Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T68766 | Dp2mT | ||
Dp2mT is an iron chelator which inhibits HIV-1 transcription. | |||
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。 | |||
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。 | |||
T10691 |
CAY10595
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
CAY10595 是 CRTh2 (DP2) 受体的拮抗剂,Ki 为 10 nM。 | |||
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。 | |||
T7652 |
AM211
AM211 free acid |
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
AM211 (AM211 free acid) 是可口服的选择性前列腺素受体拮抗剂,对人、小鼠、豚鼠和大鼠的 DP2 的IC50值分别为 4.9、7.8、4.9 和 10.4 nM。 | |||
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。 | |||
T14565 |
BI-671800
AP-761,Cmpd A |
GPR; Prostaglandin Receptor | Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation |
BI-671800 (AP-761) 是高特异性的前列腺素 D2 受体拮抗剂,对哮喘有研究潜力,对人和小鼠 CRTH2 转染细胞中 PGD2 结合 CRTH2 的 IC50值分别为 4.5 和 3.7 nM。 | |||
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 | |||
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. | |||
T41073 |
Pexopiprant
|
||
Pexopiprant, a potent oral antagonist of the prostaglandin D2 receptor 2 (DP2) with a K i value less than 100nM, is a valuable compound for asthma research. | |||
T70989 |
AM-461 sodium
|
||
AM-461 sodium is the sodium salt of AM-461 --- a novel DP2 receptor antagonist | |||
T27799 |
LAS191859
LAS-191859,LAS 191859 |
||
LAS191859 is a CRTH2/DP2 antagonist with IC50 values of 7.6, 9.58, 14 and 15.5nM for recombinant guinea pig, human, rat and mouse CRTH2/DP2 receptors, respectively. LAS191859 has a residence time half-life of 21h at CRTh2 that translates into a long-lasti | |||
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... | |||
T71244 | AM-461 | ||
AM-461 is a DP2 receptor antagonist. | |||
T82239 |
HAP-1
|
||
HAP-1为针对滑膜细胞的转导肽,可促进蛋白质复合物在人类及兔子滑膜细胞中的特异性内吞作用。当HAP-1与抗菌肽(KLAK)2融合时,形成促进细胞凋亡的肽DP2。 | |||
T37264 |
15(R)-15-methyl Prostaglandin D2
15(R)15methyl PGD2 |
GPR | Endocrinology/Hormones; GPCR/G Protein |
15(R)-15-methyl Prostaglandin D2 (15(R)15methyl PGD2) 是一种 PGD2 合成类似物,也是一种具有选择性和强效性的 CRTH2/DP2 受体激动剂,可调节嗜酸性粒细胞 CD11b 表达、肌动蛋白聚合和趋化。 | |||
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. | |||
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. | |||
T14211 | AMG-009 | Others | Others |
AMG-009 is a prostaglandin D2 antagonist. For CRTH2 and DP receptors, the IC50s are 3 nM and 12 nM, respectively. | |||
T16097 |
MK-8318
|
Others | Others |
MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM). | |||
T15828 |
L 888607
|
Others | Others |
L 888607 is an effective and selective CRTH2 agonist (Ki: 0.8 nM). |