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28

抑制剂 & 化合物

5

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T38961	DP-1
	DP-1, a Ganetespib degradation product, represents a fragment derived from SDC-TRAP-0063. Ganetespib itself functions as an inhibitor of heat shock protein 90 (HSP90), exhibiting notable anti-tumor properties.
T38961L	DP-1 hydrochloride DP-1 hydrochloride(1472616-61-7 Free base)	Drug Metabolite	Metabolism
	DP-1 hydrochloride是 SDC-TRAP-0063 的降解产物，是 Ganetespib 的一个片段。Ganetespib 是一种具有抗肿瘤活性的热休克蛋白 90 (HSP90) 抑制剂。
T4297	Flibanserin BIMT-17BS,氟立班丝氨,Girosa,BIMT-17	Dopamine Receptor; 5-HT Receptor	GPCR/G Protein; Neuroscience
	Flibanserin (Girosa) 一种具有口服活性的 5-HT1A 受体激动剂和 5-HT2A 受体拮抗剂，Ki 值分别为 1 和 49 nM。它与多巴胺 D4 受体结合，Ki 值在 4 到 24 nM 之间。它是一种血清素能抗抑郁药，用于治疗性欲减退症。
T76219	MDP1
	MDP1是一种源自蜂毒肽(melittin)的衍生肽，具有破坏革兰氏阳性及阴性细菌膜完整性的能力，能够通过膜损伤方式杀灭细菌。该化合物对金黄色葡萄球菌、大肠杆菌以及铜绿假单胞菌的耐多药(MDR)和参考菌株显示出高度的抗菌活性。
T62965	TDP1 Inhibitor-2
	TDP1 Inhibitor-2 是一种 TDP1 (酪氨酰 -DNA 磷酸二酯酶 1) 的有效抑制剂 (IC50: 99 nM)。TDP1 Inhibitor-2 对 SCAN1 (脊髓小脑共济失调综合征伴轴突神经病变) 具有抑制作用 (IC50: 3.5 μM)。
T13109	TDP1 Inhibitor-1	Others	Others
	TDP1 Inhibitor-1 is a potent inhibitor of Tyrosyl-DNA Phosphodiesterase 1 (TDP1) (IC50 of 7 μM).
T78033	SDP116
	SDP116为合成的GPR116 Stachel肽衍生物，具备ADGRF5激动剂功能。
T76219L	MDP1 acetate
	MDP1 acetate为一种基于蜂毒肽(melittin)的衍生肽，能够破坏革兰氏阳性及革兰氏阴性细菌的膜完整性，进而通过膜损伤机制杀灭细菌。该化合物对金黄色葡萄球菌、大肠杆菌及铜绿假单胞菌等耐多药(MDR)与标准菌株表现出显著的抗菌活性。
T5386	Asapiprant	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Asapiprant 是一种强选择性DP1受体拮抗剂，Ki 值为 0.44 nM，对DP1受体表现出高亲和力和选择性。
T63349	Treprostinil diethanolamine UT-15C	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Treprostinil diethanolamine (UT-15C) 是EP2、DP1和IP 的有效激动剂，对EP2、DP1、IP、EP1、EP4、EP3 和 FPKi 的值分别为 3.6、4.4、32.1、212、826、2505 和 4680 nM。Treprostinil diethanolamine 能够促使 cAMP 的上调，进而维持血管系统内的稳态，并造成人肺动脉的血管扩张。
T4635	Ralinepag APD811	Others; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Others
	Ralinepag (APD811) 是一种可口服的非前列腺素前列环素 (IP) 受体激动剂，对人和大鼠 IP 受体以及人 DP1 受体的 EC50 分别为 8.5、530 和 850 nM。
T5150	Treprostinil LRX-15,曲前列环素,Orenitram,曲前列尼尔,Remodulin	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Treprostinil (Orenitram) 是有效的 DP1、IP 和 EP2 激动剂，EC50分别为0.6、1.9 和 6.2 nM。
T5171	Treprostinil Sodium 曲前列尼尔钠,UT-15	VEGFR; c-RET; Prostaglandin Receptor	Angiogenesis; Apoptosis; GPCR/G Protein; Immunology/Inflammation; Tyrosine Kinase/Adaptors
	Treprostinil Sodium (UT-15) 是有效的 DP1、IP 和 EP2 激动剂，EC50分别为0.6、1.9 和 6.2 nM。
T15712	Laropiprant MK-0524	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	Laropiprant (MK-0524) 是 DP receptor 的选择性拮抗剂，Ki 为 0.57 nM，对 TP 受体的 Ki 为 2.95 nM。
T14842	BW 245C BW245C	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	BW 245C 是一种选择性的前列腺素类DP受体(DP1)激动剂，是一种前列腺素类似物，对胶原蛋白的聚集反应有抑制作用，可用于研究中风等疾病。
T7359	CAY10471 Racemate TM30089 Racemate,3-[[(4-氟苯基)磺酰基]甲基氨基]-1,2,3,4-四氢-9H-咔唑-9-乙酸	GPR; Prostaglandin Receptor	Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation
	CAY10471 Racemate (TM30089 Racemate) 是一种高选择性的 CRTH2/DP 2 受体拮抗剂，对 hCRTH2 的Ki 值为 0.6 nM，对其选择性远高于人血栓素 A2 受体 TP 或 PGD2 受体 DP。它对大小鼠的同源 CRTH2 也具有拮抗作用。
T3306	PF-04418948 PF 04418948,PF04418948	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	PF-04418948 是一种可口服的，选择性的前列腺素EP2受体拮抗剂，IC50为16 nM。
T5482	TG4-155	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	TG4-155 是一种脑渗透性 EP2 拮抗剂，对 EP2 和 DP1 具有低纳摩尔的拮抗活性。它作用于 EP2 的 KB 为 2.4 nM，比对 DP1 受体的选择性高 14 倍，比对 EP1、EP3、EP4 和 IP 的选择性比高 550-4750 倍。
T6399	AZD1981	GPR; Prostaglandin Receptor	Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation
	AZD1981 是一种有效且特异性的 CRTh2 (DP2) 受体拮抗剂，IC50为 4 nM，用于研究哮喘、绝经后、药代动力学、哮喘患者和药物相互作用等治疗和基础科学的试验。
T15829	L 888607 Racemate	Aurora Kinase	Cell Cycle/Checkpoint; Chromatin/Epigenetic
	L 888607 Racemate is a selective antagonist of prostaglandin D2 receptor subtype 1 (DP1) (Kis: 132 nM and 17 nM for DP1 and thromboxane A2 receptor (TP), respectively).
T39165	Treprostinil palmitil Treprostinil palmitil,INS-1009
	Treprostinil Palmitil (TP), a prodrug of the DP1 and EP2 agonist Treprostinil (UT-15), exhibits EC50 values of 0.6 and 6.2 nM, respectively. It is a pure prodrug without any inherent binding affinity for G-protein coupled receptors, including prostanoid receptors.
T69967	Laropiprant analog
	Laropiprant analog is an antagonist of the prostaglandin PGD2 receptor DP1.
T28651	S-5751 S 5751
	S-5751, a prostanoid DP (DP1) antagonist, is used potentially for the treatment of bronchial asthma.
T36545	Prostaglandin D2 methyl ester Prostaglandin D2 methyl ester
	Prostaglandin D2 (PGD2) is the major eicosanoid product of mast cells and is produced in large quantities by hematopoietic PGD synthase during allergic and asthmatic anaphylaxis. It causes vasodilation, flushing, hypotension, and is an inhibitor of platelet aggregation. Prostaglandin D2 methyl ester (PGD2 methyl ester) is a more lipid-soluble, cell-permeable prodrug form of PGD2. It binds to the human and mouse PGD2 receptors (DP1 and CRTH2/DP2) with 5-10 fold lower affinity than PGD2.
T4981	Anisotropine Methylbromide	Prostaglandin Receptor; AChR	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Anisotropine Methylbromide 是一种抗胆碱能药物，已用于缓解胃肠道痉挛和抑制胃酸分泌。
T38365	CAY10597
	The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2. CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM. The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the...
T10891	CRTH2-IN-1 Ramatroban analog	P450	Metabolism
	CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay.
T15828	L 888607	Others	Others
	L 888607 is an effective and selective CRTH2 agonist (Ki: 0.8 nM).

化合物

Cat.No: T38961

DP-1 hydrochloride

Cat.No: T38961L

Synonym: DP-1 hydrochloride(1472616-61-7 Free base)

Target: Drug Metabolite

Cat.No: T4297

Synonym: BIMT-17BS,氟立班丝氨,Girosa,BIMT-17

Target: Dopamine Receptor, 5-HT Receptor

Cat.No: T76219

TDP1 Inhibitor-2

Cat.No: T62965

TDP1 Inhibitor-1

Cat.No: T13109

Target: Others

Cat.No: T78033

Cat.No: T76219L

Cat.No: T5386

Target: Prostaglandin Receptor

Treprostinil diethanolamine

Cat.No: T63349

Synonym: UT-15C

Target: Prostaglandin Receptor

Cat.No: T4635

Synonym: APD811

Target: Others, Prostaglandin Receptor

Cat.No: T5150

Synonym: LRX-15,曲前列环素,Orenitram,曲前列尼尔,Remodulin

Target: Prostaglandin Receptor

Treprostinil Sodium

Cat.No: T5171

Synonym: 曲前列尼尔钠,UT-15

Target: VEGFR, c-RET, Prostaglandin Receptor

Cat.No: T15712

Synonym: MK-0524

Target: Prostaglandin Receptor

Cat.No: T14842

Synonym: BW245C

Target: Prostaglandin Receptor

CAY10471 Racemate

Cat.No: T7359

Synonym: TM30089 Racemate,3-[[(4-氟苯基)磺酰基]甲基氨基]-1,2,3,4-四氢-9H-咔唑-9-乙酸

Target: GPR, Prostaglandin Receptor

Cat.No: T3306

Synonym: PF 04418948,PF04418948

Target: Prostaglandin Receptor

Cat.No: T5482

Target: Prostaglandin Receptor

Cat.No: T6399

Target: GPR, Prostaglandin Receptor

L 888607 Racemate

Cat.No: T15829

Target: Aurora Kinase

Treprostinil palmitil

Cat.No: T39165

Synonym: Treprostinil palmitil,INS-1009

Laropiprant analog

Cat.No: T69967

Cat.No: T28651

Synonym: S 5751

Prostaglandin D2 methyl ester

Cat.No: T36545

Synonym: Prostaglandin D2 methyl ester

Anisotropine Methylbromide

Cat.No: T4981

Target: Prostaglandin Receptor, AChR

Cat.No: T38365

Cat.No: T10891

Synonym: Ramatroban analog

Target: P450

Cat.No: T15828

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T19329	Fructo-oligosaccharide DP12/GF11 蔗果十二糖	Others	Others
	Fructo-oligosaccharide DP12/GF11 is a member of fructooligosaccharides (FOS) characterized by a degree of polymerization (DP) of 12. FOS compounds consist of 11 fructose units connected by (2→1)-β-glycosidic bonds, with a lone D-glucosyl unit located at the non-reducing end.
T82369	Fructo-oligosaccharide DP14
	Fructo-oligosaccharide DP14为从Atractylodes lancea中提取的寡糖。
T19328	Fructo-oligosaccharide DP11/GF10	Others	Others
	Fructo-oligosaccharide DP11/GF10 is a fructooligosaccharide (FOS) compound with a degree of polymerization (DP) equal to 11. FOS consists of 10 fructose units connected by (2→1)-β-glycosidic bonds, with a single D-glucosyl unit present at the non-reducing end.
T82370	Fructo-oligosaccharide DP13
	Fructo-oligosaccharide DP13，一种Inulin型低聚果糖，可从Morinda Officinalis中分离。
TN2358	Fructo-oligosaccharide DP10/GF9 蔗果十糖,Fructo-oligosaccharide DP10/GF9	Others	Others
	Fructo-oligosaccharide DP10/GF9 is a compound classified as a fructooligosaccharide (FOS) with a degree of polymerization (DP) of 10. FOS consists of a chain of 9 fructose units connected by (2→1)-β-glycosidic bonds, with a lone D-glucosyl unit located at the non-reducing end.

天然产物

Fructo-oligosaccharide DP12/GF11

Cat.No: T19329

Synonym: 蔗果十二糖

Target: Others

Fructo-oligosaccharide DP14

Cat.No: T82369

Fructo-oligosaccharide DP11/GF10

Cat.No: T19328

Target: Others

Fructo-oligosaccharide DP13

Cat.No: T82370

Fructo-oligosaccharide DP10/GF9

Cat.No: TN2358

Synonym: 蔗果十糖,Fructo-oligosaccharide DP10/GF9

Target: Others

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