptors
	β-Chamigrenal has anti-inflammatory activity, it has inhibitory effects on lipopolysaccharide-induced nitric oxide and prostaglandin E2 production in RAW 264.7 macrophages. Chamigrenal shows platelet-activating factor antagonistic activity and the IC(50)
TN5221	(-)-Variabilin
	Variabilin, a novel inhibitor of human platelet aggregation, it is a potent RGD (Arg-Gly-Asp)-containing antagonist of the fibrinogen receptor glycoprotein IIb-IIIa (GPIIb-IIIa; αIIbβ3) and the vitronectin receptor αvβ3.Variabilin is also an antimicrobial furanosesterterpene. Variabilin is an inhibitor of human secretory and cytosolic phospholipase A2 (PLA2) activities that controls eicosanoid production in vitro and in vivo, inhibits neutrophil degranulation and superoxide generation in vitro a...
T38330	Collinin
	Collinin is a coumarin that has been found in Z. schinifolium and has diverse biological activities.1,2,3,4 It is active against drug-susceptible and -resistant strains of M. tuberculosis (MIC50s = 3.13-6.25 μg/ml).1 Collinin inhibits LPS-induced nitric oxide (NO) production (IC50 = 5.9 μM) and reduces COX-2 protein levels in RAW 264.7 cells.2 It completely inhibits aggregation of isolated rabbit platelets induced by arachidonic acid , collagen, or platelet activating factor (PAF) when used at a...

天然产物

p-Hydroxycinnamic acid

Cat.No: T7053

Synonym: p-Coumaric acid,p-Cumaric acid,p-Hydroxy-cinnamic acid,对羟基肉桂酸,NSC 59260

Target: Thrombin, Endogenous Metabolite, Prostaglandin Receptor

Cat.No: T0131

Synonym: NSC-623442,千金藤碱,千金藤素

Target: Apoptosis, TNF, HIV Protease, Autophagy

Cat.No: T0070

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

Target: HIV Protease, PDE, Adenosine Receptor, Autophagy

Zanthobungeanine

Cat.No: TN6056

Synonym: 8-Methoxy-N-methylflindersine

Cat.No: T3P2855

Target: EGFR, NOS, PAFR, COX, Prostaglandin Receptor

Cat.No: TN5221

Cat.No: T38330

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