ip receptor

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

Treprostinil (Orenitram) 是有效的 DP1、IP 和 EP2 激动剂，EC50分别为0.6、1.9 和 6.2 nM。

Treprostinil Sodium (UT-15) 是有效的 DP1、IP 和 EP2 激动剂，EC50分别为0.6、1.9 和 6.2 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.

AMG 487 是可口服的选择性趋化因子受体3拮抗剂，对 I-IP-10、I-ITAC 和 MIG 的 IC50 值分别为 8、15 和 36nM。

1V209 (TLR7 agonist T7) 是一种 Toll 样受体 7 (TLR7) 激动剂，可与各种多糖缀合，以改善其水溶性，增强功效并保持低毒性，具有抗肿瘤作用。

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 是一种部分激动prostacyclin (IP)受体的前列腺素类化合物。它能够与Prostaglandin E2 (PGE2)、ONO-AE1-259 (选择性 EP2 激动剂)及乙酰胆碱相互作用，并显示出显著的心脏保护作用。

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是一种选择性和可逆的非肽的neurotensin receptor（神经紧张素受体）拮抗剂，能够阻断由脑室内注射NT引起的体温过低和镇痛效应，能够浓度和体积依赖性地阻断NMDA诱导的多巴胺释放。

Alprostadil sodium 是一种前列腺素受体配体，对小鼠 EP1、EP2、EP3、EP4和 IP 的 Ki 值分别为 36、10、1.1、2.1 和 33 nM。它诱导血管舒张并抑制血小板聚集，可作为血管扩张剂用于外周血管疾病的研究。

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) 是一种口服的长效前列环素受体激动剂前药，是 Selexipag 的活性代谢物，用于治疗肺动脉高压。

Ralinepag (APD811) 是一种可口服的非前列腺素前列环素 (IP) 受体激动剂，对人和大鼠 IP 受体以及人 DP1 受体的 EC50 分别为 8.5、530 和 850 nM。

Anisotropine Methylbromide 是一种抗胆碱能药物，已用于缓解胃肠道痉挛和抑制胃酸分泌。

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 prostacyclin receptor (IP) agonist, which induces relaxation of the artery via concentration-dependent mechanisms. Its EC50 value, determined to be 5.8 nM [1], further highlights its potency.

Treprostinil diethanolamine (UT-15C) 是EP2、DP1和IP 的有效激动剂，对EP2、DP1、IP、EP1、EP4、EP3 和 FPKi 的值分别为 3.6、4.4、32.1、212、826、2505 和 4680 nM。Treprostinil diethanolamine 能够促使 cAMP 的上调，进而维持血管系统内的稳态，并造成人肺动脉的血管扩张。

Cefminox (Sodium) is a new cephamycin antibiotic possessing a D-amino acid moiety derived from D-cysteine at the C-7B side chain. Cefminox is active against a wide range of bacteria, especially Gram-negative and anaerobic bacteria. Cefminox shows excellent in vivo efficacy (ED50) which is higher than would be expected from its in vitro activity (MIC). Moreover, cefminox possesses more potent activity in suppression of bacterial regrowth than other cephems[1]. Cefminox (Sodium) was the most active beta-lactam, with an MIC at which 50% of isolates are inhibited (MIC50) of 1.0 microg ml and an MIC90 of 16.0 microg ml. Cefminox was especially active against Bacteroides fragilis (MIC90, 2.0 microg ml), Bacteroides thetaiotaomicron (MIC90, 4.0 microg ml), fusobacteria (MIC90, 1.0 microg ml), peptostreptococci (MIC90, 2.0 microg ml), and clostridia, including Clostridium difficile (MIC90, 2.0 microg ml)[2]. The use of a single preoperative dose of cefminox was similar in efficacy to 3 doses of cefoxitin administered every 4 hours, and that the serum and tissue concentrations attained provide adequate antibiotic coverage[3]. Moreover, cefminox as a dual agonist of IP (Prostacyclin receptor) and PPARγ (peroxisome proliferator-activated receptor-gamma) that significantly inhibits PASMC proliferation by up-regulation of PTEN (phosphatase and tensin homolog) and cAMP ( cyclic adenosine monophosphate), suggesting that it has potential for treatment of PAH(pulmonary arterial hypertension)[4].