Prostaglandin Receptor Antagonist

CT-133 is a selective and potent CRTH2 Receptor antagonist, with a K_i value of 2.2 nM. The K_i value for the DP1 receptor is greater than 3800 nM. CT-133 inhibits neutrophil migration induced by PGD2 (HY-101988). CT-133 significantly alleviates lung inflammation and improves lung function impairment in a mouse model of acute lung injury (ALI) induced by cigarette smoke. CT-133 effectively inhibits the excessive expression of pro-inflammatory cytokines (TNF-α, IL-1β, and IL-6) and chemokines (KC), and reverses the inhibition of the anti-inflammatory factor IL-10. CT-133 can be used for the study of ALI.

S-5751 is an orally active prostaglandin DP receptor antagonist. S-5751 inhibits cAMP generation in platelet-rich plasma induced by PGD2 with IC₅₀ 0.12 μM. S-5751 has anti-inflammatory activity. S-5751 can be used in asthma research.

L 655240 is thromboxane antagonist. L 655240 attenuates early ischemia- and reperfusion-induced arrhythmias in a canine model of coronary artery occlusion. L 655240 also involves in cancer and autoimmune disorders.

ONO-8539 is an orally active prostanoid EP1 receptor antagonist with competitive, insurmountable binding and slow receptor dissociation for long-duration inhibition. ONO-8539 modulates afferent nerve function related to bladder activity, inhibits detrusor overactivity-related contractions, decreases nonvoiding contractions and voiding duration, and increases uroflow rate with ATP (HY-B2176)-induced detrusor overactivity. ONO-8539 attenuates acid-induced heartburn symptoms, extends time to first heartburn sensation, and prevents primary hypersensitivity after distal esophageal acidification. ONO-8539 can be used for the research of overactive bladder and gastroesophageal reflux disease.

EP3 antagonist 2 (Compound Exp 1) is a potent and selective EP3 receptor antagonist. EP3 antagonist 2 has a strong binding affinity for the human EP3 receptor (K_i: 3.3 nM) and significant antagonistic activity (IC₅₀: 30.8 nM, determined by cellular cAMP levels).

SC 51089 free base (Standard) is the analytical standard of SC 51089 (free base) (HY-108563A). This product is intended for research and analytical applications. SC 51089 free base is a selective antagonist of prostaglandin E2 EP1 receptor, with K_is of 1.3, 11.2, 17.5, and 61.1 μM for EP1, TP, EP3, and FP receptors, respectively. SC 51089 free base exhibits neuroprotective activity.

SC-19220 (Standard) is the analytical standard of SC-19220 (HY-102065). This product is intended for research and analytical applications. SC-19220 is a prostaglandin E₂ receptor EP1 antagonist. SC-19220 blocks functional EP1 receptor activation, and RANK/RANKL signaling pathway. SC-19220 inhibits osteoclast formation and bone resorption by pre-existing osteoclasts. SC-19220 can be used for the research of osteoporotic disorders, inflammatory bone resorption.

L 657925 is a potent thromboxane A2 (TXA2) antagonist. L 657925 selectively abolishes ONO 11113-evoked transient increment in [Ca2²⁺].

Setipiprant (Standard) is the analytical standard of Setipiprant. This product is intended for research and analytical applications. Setipiprant (ACT-129968) is an orally active and selective CRTH2 antagonist. Setipiprant interacts with hCRTH2 receptor with an IC50 value of 6 nM. Setipiprant inhibits prostanoid receptors hDP1 and hEP2 with IC50 values of 1290 and 2600 nM, respectively. Setipiprant can be used for the research of asthma and rhinitis.

AH 6809 (Standard) is the analytical standard of AH 6809. This product is intended for research and analytical applications. AH 6809 is an antagonist of EP and DP receptor, with Kis of 1217, 1150, 1597, and 1415 nM for the cloned human EP1, EP2, EP3-III, and DP receptor respectively. AH 6809 has a Ki of 350 nM for mouse EP2 receptor.

Linotroban (HN11500), a Sulotroban (HY-158332) derivative, is an orally active, potent non-prostanoid thromboxane receptor antagonist (TXRA) with a strong antiplatelet profile. Linotroban is used as antithrombotic agent.

Pexopiprant (Standard) is the analytical standard of Pexopiprant (HY-109186). This product is intended for research and analytical applications. Pexopiprant is an oral antagonist of the prostaglandin D2 receptor 2 (DP2),K_i ＜ 100nM. Pexopiprant can be used in studies of asthma.

MF498 (Standard) is the analytical standard of MF498 (HY-10794). This product is intended for research and analytical applications. MF498 is a selective and orally active E prostanoid Receptor 4 (EP4) antagonist with a K_i value of 0.7 nM. MF498 can be used in the research of inflammation, such as rheumatoid and osteoarthritis.

Ifetroban sodium (Standard) is the analytical standard of Ifetroban sodium (HY-105218A). This product is intended for research and analytical applications. 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.

L-641953 is an orally active, selective TXA/PG-END receptor (thromboxane-prostaglandin endoperoxide receptor) antagonist. L-641953 significantly inhibits arachidonic acid-induced bronchoconstriction. L-641953 may be used in cardiovascular disease research.

Vapiprost (GR 32191) is a thromboxane A2 receptor (TXA2 Receptor) antagonist. Vapiprost hydrochloride (GR 32191 hydrochloride) inhibits the aggregation and ATP release stimulated with U-46619, collagen or arachidonic acid (AA) at an IC₅₀ of less than 2.1×10^-8 M.

Grapiprant (Standard) is the analytical standard of Grapiprant. This product is intended for research and analytical applications. Grapiprant (CJ-023423) is a selective EP4 receptor antagonist whose physiological ligand is prostaglandin E2 (PGE2). Grapiprant displaces [3H]-PGE2 (1 nM) binding to dog recombinant EP4 receptor with IC50 value of 35 nM and Ki value of 24 nM. Grapiprant has the potential for osteoarthritic pain and inflammation treatment .

CRTH2-IN-1 (Ramatroban analog) is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist with an IC₅₀ of 6 nM in a human DP2 binding assay.

(S)-AL 8810 is an 11β-fluoro analog of PGF2α that acts as a potent and selective antagonist at the FP receptor. (S)-AL 8810 is the C-15 epimer of AL 8810, having the inverse, (S), or "natural" configuration at C-15 relative to AL 8810, which is 15-(R).

AZD1981 (Standard) is the analytical standard of AZD1981. This product is intended for research and analytical applications. AZD1981 is the antagonist for GPR44 (also known also PTGDR2, DP2 or CRTh). AZD1981 blocks the binding of PGD2 to CRTH2. AZD1981 exhibits immunomodulatory effects and can be used in research of chronic spontaneous urticaria.