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Search Results for " prostacyclin "

37

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T15238	Epoprostenol sodium Prostaglandin I2 sodium salt,Prostacyclin sodium salt,Flolan	Others	Others
	Epoprostenol sodium is a potent inhibitor of platelet aggregation used in pulmonary hypertension and transplantation.
T26745	BAY 73-1449 BAY-73-1449,BAY73-1449	Others	Others
	BAY 73-1449 是前列环素受体选择性拮抗剂，在人 HEL 细胞和大鼠 DRG 的 cAMP 分析中具有很高的效价，IC50小于 0.1 nM。BAY 73-1449在降血压方面有研究的价值。
T36236	5-cis Carbaprostacyclin
	5-cis Carbaprostacyclin is a stable analog of PGI2 and an isomer of carbaprostacyclin. It is a weak inhibitor of human platelet aggregation with an IC50 of 2.8 μM compared to 0.3 μM for carbaprostacyclin. 5-cis Carbaprostacyclin is a much weaker effector of rabbit mesenteric artery relaxation with an EC50 of 104 μM compared to 5.9 μM for carbaprostacyclin. It even antagonizes the adenylate cyclase activation induced by carbaprostacyclin.
T36774	13,14-dehydro-15-cyclohexyl Carbaprostacyclin
	13,14-dehydro-15-cyclohexyl Carbaprostacyclin is a chemically stable analog of PGI2. It inhibits the ADP-induced aggregation of human platelets with an ED50 of about 40 nM in PRP and 77 nM in washed platelets, which is comparable to the potency of carbaprostacyclin.
T3216	Selexipag NS-304,ACT-293987,赛乐西帕,Uptravi	Others; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Others
	Selexipag (ACT-293987) 是前列环素受体激动剂，可引起肺血管舒张，用于治疗肺动脉高压。
T69360	RO3244794	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	RO3244794是一种具有选择性的前列环素（IP）受体拮抗剂，可用于研究肝脏损伤。
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。
TP1277	Bradykinin 缓激肽	Endogenous Metabolite; Bradykinin Receptor	GPCR/G Protein; Metabolism
	Bradykinin 是由激肽释放酶-激肽系统产生的活性肽。它是炎症调节因子和神经调节因子，对几种血管和肾功能也有调节作用。
T21443	Prednicarbate Hoe 777,Hoe-777,Dermatop E emollient,UNII-V901LV1K7D	Others	Others
	Prednicarbate (Hoe 777) 是一种外用皮质类固醇。Prednicarbate 可用于炎症性皮肤病的研究，如特应性皮炎。
T4436	RO1138452 CAY10441	Others; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Others
	RO1138452 (CAY10441) 是一种选择性和可口服的前列环素受体拮抗剂，pKi 为8.3。它拮抗卡前列环素诱导的人神经母细胞瘤腺苷酸环化酶的激活，以剂量依赖性方式阻断环 AMP 积累，具有镇痛活性。
T34417	RS 93427-007 RS-93427-007,RS93427-007
	RS-93427-007 is an orally active stable mimetic agent of prostacyclin for the study of mechanisms of atherogenesis.
T68751	Hoe 892
	Hoe 892 is a stable thia-thimo-analogue of prostacyclin and acts as a platelet aggregation inhibitor.
T34796	TEI-9063 TEI9063
	TEI-9063 is a stable and highly specific prostacyclin analogue of prostacyclin receptor in mast cell tumor p-815 cells.
T30426	Beraprost ML 1229,MDL 201229,ML-1229,MDL-201229
	Beraprost is a stable prostacyclin analog.
T33579	Nafazatrom Nafazatromum
	Nafazatrom is a pyrazolinone derivative and lipoxygenase inhibitor that increases endogenous prostacyclin (PGI2) and has experimental anticancer activity. Nafazatrom is also an antithrombotic drug that increases prostacyclin levels and reduces the inciden
T23657	AFP-07 AFP07
	AFP-07 is a highly selective and potent agonist. It was used for the prostacyclin receptor.
T71025	KP 10614
	KP 10614 is a new prostacyclin analog that inhibits platelet-polymorphonuclear leukocyte interaction.
T28254	OP-2507
	OP-2507, a prostacyclin agonist, is used potentially for the treatment of hepatic insufficiency and hypertension.
T10673	Carbacyclin Carbaprostacyclin,Carba-PGI2	Others	Others
	Carbacyclin, a PGI2 analog, is a prostacyclin (PGI2) receptor agonist and vasodilator with potent inhibitory platelet aggregation.
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 ...
T15560	Iloprost ZK 36374,Ciloprost,伊洛前列素	Others	Others
	Iloprost is a synthetic analogue of prostacyclin PGI2. Iloprost commonly employed in the treatment of peripheral vascular disease and also indicated in the treatment of patients affected by systemic sclerosis (SSc) in the presence of severe Raynaud's phen
T61526	Cicaprost
	Cicaprost (ZK 96480) is a prostacyclin receptor (IP) agonist, which induces relaxation of the artery via concentration-dependent mechanisms. Its EC50 value, determined to be 5.8 nM [1], further highlights its potency.
T36211	16(R)-Iloprost
	Iloprost is a second generation structural analog of prostacyclin (PGI2) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the recombinant human IP and EP1 receptors with a Ki value of 11 nM. Most preparations of iloprost contain 16(S) and 16(R) stereoisomers. 16(R)-Iloprost inhibits platelet aggregation with an IC50 value of 65 nM.
T68639	Ciprostene (free base)
	Ciprostene (free base) is a synthetic, chemically stable analog of prostacyclin (PGI2). In animal models, administration of ciprostene resulted in dose-dependent hypotension, tachycardia, and inhibition of ex vivo ADP-induced platelet aggregation. Ciprostene was evaluated in clinical trials in patients with peripheral vascular disease. It was found to reduce restenosis in patients with coronary artery disease undergoing therapeutic percutaneous transluminal coronary angioplasty.
TMIH-0520	Selexipag-d7
	Selexipag-d7 是 Selexipag 的氘代化合物。Selexipag 的 CAS 号为 475086-01-2。Selexipag 是前列环素受体激动剂，可引起肺血管舒张，用于治疗肺动脉高压。
T41251	Taprostene
	Taprostene (CG-4203) 是一种合成的、化学稳定的前列环素 (PGI2) 类似物。Taprostene 对猫急性心肌缺血再灌注后内皮和心肌有保护作用。Taprostene 增强细胞保护作用，同时减少不必要的血液动力学影响。
T35943	15(S)-HpETE
	15(S)-HpETE is a monohydroperoxy polyunsaturated fatty acid (PUFA) produced by the action of 15-lipoxygenase (15-LO) on arachidonic acid. It is either metabolized to 14,15-leukotriene A4 [1] or reduced to 15(S)-HETE by peroxidases.[2] [1] 15(S)-HpETE mediates a number of biological functions including the induction of c-fos and c-jun, and activation of AP-1. [3] 15(S)-HpETE inhibits prostacyclin synthesis in porcine aortic microsomes and bovine endothelial cells, and can cause the suicide inac...
T36212	16(S)-Iloprost
	Iloprost is a second generation structural analog of prostacyclin (PGI2) with about ten-fold greater potency than the first generation stable analogs, typified by carbaprostacyclin. Iloprost binds with equal affinity to the recombinant human IP and EP1 receptors with a Ki value of 11 nM. Most preparations of iloprost contain 16(S) and 16(R) stereoisomers. 16(S)-Iloprost potently inhibits platelet aggregation with an IC50 value of 3.5 nM.
TMIH-0519	Selexipag Active Metabolite-d7
	Selexipag Active Metabolite-d7 是 Selexipag Active Metabolite 的氘代化合物。Selexipag Active Metabolite 的 CAS 号为 475085-57-5。MRE269 是一种口服的长效前列环素受体激动剂前药，是 Selexipag 的活性代谢物，用于治疗肺动脉高压。
T37234	(±)14(15)-EpETE
	EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids, produces epoxides such as (±)14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid and docosahexaenoi...
T36552	CG 4305
	Prostacyclin (PGI2) is a cyclooxygenase metabolite with antithrombotic properties found in vascular endothelial cells. The half-life is short both in vivo and in vitro, ranging from 30 seconds to a few minutes. CG 4305 is a stable carbacyclic analog of PGI2 that inhibits ADP-induced platelet aggregation 25% at a concentration of 50 nM. Doses of 10 mg/kg (oral) or 1 mg/kg (intraduodenal) have been shown to prevent rabbit carotid artery thrombosis.
T70865	BMY-42393
	BMY-42393 is orally active and selective platelet aggregation inhibitor. BMY-42393 is also a prostacyclin partial agonist that inhibited ADP, collagen and thrombin-induced platelet aggregation (IC50 range 0.3 - 2.0 microM). BMY-42393 stimulated platelet adenylate cyclase activity (EC50 = 25 nM). Platelets treated with BMY 42393 showed an elevation of cAMP levels and activation of cAMP-dependent protein kinase. BMY 42393 also inhibited thrombin-induced elevation of intracellular free calcium. B...
T37238	(±)19(20)-EpDPA
	EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as (±)14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid and docosahexaenoic...
T37235	(±)16(17)-EpDPA (±)16,17-EpDPE,(±)16,17 EDP,(±)16,17-epoxy Docosapentaenoic Acid,(±)16,17-epoxy DPA,(±)16(17)-EpDPA
	EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators.[1],[2]Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as (±)14(15)-EET which are prime candidates for the actual active mediator.[3] However, the CYP450 metabolites of eicosapentaenoic acid and docosahex...
T65598	Cefminox sodium
	Cefminox (Sodium) is a new cephamycin antibiotic possessing a D-amino acid moiety derived from D-cysteine at the C-7B side chain. Cefminox is active against a wide range of bacteria, especially Gram-negative and anaerobic bacteria. Cefminox shows excellent in vivo efficacy (ED50) which is higher than would be expected from its in vitro activity (MIC). Moreover, cefminox possesses more potent activity in suppression of bacterial regrowth than other cephems[1]. Cefminox (Sodium) was the most activ...
T35789	Palmitic acid-1-13C
	Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.1 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.2 Palmitic acid is involved in the acylation of proteins to anchor membrane-bound proteins to the lipid bilayer.2,3,4,5,6 \|1. Santos, M.J., López-Jurado, M., Llopis, J., et a...
T35791	Palmitic acid-13C
	Palmitic acid-13C is intended for use as an internal standard for the quantification of palmitic acid by GC- or LC-MS. Palmitic acid-13C contains 13C at the C2 position and has been used in the study of free fatty acid incorporation into phospholipid fatty acids in soil microbes.1 Palmitic acid is a 16-carbon saturated fatty acid. It comprises approximately 25% of human total plasma lipids.2 It increases protein levels of COX-2 in RAW 264.7 cells when used at a concentration of 75 μM.3 Palmitic ...

化合物

Epoprostenol sodium

Cat.No: T15238

Synonym: Prostaglandin I2 sodium salt,Prostacyclin sodium salt,Flolan

Target: Others

Cat.No: T26745

Synonym: BAY-73-1449,BAY73-1449

Target: Others

5-cis Carbaprostacyclin

Cat.No: T36236

13,14-dehydro-15-cyclohexyl Carbaprostacyclin

Cat.No: T36774

Cat.No: T3216

Synonym: NS-304,ACT-293987,赛乐西帕,Uptravi

Target: Others, Prostaglandin Receptor

Cat.No: T69360

Target: Prostaglandin Receptor

Cat.No: T4635

Synonym: APD811

Target: Others, Prostaglandin Receptor

Cat.No: TP1277

Synonym: 缓激肽

Target: Endogenous Metabolite, Bradykinin Receptor

Cat.No: T21443

Synonym: Hoe 777,Hoe-777,Dermatop E emollient,UNII-V901LV1K7D

Target: Others

Cat.No: T4436

Synonym: CAY10441

Target: Others, Prostaglandin Receptor

Cat.No: T34417

Synonym: RS-93427-007,RS93427-007

Cat.No: T68751

Cat.No: T34796

Synonym: TEI9063

Cat.No: T30426

Synonym: ML 1229,MDL 201229,ML-1229,MDL-201229

Cat.No: T33579

Synonym: Nafazatromum

Cat.No: T23657

Synonym: AFP07

Cat.No: T71025

Cat.No: T28254

Cat.No: T10673

Synonym: Carbaprostacyclin,Carba-PGI2

Target: Others

Ro 1138452 hydrochloride

Cat.No: T38171

Cat.No: T15560

Synonym: ZK 36374,Ciloprost,伊洛前列素

Target: Others

Cat.No: T61526

Cat.No: T36211

Ciprostene (free base)

Cat.No: T68639

Cat.No: TMIH-0520

Cat.No: T41251

Cat.No: T35943

Cat.No: T36212

Selexipag Active Metabolite-d7

Cat.No: TMIH-0519

(±)14(15)-EpETE

Cat.No: T37234

Cat.No: T36552

Cat.No: T70865

(±)19(20)-EpDPA

Cat.No: T37238

(±)16(17)-EpDPA

Cat.No: T37235

Synonym: (±)16,17-EpDPE,(±)16,17 EDP,(±)16,17-epoxy Docosapentaenoic Acid,(±)16,17-epoxy DPA,(±)16(17)-EpDPA

Cefminox sodium

Cat.No: T65598

Palmitic acid-1-13C

Cat.No: T35789

Palmitic acid-13C

Cat.No: T35791

Cat. No.	Product Name	Target	Signaling Pathways
TMA0536	2-Acetylbenzoic acid	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	2-Acetylbenzoic acid 在抑制血小板功能和血小板前列腺素 (PG) 合成方面比 2-丙酰氧基苯甲酸更有效，尽管这些药物在抑制前列环素 (PGI2) 合成方面的效力相当。
T3S2007	MRE-269 3-氧代-12-烯-28-乌苏酸,MRE 269,ACT-333679,MRE269	Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation
	MRE-269 (ACT-333679) 是一种口服的长效前列环素受体激动剂前药，是 Selexipag 的活性代谢物，用于治疗肺动脉高压。
T73776	13-Hydroxyoctadecadienoic acid
	13-hydroxyoctadecadienoic acid (13-HODE) 是 Linoleic acid 的一种内源性脂氧合酶代谢产物。13-hydroxyoctadecadienoic acid 通过增强磷脂中花生四烯酸 (AA) 的释放来刺激前列环素的产生。

天然产物

2-Acetylbenzoic acid

Cat.No: TMA0536

Target: Prostaglandin Receptor

Cat.No: T3S2007

Synonym: 3-氧代-12-烯-28-乌苏酸,MRE 269,ACT-333679,MRE269

Target: Prostaglandin Receptor

13-Hydroxyoctadecadienoic acid

Cat.No: T73776

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