Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10889 |
CRTh2 antagonist 2
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
CRTh2 antagonist 2 是一种有效的选择性 CRTH2 抑制剂,对 CRTH2 的 IC50 值为 ≤10 nM。CRTh2 antagonist 2 可用于雄激素性脱发的研究。 | |||
T10084 |
CRTh2 antagonist 1
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
CRTh2 antagonist 1 是 CRTh2 拮抗剂,IC50 值为 89 nM。 | |||
T10890 | CRTh2 antagonist 3 | Others | Others |
CRTh2 antagonist 3 is a powerful chemokine receptor homologous molecule expressed on Th2 cell (CRTh2) antagonists. CRTh2 antagonist 3 enhanced the activity of PDK1 on short peptide substrates with EC50 of 2 μM and Kd of 8.4 μM. CRTh2 antagonist 3 has 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. | |||
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。 | |||
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。 | |||
T3965 |
Fevipiprant
QAW039,NVP-QAW039,非维匹仑 |
GPR; Prostaglandin Receptor | Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation |
Fevipiprant (NVP-QAW039) 是一种选择性、强效、可逆的竞争性 CRTh2 拮抗剂,KD 值为1.1 nM,IC50为0.44 nM,能够引发人体嗜酸性粒细胞的形状变化。 | |||
T3520 |
Setipiprant
KYTH-105,塞替匹仑,ACT-129968 |
GPR; Prostaglandin Receptor | Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation |
Setipiprant (ACT-129968) 是一种口服的选择性 CRTH2 拮抗剂,IC50为6.0 nM。 | |||
T10691 |
CAY10595
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
CAY10595 是 CRTh2 (DP2) 受体的拮抗剂,Ki 为 10 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。 | |||
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。 | |||
T77601 |
(2-{[2-(2-fluorophenoxy)ethyl]sulfanyl}-1H-benzimidazol-1-yl)acetic acid
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
(2-{[2-(2-fluorophenoxy)ethyl]sulfanyl}-1H-benzimidazol-1-yl)acetic acid是一种前列腺素类 CRTH2拮抗剂,其IC50< 10 μM,可用于研究鼻炎、慢性阻塞性肺疾病、类风湿性关节炎、湿疹和结膜炎。 | |||
T2396 |
Ramatroban
BAY u3405,雷马曲班 |
GPR; Prostaglandin Receptor; PPAR | DNA Damage/DNA Repair; Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Metabolism |
Ramatroban (BAY u3405) 是一种血栓素 A(2) (TxA(2)) 拮抗剂,IC50为 14 nM。它还通过抑制PGD2结合从而拮抗CRTH2,IC50为113 nM。它用于治疗过敏性鼻炎,可用于治疗哮喘的研究。 | |||
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。 | |||
T28927 |
TASP0412098
TASP 0412098,TASP-0412098 |
||
TASP0412098 is a potent, selective CRTH2 antagonist with oral activity. | |||
TQ0051 |
MK-7246
|
GPR | Endocrinology/Hormones; GPCR/G Protein |
MK-7246 is a potent and specific CRTH2 antagonist (Ki: 2.5 nM). | |||
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). | |||
T37328 |
Prostaglandin H1
Prostaglandin H1 |
||
Prostaglandin H1 是 DGLA 的环氧化酶代谢物,也是一种 CRTh2 激动剂以及 1 系列抗炎前列腺素的前体物质。Prostaglandin H1 可用于炎症的研究。 | |||
T15828 |
L 888607
|
Others | Others |
L 888607 is an effective and selective CRTH2 agonist (Ki: 0.8 nM). | |||
T28925 |
TASP0376377
TASP-0376377,TASP 0376377 |
||
TASP0376377 is a potent antagonist of CRTH2. | |||
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 | |||
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。 | |||
T12067 |
MK-7246 S enantiomer
|
Others | Others |
MK-7246 S enantiomer is a potent and selective CRTH2 antagonist. | |||
T28221 |
NVP-QAV-680
NVP-QAV680,QAV690 free acid,NVP,QAV-690 free acid,NVPQAV680,QAV 690 free acid |
||
NVP-QAV-680 is a potent and selective antagonist of CRTh2 receptor. NVP-QAV-680 has nM functional potency for inhibition of CRTh2 driven human eosinophil and Th2 lymphocyte activation in vitro. | |||
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... | |||
T71245 |
ARRY-502
|
||
ARRY-502 is a CRTH2 antagonist. Regulation of cytokine activity is important in molecularly targeted therapies for 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. |