ip receptor

L 888607 is an effective and selective CRTH2 agonist (Ki: 0.8 nM).

MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib(Iressa). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax> 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioavailable in mice following ip administration.

RO3244794 is a selective prostacyclin (IP) receptor antagonist that can be used to study liver injury.

1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist known for its anti-tumor properties.

AMG 487 is a potent and selective antagonist of chemokine (C-X-C motif) receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.

KAG-308 is an effective selective and orally active agonist of the EP4 receptor (Ki: 2.57 nM and EC50: 17 nM for human EP4 receptor), more selective over EP1, EP2, EP3, and IP receptor. KAG-308 suppresses colitis and promotes histological mucosal healing,

Taprostene sodium acts as a partial agonist of the prostacyclin (IP) receptor in the prostaglandin class. It interacts with Prostaglandin E2 (PGE2), ONO-AE1-259 (a selective EP2 agonist), and acetylcholine. Taprostene sodium offers significant cardioprotective effects.

Prostaglandin I2 is an unstable prostaglandin compound that inhibits platelet aggregation and induces vasodilation in the pulmonary vasculature via the "I prostanoid" (IP) receptor. AFP 07, a 7,7-difluoroprostacyclin derivative, serves as a selective and potent agonist for the IP receptor (Ki=0.561 nM). It exhibits weaker affinity for EP receptors, with a Ki value of > 100 nM for EP1-3 and > 10 nM for EP4. The compound 16(R)-AFP 07 free acid is an enantiomer of AFP 07. Its biological properties, particularly those involving IP and EP receptors, are yet to be fully assessed.

AMG 487 is an effective and selective antagonist of chemokine receptor 3. AMG 487 inhibited CXCR3-mediated cell migration induced by three CXCR3 chemokines, IP-10, ITAC and MIG (IC50: 8, 15 and 36 nM, respectively).

AFP 07 free acid is a 7,7-difluoroprostacyclin derivative. It also acts as a selective and highly potent agonist for the IP receptor.

FR-181157, a novel prostaglandin (PG) mimetic, shows high potency and agonist efficacy at the IP receptor and has good bioavailability.

Ono 1301 is a prostaglandin I2 mimetic coumpound with inhibitory activity against thromboxane A2 synthase. Ono 1301 suppresses pancreatic fibrosis in the DBTC-induced CP model by inhibiting monocyte activity not only with induction of HGF but also by Ono

SR142948A is a selective and reversible non-peptide neurotensin receptor antagonist capable of blocking hypothermia and analgesic effects induced by intracerebroventricular injection of NT, and capable of concentration- and volume-dependent blockade of NMDA-induced dopamine release.

Alprostadil sodium is a prostaglandin receptor ligand with Ki values of 36, 10, 1.1, 2.1, and 33 nM for EP1, EP2, EP3, EP4, and IP, respectively, in mice.It induces vasodilatation and inhibits platelet aggregation, and it can be used as a vasodilator for the study of peripheral vascular disease.

The inositol phosphates (IPs) are a family of molecules produced by altering the phosphorylation status of each of the six carbons on the cyclic inositol structure. They act as second messengers, regulating a wide array of cellular functions. D-myo-inositol-1,3,4,6-tetraphosphate(Ins(1,3,4,6)-P4) largely acts an intermediate, serving as substrate for inositol-1,3,4,6-tetraphosphate 5-kinase to produce inositol-1,3,4,5,6-pentaphosphate, or inositol-1,3,4,6-tetraphosphate 2-kinase to give inositol-1,2,3,4,6-pentaphosphate. These inositol pentaphosphates can be further phosphorylated to produce inositol-1,2,3,4,5,6-hexakisphosphate, or phytic acid, which serves diverse roles in eukaryotic tissues. Ins(1,3,4,6)-P4 is a poor activator of the inositol 1,4,5-trisphospate receptor in vitro. Other functions of this IP remain to be elucidated.

STING agonist 12b is an agonist of stimulator of interferon genes (STING).1It binds to STING (Kd= 26.4 μM) and induces interferon reporter gene expression in cells expressing human or mouse STING (EC50s = 7.45 and 10.23 μM, respectively). STING agonist 12b (40 μM) induces expression of TNF-a, IL-6, IP-10, and IL-1b in THP-1 cells. 1.Hou, S., Lan, X.-j., Li, W., et al.Design, synthesis and biological evaluation of acridone analogues as novel STING receptor agonistsBioorg. Chem.95103556(2020)

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 and platelet preparations. Br.J.Pharmacol. 149 110 PMID:16880763 |Bley et al (2006) RO1138452 and RO3244794: characterization of structurally distinct, potent and selective IP (prostacyclin) receptor antagonists. Br.J.Pharmacol. 147 335 PMID:16331286

MRE-269 (ACT-333679) is an orally available and long-acting prostacyclin receptor agonist prodrug. MRE-269(ACT-333679) is used for the treatment of pulmonary arterial hypertension. MRE-269(ACT-333679) is an active metabolite of Selexipag (S253150).

Ralinepag (APD811) is a potent, orally bioavailable agonist of non-prostanoid prostacyclin (IP) receptor, with EC50s of 8.5 nM, 530 nM and 850 nM for human and rat IP receptor and human DP1 receptor, respectively.

Anisotropine Methylbromide is an anticholinergic agent and has been used for relief of gastrointestinal spasm and for the suppression of gastric acid secretion.

Treprostinil (Orenitram) is a potent DP1, IP and EP2 agonist (EC50: 0.6/1.9/6.2 nM).

Treprostinil Sodium (UT-15) is a potent DP1, IP and EP2 agonist (EC50: 0.6/1.9/6.2 nM).

ROS 234 is a highly effective H3 antagonist, demonstrating a strong binding affinity (pK B) of 9.46 for the Guinea-pig ileum H3 receptor and a pKi of 8.90 for the Rat cerebral cortex H3 receptor. Additionally, it exhibits an ex vivo ED50 of 19.12 mg/kg (ip) in the Rat cerebral cortex. It should be noted that ROS 234 demonstrates limited central access, as reported in [1] and [2].

Cicaprost (ZK 96480) is a potent prostacyclin receptor (IP) agonist, inducing artery relaxation through concentration-dependent mechanisms with an EC50 value of 5.8 nM [1].