ip receptor

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

[D-p-Cl-Phe6,Leu17]-VIP acetate 是一种竞争性和选择性的血管活性肠肽 (VIP) 受体拮抗剂 (IC50 = 125.8 nM)。

VIP(6-28)(human, rat, porcine, bovine) acetate 是外源性血管活性肠肽 (VIP) 受体对颈上神经节 (SCG) 中 cAMP 作用的拮抗剂。

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,

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。

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.

RO3244794是一种具有选择性的前列环素 （IP）受体拮抗剂，可用于研究肝脏损伤。

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。

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。

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。

Prostaglandin I2 是一种不稳定的前列腺素，借助“I 前列腺素类物质”(IP) 受体来抑制血小板聚集并促进肺血管床的血管扩张。AFP 07 是一种 7,7-二氟前列环素衍生物，充当 IP 受体的选择性高效激动剂 (Ki=0.561 nM)。在EP受体上，AFP 07 的亲和力相对较弱，对 EP1-3 的 Ki 值大于 100 nM，对 EP4 的 Ki 值大于 10 nM。16(R)-AFP 07 free acid 是其差向异构体，其在生物学特性上（尤其是通过 IP 和 EP 受体）仍需进一步研究。

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

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。