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Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
T15718 |
Latanoprost acid
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
Latanoprost acid 是前列腺素受体的选择性激动剂,通过抑制 c-fos/NFATc1 通路抑制 RANKL 诱导的破骨细胞生成和功能。 拉坦前列素酸可用于降低眼内压力的研究。 | |||
T1978 |
GW627368
GW 627368X |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
GW627368 (GW 627368X) 是一种新型、强效和选择性的前列腺素 EP4 受体拮抗剂,还对血栓素受体TP 有亲和力。对人 EP4 和 TP 的pKi 值分别为 7.0 和 6.8。 | |||
T2528 |
Latanoprost
Xalatan,PHXA41,拉坦前列腺素,拉坦前列素 |
GPR; Prostaglandin Receptor; RAR/RXR | Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism |
Latanoprost (Xalatan) 是前列腺素 F2α 类似物,是一种前列腺素受体激动剂,能够降低眼内压。 | |||
T2664 |
Timapiprant
OC000459 |
GPR; Prostaglandin Receptor | Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation |
Timapiprant (OC000459) 是一种有效的选择性 D 前列腺素受体 2(DP2) 拮抗剂,IC50为 13 nM。它抑制肥大细胞激活 Th2 淋巴细胞和嗜酸性粒细胞,有效地置换来自人重组 DP2、大鼠重组 DP2 和人天然 DP2 的 [3H] PGD2。 | |||
T17232 |
Vidupiprant
AMG 853 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
Vidupiprant (AMG 853) 是一种有效的 CRTH2 和前列腺素 D 受体双重拮抗剂,在人源血浆中的 IC50 分别为 8 nM 和 35 nM。 Vidupiprant 可用于治疗哮喘的研究。 | |||
T11211 |
EP4 receptor antagonist 1
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
EP4 receptor antagonist 1 是一种有效的特异性前列腺素 EP4受体拮抗剂,对人和小鼠 EP4受体的 IC50分别为6.1 nM 和16.2 nM。 EP4 receptor antagonist 1 可用于癌症免疫治疗的研究。 | |||
T69229 |
ONO-8539
|
||
ONO-8539 is a prostanoid EP1 receptor antagonist. | |||
T69602 |
ONO-DI-004
|
||
ONO-DI-004 is a selective EP1 Prostanoid receptor agonist. | |||
T27875 |
LY 150310
LY150310,LY-150310 |
||
LY 150310, a histamine H1-receptor antagonist, can alter prostanoid concentrations in vitro and in vivo. | |||
T29734 |
AH 19437
AH-19437,AH19437 |
||
AH 19437 is a prostanoid receptor. | |||
T26578 |
AH13205
AH-13205,AH 13205 |
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AH13205 is an agonist of EP2 prostanoid receptor. | |||
T15689 |
L-798106
CM9,GW671021 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
L-798106 is a highly selective prostanoid EP3 receptor antagonist (Ki=0.3 nM). It also has micromolar activities at EP4, EP1, and EP2 receptors (Ki: 916 nM, >5000 nM, and >5000 nM at EP4, EP1, and EP2, respectively). | |||
T23332 |
SC 51322
|
Others | Others |
SC 51322 is an EP1 prostanoid receptor antagonist. | |||
T16389 | Omidenepag | Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
Omidenepag is a pharmacologically active form of Omidenepag Isopropyl and is a selective, non-prostanoid EP2 receptor agonist (EC50: 1.1 nM). Omidenepag displays binding affinities (IC50: 10 nM for h-EP2). | |||
T19660 |
QCC-374
QCC374 |
||
QCC-374 is a prostanoid agonist. It potentially for the treatment of pulmonary arterial hypertension. | |||
T20644 |
Unoprostone isopropyl
UF021,Rescula,UF-021,UF 021 |
||
Unoprostone isopropyl, a prostanoid and synthetic docosanoid, is approved for the treatment of ocular hypertension and open-angle glaucoma. | |||
T27765 |
L-644,698
|
||
L-644,698 is a selective agonist of human prostanoid DP receptor. | |||
T17099 |
Timapiprant sodium
OC000459 sodium |
Others | Others |
Timapiprant sodium inhibits mast cell activation of Th2 lymphocytes and eosinophils. Timapiprant sodium is a potent and selective D prostanoid receptor 2 antagonist. Timapiprant sodium potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), ra | |||
T39165 |
Treprostinil palmitil
Treprostinil palmitil,INS-1009 |
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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. | |||
T28651 |
S-5751
S 5751 |
||
S-5751, a prostanoid DP (DP1) antagonist, is used potentially for the treatment of bronchial asthma. | |||
T29813 |
AL-3138
AL3138,AL 3138,11-Deoxy-16-fluoro PGF2alpha |
||
AL-3138 is a prostaglandin F2alpha (PGF2alpha) analogue which antagonizes FP prostanoid receptor-mediated inositol phosphates generation. | |||
T28032 |
MF266-1
MF 266-1,MF-266-1 |
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MF266-1, a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of osteoarthritis and rheumatoid. | |||
T16069 |
MF498
|
Others | Others |
MF498 is a novel and selective E prostanoid receptor 4 (EP4 receptor) antagonist, displayed a strong binding affinity for the EP4 receptor (Ki: 0.7 nM). | |||
T15690 |
L-902688
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
L-902688 is an orally active EP4 receptor agonist (Ki: 0.38 nM; EC50: 0.6 nM). L-902688 displays >4,000-fold selective for EP4 over other EP and prostanoid receptors. | |||
T11821 |
Latanoprost lactone diol
|
Others | Others |
Latanoprost lactone diol is an important intermediate compound in the synthesis of Latanoprost. Latanoprost, classified as a prostaglandin F2α analogue, functions as an agonist for the FP prostanoid receptor, resulting in a reduction in intraocular pressure (IOP). | |||
T71088 | AM-211 sodium | ||
AM-211 sodium is a novel and potent antagonist of the prostaglandin D2 receptor type 2. AM-211 is active in animal models of allergic inflammation. AM211 has high affinity for human, mouse, rat, and guinea pig DP2 and it shows selectivity over other prostanoid receptors and enzymes. AM211 exhibits good oral bioavailability in rats and dogs and dose-dependently inhibits 13,14-dihydro-15-keto-PGD(2)-induced leukocytosis in a guinea pig pharmacodynamic assay. | |||
T38389 |
Prostaglandin D2 Ethanolamide
Prostaglandin D2 Ethanolamide |
||
Prostaglandin D2 ethanolamide (PGD2-EA) is a bioactive lipid produced by the sequential metabolism of anandamide (arachidonoyl ethanolamide) by cyclooxygenase (COX) enzymes, in particular by COX-2, and PGD synthase. The biosynthesis of PGD2-EA from anandamide can also be increased when anandamide metabolism is diminished by deletion of fatty acid amide hydrolase. PGD2-EA is inactive against recombinant prostanoid receptors, including the D prostanoid receptor. It increases the frequency of minia... | |||
T37724 | Lumula | ||
There are currently four prostaglandin (PG) derivatives which have been approved for human clinical use for the treatment of glaucoma. The names of the PGs and the concentrations of the approved doses are: travoprost (40 μg/ml), latanoprost (50 μg/ml), bimatoprost (300 μg/ml), and unoprostone (1,500 μg/ml). All of these compounds are modified at C-1 in order to act as lipophilic prodrugs in the eye. All have also been postulated to function via activation of the prostanoid FP receptor. Unoprosto... | |||
T14139 |
Aganepag
AGN 210937 |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
Aganepag, a potent Prostanoid EP2 receptor agonist, exhibits remarkable selectivity with an EC50 of 0.19 nM, demonstrating no activity at the EP4 receptor. Its applications are primarily in the fields of wound healing, scar reduction, scar prevention, and the treatment and prevention of wrinkles. | |||
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 ... | |||
T37441 |
KMN-80
|
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The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other pro... | |||
T37383 |
1,2,3-Trilinoelaidoyl-rac-glycerol
|
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1,2,3-Trilinoelaidoyl-rac-glycerol is a triacylglycerol that contains linoelaidic acid at the sn-1, sn-2, and sn-3 positions. Dietary administration of 1,2,3-trilinoelaidoyl-rac-glycerol (0.6-6.3% w/w) lowers serum levels of thromboxane B2 , prostaglandin F2 (PGF2), and PGE in rats.1 |1. Bruckner, G., Goswami, S., and Kinsella, J.E. Dietary trilinoelaidate: Effects on organ fatty acid composition, prostanoid biosynthesis and platelet function in rats. J. Nutr. 114(1), 58-67 (1984). |
Cat. No. | Product Name | Target | Signaling Pathways |
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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。 |