2. Signaling Pathways
  3. GPCR/G Protein
  4. Prostaglandin Receptor
  5. Prostaglandin Receptor Isoform
  6. Prostaglandin Receptor Antagonist

Prostaglandin Receptor Antagonist

Prostaglandin Receptor Antagonists (48):

Cat. No. Product Name Effect Purity
  • HY-100449
    AL-8810
    		Antagonist 99.00%
    AL-8810 is a potent and selective antagonist of the PGF 2α receptor (FP receptor). AL-8810 is an activator of MAPK and ERK1/2. The Ki of the FP receptor of mouse 3T3 cells and rat A7r5 cells are 0.2±0.06 μM and 0.4±0.1 μM, respectively. AL-8810 can be used in the study of elevated intraocular pressure (OHT) and primary open-angle glaucoma (POAG).
  • HY-16978
    TG6-10-1
    		Antagonist 99.92%
    TG6-10-1 is an EP2 antagonist, shows low-nanomolar antagonist activity against only EP2, >300-fold selectivity over human EP3, EP4, and IP receptors, 100-fold selectivity over EP1 receptors.
  • HY-12182A
    ONO-8711 dicyclohexylamine
    		Antagonist 98.09%
    ONO-8711 dicyclohexylamine is a selective and orally active EP1 competitive antagonist with Ki value of 0.6 nM and 1.7 nM for human and mouse EP1 respectively. ONO-8711 dicyclohexylamine effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer.
  • HY-164049
    TG8-260
    		Antagonist 98.25%
    TG8-260 is a second-generation EP2 antagonist developed to alleviate the pathology of central nervous system and peripheral diseases driven by inflammation. TG8-260 can reduce neuroinflammation and gliosis in the hippocampus of rats after pilocarpine-induced persistent epileptic status. Pharmacokinetic data of TG8-260 showed that its plasma half-life was 2.14 hours and its oral bioavailability was 77.3%. TG8-260 is also a potent inhibitor of CYP450 and shows antagonistic activity in inhibiting EP2 receptor-mediated inflammatory gene expression in BV2-hEP2 microglia, which is suitable for studying anti-inflammatory pathways in animal models of peripheral inflammatory diseases.
  • HY-15342
    Timapiprant
    		Antagonist 99.48%
    Timapiprant (OC000459) is a potent, selective, and orally active D prostanoid receptor 2 (DP2, also known as CRTH2) antagonist. Timapiprant (OC000459) potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), rat recombinant DP2 (Ki=3 nM), and human native DP2 (Ki=4 nM). Timapiprant (OC000459) inhibits mast cell activation of Th2 lymphocytes and eosinophils.
  • HY-14973
    Vidupiprant
    		Antagonist 98.33%
    Vidupiprant (AMG 853) is a phenylacetic acid derivative. Vidupiprant is a potent and orally active CRTH2 (DP2) and prostanoid D receptor (DP or DP1) dual antagonist with IC50s of 3 nM and 4 nM in buffer, and 8 nM and 35 nM in human plasma, respectively. Vidupiprant has the potential for asthma treatment.
  • HY-16991
    Terutroban
    		Antagonist 99.91%
    Terutroban is a thromboxane-prostaglandin receptor antagonist.
  • HY-105218A
    Ifetroban sodium
    		Antagonist 99.24%
    Ifetroban (BMS-180291) sodium is an orally active antagonist of thromboxane A2 (TXA2) or prostaglandin H2 (PGH2) receptor. Ifetroban sodium shows antiplatelet activity, and inhibits tumor cell migration without affecting cell proliferation. Ifetroban sodium can be used for myocardial ischemia, hypertension, stroke, thrombosis, cardiomyopathy research.
  • HY-133123
    EP4 receptor antagonist 1
    		Antagonist 99.66%
    EP4 receptor antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist for cancer immunotherapy. EP4 receptor antagonist 1 inhibits human and mouse EP4 receptor with IC50s of 6.1 nM and 16.2 nM, respectively. IC50s >10 μM for human EP1, EP2,and EP3 receptors.
  • HY-108972
    SQ 29548
    		Antagonist ≥99.0%
    SQ 29548, a high affinity radioligand, is a selective thromboxane-prostanoid (TP) receptor antagonist.
  • HY-101430
    PGD2-IN-1
    		Antagonist 98.24%
    PGD2-IN-1 is an antagonist of DP extracted from patent WO 2006044732 A2, example 15 (d); has an IC50 of 0.3 nM.
  • HY-13213
    AM211
    		Antagonist 98.79%
    AM211 is a potent, selective and orally bioavailable prostaglandin D2 (PGD2) receptor type 2 (DP2) antagonist, with IC50s of 4.9 nM, 7.8 nM, 4.9 nM, 10.4 nM for human, mouse, guinea pig, and rat DP2, respectively.
  • HY-156649
    Vorbipiprant
    		Antagonist 99.72%
    Vorbipiprant (CR6086) is an EP4 receptor antagonist, serving as a targeted immunomodulator. Thus, Vorbipiprant is also a potential immune checkpoint inhibitor, to turn cold tumors into hot tumors. Vorbipiprant also antagonizes PGE2-stimulated cAMP production (IC50=22 nM). Vorbipiprant exhibit striking DMARD effects in rodents, and anti-inflammatory activity to inhibt immune-mediated inflammatory diseases.
  • HY-12284
    NVP-QAV680
    		Antagonist
    NVP-QAV680 is a potent and selective CRTh2 receptor antagonist with low nanomolar (nM) functional potency to inhibit CRTh2-driven activation of human eosinophils and Th2 lymphocytes. NVP-QAV680 exhibits good oral bioavailability and demonstrates efficacy in CRTh2-dependent mechanisms and allergic disease models in rats.
  • HY-111304
    MF266-1
    		Antagonist
    MF266-1 is a selective E prostanoid receptor 1 (EP1) antagonist with an Ki value of 3.8 nM. MF266-1 also has moderate selectivity for thromboxane A2 receptor (TP). MF266-1 is promising for research of arthritis.
  • HY-100570
    KF15766
    		Antagonist
    KF15766 (compd 34E) is an orally active TXA2 and H1 dual antagonist with Kis of 740 and 20 nM. KF15766 can be used for antiallergic research.
  • HY-153256
    EP3 antagonist 4
    		Antagonist
    EP3 antagonist 4 (Compound 28) is an EP3 antagonist, with a Ki value of 2 nM for hEP. EP3 antagonist 4 shows low in vivo clearance, high oral AUC, and good bioavailability in the rat full PK studies. EP3 antagonist 4 can be used for research of beta cell dysfunction in diabetes.
  • HY-118388
    AS604872
    		Antagonist
    AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour.
  • HY-112265
    CRTh2 antagonist 1
    		Antagonist
    CRTh2 antagonist 1 is a CRTh2 antagonist with an IC50 of 89 nM.
  • HY-160664
    TP receptor antagonist-2
    		Antagonist
    TP receptor antagonist-2 (example 7n) is a thromboxane A2 receptor (TP receptor) antagonist, with IC50 values of 5.64 and 5.27 μM for TPα and TPβ, respectively. TP receptor antagonist-2 inhibits platelet aggregation.