Prostaglandin Receptor

抑制剂选择性比较

Prostaglandin Receptor产品

目录号 产品描述 文献引用 实验数据
S2496

Ozagrel

Ozagrel (OKY-046)是一种有效的,选择性的血栓素A2合成酶抑制剂,IC50为4 nM。

S2067

Ozagrel HCl

Ozagrel HCl (OKY-046)是选择性血栓素A2合成酶抑制剂,其在兔子血小板中IC50为11 nM, 用作改善手术后脑血管收缩,以及伴随的脑梗塞。

S3304New

Stylopine

Stylopine ((R,S)-Stylopine, Tetrahydrocoptisine) 可降低LPS刺激引起的 nitric oxide (NO)tumor necrosis factor-alpha (TNF-alpha)interleukin-1beta (IL-1beta)IL-6 的生成,以及 cyclooxygenase-2 (COX-2) 的活性。Stylopine 是 Chelidonium majus L 的叶子的主要成分。

S6850New

NE 52-QQ57

NE 52-QQ57 是一种 G-protein coupled receptor 4 (GPR4) 的选择性口服拮抗剂,其IC50值为0.07 μM。NE 52-QQ57 可有效地阻断GPR4介导的cAMP积累,在HEK293细胞中的IC50值为26.8 nM。NE 52-QQ57对GPR4的拮抗作用可显著地抑制AGE诱导的几种关键炎性细胞因子和信号分子表达的增加,包括 tumor necrosis factor-α (TNF-α)interleukin (IL)-1βIL-6inducible nitric oxide synthase (iNOS)nitric oxide (NO)cyclooxygenase 2 (COX2)prostaglandin E2 (PGE2)

S0141New

NQ301

NQ301 (compound 211) 是一种抗血小板和抗血栓形成剂,也是一种选择性的 CD45 的抑制剂,IC50值为200 nM。NQ301 可抑制兔血小板中的 thromboxane A2 receptor (TXA2) 和合酶synthase的活性。

S6649New

E7046(ER-886406)

E7046是prostaglandin E2 (PGE2) receptor EP4的选择性抑制剂,IC50为13.5 nM,Ki为23.14 nM

S5252

Ozagrel sodium

Ozagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase inhibitor with neuroprotective properties.

S3816

Dehydroevodiamine

Dehydroevodiamine (DHED), a constituent of Evodia rutaecarpa, has various biological effects such as hypotensive, negative chronotropic, ion channel depressant, inhibition of nitric oxide production and cerebral blood flow enhancing activities. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.

S5594

α-Terpineol

α-Terpineol, a natural monoterpene, is the major component of essential oils of several species of aromatic plants such as Origanium vulgare L. and Ocimum canum Sims which are widely used for medicinal purposes. It is widely used in the manufacturing of cosmetics, soaps, perfumes, antiseptic agents and is considered one of the most frequently used fragrance compounds.

S0495New

BI-671800

BI-671800 (AP-761, Cmpd A) 是一种高度特异性的 chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2) 的强效拮抗剂,对PGD2结合人类CRTH2和鼠CRTH2的IC50值分别为4.5 nM和3.7 nM。BI-671800 与无症状的初治哮喘患者和ICS患者的FEV1略有改善有关。

S0305New

RO1138452

RO1138452 (CAY10441) 是一种有效的、选择性的 IP (prostacyclin, PGI2) receptor 的拮抗剂,在人血小板和重组IP受体系统中的pKi值分别为9.3和8.7。

S6793New

TG4-155

TG4-155是一种有效的、选择性的 Prostaglandin Receptor EP2(PTGER2) 拮抗剂,Ki值为9.9 nM。

S5753

Setipiprant (ACT-129968)

Setipiprant (ACT-129968, KYTH-105) is a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2) that that has been shown to have greater specificity for DP2 (CRTH2) than for DP1.

S7211

PF-04418948

PF-04418948 是一种有效的选择性前列腺素 EP₂ receptor 拮抗剂,IC50 为 16 nM。Phase 1.

S5286

Ramatroban

Ramatroban (BAY u 3405) is a thromboxane A2(TxA2) receptor antagonist with Ki value of 10 to 13 nM. It also antagonizes a newly identified PGD2 receptor, CRTh2 expressed on the inflammatory cells.

S2072

Seratrodast(AA-2414)

Seratrodast (AA-2414, ABT-001) 是一种有效的选择性的血栓素A2受体(TP)拮抗剂,IC50为40 nM ,主要用于治疗治疗哮喘,也是抗炎药。

S1407

Bimatoprost

Bimatoprost是一种前列腺素类似物,局部(眼药水)用药,治疗青光眼和高眼压症。

S1508

Alprostadil

Alprostadil (Prostaglandin-E1) 用于治疗勃起功能障碍,具有血管舒张的特性。它是前列腺素的类似物,是Prostaglandin E1的激动剂。

S3003

Prostaglandin E2 (PGE2)

Prostaglandin E2 (PGE2, Dinoprostone) 在分娩中发挥重要作用(可软化宫颈,引起子宫收缩),也刺激成骨细胞释放能刺激破骨细胞吸收的因子。

S0325New

Treprostinil sodium

Treprostinil sodium (UT-15, Remodulin, Orenitram, Tyvaso, Trevyent) 是一种有效的 DP1EP2IP 受体的激动剂,对应的Ki值分别为4.4 nM、3.6 nM和32 nM。

S0010New

Ralinepag

Ralinepag (APD811) is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist with EC50 of 8.5 nM, 530 nM and 850 nM for human IP receptor, rat IP receptor and human DP1 receptor, respectively.

S4851

Tafluprost

Tafluprost (AFP-168) 是一种新型的前列腺素类似物,对氟代前列腺素受体PGF2α具有高亲和力。是对前列腺素类具有选择性的FP receptor激动剂。

S9327

Carboprost

Carboprost is a synthetic prostaglandin analogue of PGF2α with oxytocic properties.

S5819

MRE-269 (ACT-333679)

MRE-269 (ACT-333679)是前列腺素I2受体(prostaglandin I2 receptor)激动剂,对人源前列腺素I2受体的结合亲和力是对其他人源前列腺素受体的130倍。

S3726

Selexipag

Selexipag (NS-304, ACT-293987) is an orally active, first-in-class, selective prostacyclin IP receptor agonist with Ki value of 260 nM for human IP, whereas Ki values > 10,000 nM are measured at the other human G-protein-coupled prostanoid receptors (EP1-4, DP, FP and TP).

S3738

Travoprost

Travoprost是PGF2α的类似物,作为一种滴眼液用于治疗开角青光眼造成的眼内高血压。

S5056

Dinoprost tromethamine

Dinoprost Tromethamine (Dinolytic, PGF2-alpha tham, Zinoprost, Prostin F2 alpha, Dinoprost Trometamol) 是一种合成的prostaglandin F2 alpha类似物,prostaglandin F2 alpha可通过直接作用于黄体素,刺激子宫肌层活性、使宫颈舒张、抑制黄体类固醇生成、诱导黄体溶解。

S4415

Misoprostol

S0541New

Dazoxiben hydrochloride

Dazoxiben hydrochloride (HCl) 是一种 thromboxane (TX) synthase.的有效,选择性和口服活性抑制剂。Dazoxiben 可抑制人全血中 TXB2 的产生,其IC50值为0.3 μM,并可平行地增强 PGE2 的产生。

S4152

Ethamsylate

Ethamsylate (Etamsylate)是一种止血药,抑制前列腺素的生物合成和功能,提高毛细血管内皮阻力和血小板粘附。

目录号 产品描述 文献引用 实验数据
S2496

Ozagrel

Ozagrel (OKY-046)是一种有效的,选择性的血栓素A2合成酶抑制剂,IC50为4 nM。

S2067

Ozagrel HCl

Ozagrel HCl (OKY-046)是选择性血栓素A2合成酶抑制剂,其在兔子血小板中IC50为11 nM, 用作改善手术后脑血管收缩,以及伴随的脑梗塞。

S3304New

Stylopine

Stylopine ((R,S)-Stylopine, Tetrahydrocoptisine) 可降低LPS刺激引起的 nitric oxide (NO)tumor necrosis factor-alpha (TNF-alpha)interleukin-1beta (IL-1beta)IL-6 的生成,以及 cyclooxygenase-2 (COX-2) 的活性。Stylopine 是 Chelidonium majus L 的叶子的主要成分。

S6850New

NE 52-QQ57

NE 52-QQ57 是一种 G-protein coupled receptor 4 (GPR4) 的选择性口服拮抗剂,其IC50值为0.07 μM。NE 52-QQ57 可有效地阻断GPR4介导的cAMP积累,在HEK293细胞中的IC50值为26.8 nM。NE 52-QQ57对GPR4的拮抗作用可显著地抑制AGE诱导的几种关键炎性细胞因子和信号分子表达的增加,包括 tumor necrosis factor-α (TNF-α)interleukin (IL)-1βIL-6inducible nitric oxide synthase (iNOS)nitric oxide (NO)cyclooxygenase 2 (COX2)prostaglandin E2 (PGE2)

S0141New

NQ301

NQ301 (compound 211) 是一种抗血小板和抗血栓形成剂,也是一种选择性的 CD45 的抑制剂,IC50值为200 nM。NQ301 可抑制兔血小板中的 thromboxane A2 receptor (TXA2) 和合酶synthase的活性。

S6649New

E7046(ER-886406)

E7046是prostaglandin E2 (PGE2) receptor EP4的选择性抑制剂,IC50为13.5 nM,Ki为23.14 nM

S5252

Ozagrel sodium

Ozagrel sodium (KCT-0809, Cataclot, Xanbo) is a thromboxane A2 synthase inhibitor with neuroprotective properties.

S3816

Dehydroevodiamine

Dehydroevodiamine (DHED), a constituent of Evodia rutaecarpa, has various biological effects such as hypotensive, negative chronotropic, ion channel depressant, inhibition of nitric oxide production and cerebral blood flow enhancing activities. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.

S5594

α-Terpineol

α-Terpineol, a natural monoterpene, is the major component of essential oils of several species of aromatic plants such as Origanium vulgare L. and Ocimum canum Sims which are widely used for medicinal purposes. It is widely used in the manufacturing of cosmetics, soaps, perfumes, antiseptic agents and is considered one of the most frequently used fragrance compounds.

目录号 产品描述 文献引用 实验数据
S0495New

BI-671800

BI-671800 (AP-761, Cmpd A) 是一种高度特异性的 chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2) 的强效拮抗剂,对PGD2结合人类CRTH2和鼠CRTH2的IC50值分别为4.5 nM和3.7 nM。BI-671800 与无症状的初治哮喘患者和ICS患者的FEV1略有改善有关。

S0305New

RO1138452

RO1138452 (CAY10441) 是一种有效的、选择性的 IP (prostacyclin, PGI2) receptor 的拮抗剂,在人血小板和重组IP受体系统中的pKi值分别为9.3和8.7。

S6793New

TG4-155

TG4-155是一种有效的、选择性的 Prostaglandin Receptor EP2(PTGER2) 拮抗剂,Ki值为9.9 nM。

S5753

Setipiprant (ACT-129968)

Setipiprant (ACT-129968, KYTH-105) is a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2) that that has been shown to have greater specificity for DP2 (CRTH2) than for DP1.

S7211

PF-04418948

PF-04418948 是一种有效的选择性前列腺素 EP₂ receptor 拮抗剂,IC50 为 16 nM。Phase 1.

S5286

Ramatroban

Ramatroban (BAY u 3405) is a thromboxane A2(TxA2) receptor antagonist with Ki value of 10 to 13 nM. It also antagonizes a newly identified PGD2 receptor, CRTh2 expressed on the inflammatory cells.

S2072

Seratrodast(AA-2414)

Seratrodast (AA-2414, ABT-001) 是一种有效的选择性的血栓素A2受体(TP)拮抗剂,IC50为40 nM ,主要用于治疗治疗哮喘,也是抗炎药。

目录号 产品描述 文献引用 实验数据
S1407

Bimatoprost

Bimatoprost是一种前列腺素类似物,局部(眼药水)用药,治疗青光眼和高眼压症。

S1508

Alprostadil

Alprostadil (Prostaglandin-E1) 用于治疗勃起功能障碍,具有血管舒张的特性。它是前列腺素的类似物,是Prostaglandin E1的激动剂。

S3003

Prostaglandin E2 (PGE2)

Prostaglandin E2 (PGE2, Dinoprostone) 在分娩中发挥重要作用(可软化宫颈,引起子宫收缩),也刺激成骨细胞释放能刺激破骨细胞吸收的因子。

S0325New

Treprostinil sodium

Treprostinil sodium (UT-15, Remodulin, Orenitram, Tyvaso, Trevyent) 是一种有效的 DP1EP2IP 受体的激动剂,对应的Ki值分别为4.4 nM、3.6 nM和32 nM。

S0010New

Ralinepag

Ralinepag (APD811) is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist with EC50 of 8.5 nM, 530 nM and 850 nM for human IP receptor, rat IP receptor and human DP1 receptor, respectively.

S4851

Tafluprost

Tafluprost (AFP-168) 是一种新型的前列腺素类似物,对氟代前列腺素受体PGF2α具有高亲和力。是对前列腺素类具有选择性的FP receptor激动剂。

S9327

Carboprost

Carboprost is a synthetic prostaglandin analogue of PGF2α with oxytocic properties.

S5819

MRE-269 (ACT-333679)

MRE-269 (ACT-333679)是前列腺素I2受体(prostaglandin I2 receptor)激动剂,对人源前列腺素I2受体的结合亲和力是对其他人源前列腺素受体的130倍。

S3726

Selexipag

Selexipag (NS-304, ACT-293987) is an orally active, first-in-class, selective prostacyclin IP receptor agonist with Ki value of 260 nM for human IP, whereas Ki values > 10,000 nM are measured at the other human G-protein-coupled prostanoid receptors (EP1-4, DP, FP and TP).

S3738

Travoprost

Travoprost是PGF2α的类似物,作为一种滴眼液用于治疗开角青光眼造成的眼内高血压。

S5056

Dinoprost tromethamine

Dinoprost Tromethamine (Dinolytic, PGF2-alpha tham, Zinoprost, Prostin F2 alpha, Dinoprost Trometamol) 是一种合成的prostaglandin F2 alpha类似物,prostaglandin F2 alpha可通过直接作用于黄体素,刺激子宫肌层活性、使宫颈舒张、抑制黄体类固醇生成、诱导黄体溶解。

S4415

Misoprostol

目录号 产品描述 文献引用 实验数据
S0541New

Dazoxiben hydrochloride

Dazoxiben hydrochloride (HCl) 是一种 thromboxane (TX) synthase.的有效,选择性和口服活性抑制剂。Dazoxiben 可抑制人全血中 TXB2 的产生,其IC50值为0.3 μM,并可平行地增强 PGE2 的产生。

目录号 产品描述 文献引用 实验数据
S4152

Ethamsylate

Ethamsylate (Etamsylate)是一种止血药,抑制前列腺素的生物合成和功能,提高毛细血管内皮阻力和血小板粘附。

Tags: Prostaglandin Receptor agonist | Prostaglandin Receptor antagonist | Prostaglandin Receptor inhibitor