attr

Soulattrolide是一种由Calophyllum (Calophyllaceae)雨林树叶合成的天然香豆素，作为HIV-1逆转录酶（RT-HIV-1）的强效抑制剂，并显示出对Mycobacterium tuberculosis的活性。

cis-3-Hexen-1-ol ((Z)-3-Hexen-1-ol) 是发现于许多新鲜水果和蔬菜中的一种绿色草味化合物，常用作加工食品的附加风味剂，以提供新鲜的绿色品质，也是多种昆虫的引诱剂。

NFAT Transcription Factor Regulator-1 是 IL-2 合成 的抑制剂，IC50 值为182 nM。

Tazemetostat trihydrochloride is a selective and orally available inhibitor of EZH2 (IC50: 4 nM for rat EZH2). It inhibits the activity of human PRC2-containing wild-type EZH2 (Ki: 2.5 nM). It inhibits EZH2 (IC50s: 11 and 16 nM in peptide assay and nucleo

Clesacostat（PF-05221304），是一种高效且选择性的ACC抑制剂（hACC1 IC50 = 13nM；hACC2 IC50 = 9nM）。在动物模型中，PF-05221304特异性抑制肝脏的DNL，同时在非人类灵长类动物模型中展示出对血小板减少具有显著的安全裕度。

Neuromedin U-23 (NMU-23) is a neuropeptide involved in diverse biological processes, including smooth muscle contraction, energy homeostasis, and nociception.1It is an agonist of neuromedin-U receptor 1 (NMUR1; EC50= 0.17 nM for the human receptor in a calcium mobilization assay using HEK293 cells) and NMUR2 (EC50= ~1.4-2 nM for arachidonic acid release in CHO cells expressing the human receptor).2,3NMU-23 (1 μM) induces contractions in isolated rat colon smooth muscle strips.4It decreases body weight and food intake and increases core body temperature in mice when administered at a dose of 36 μg/animal.5Intrathecal administration of NMU-23 decreases the mechanical pain threshold in the von Frey test in rats.6 1.Mitchell, J.D., Maguire, J.J., and Davenport, A.P.Emerging pharmacology and physiology of neuromedin U and the structurally related peptide neuromedin SBr. J. Pharmacol.158(1)87-103(2009) 2.Szekeres, P.G., Muir, A.I., Spinage, L.D., et al.Neuromedin U is a potent agonist at the orphan G protein-coupled receptor FM3J. Biol. Chem.275(27)20247-20250(2000) 3.Hosoya, M., Moriya, T., Kawamata, Y., et al.Identification and functional characterization of a novel subtype of neuromedin U receptorJ. Biol. Chem.275(38)29528-29532(2000) 4.Brighton, P.J., Wise, A., Dass, N.B., et al.Paradoxical behavior of neuromedin U in isolated smooth muscle cells and intact tissueJ. Pharmacol. Exp. Ther.325(1)154-164(2008) 5.Peier, A., Kosinski, J., Cox-York, K., et al.The antiobesity effects of centrally administered neuromedin U and neuromedin S are mediated predominantly by the neuromedin U receptor 2 (NMUR2)Endocrinology150(7)3101-3109(2009) 6.Yu, X.H., Cao, C.Q., Mennicken, F., et al.Pro-nociceptive effects of neuromedin U in ratNeuroscience120(2)467-474(2003)

Neuropeptide Y (NPY) (3-36) is a C-terminal fragment of NPY, a neuropeptide involved in controlling appetite, blood pressure, cardiac contractility, and intestinal secretion. NPY (3-36) is an endogenous peptide produced by cleavage of NPY by dipeptidyl peptidase 4 (DPP-4). It binds selectively to the NPY receptor Y2 (Ki = 0.41 nM in CHP 234 cells) over the Y1 receptor, where it does not bind at concentrations up to 1 μM. NPY (3-36) (0.1 nM) increases migration of human umbilical vein endothelial cells (HUVECs) by 80% after 12 hours in an in vitro wound closure assay. NPY (3-36) corresponds to residues 3-36 of the human and rat protein sequence.

Cortistatin-29 (1-13) is a neuropeptide and cleavage product of cortistatin-29 , which is a cleavage product of procortistatin. Cortistatin-29 (1-13) corresponds to the first 13 amino acids of cortistatin-29.

GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr- -) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans. Dig. Dis. Sci. 34(5), 703-708 (1989).2. Gelling, R.W., Du, X.Q., Dichmann, D.S., et al. Lower blood glucose, hyperglucagonemia, and pancreatic α cell hyperplasia in glucagon receptor knockout mice. Proc. Natl. Acad. Sci. U.S.A. 100(3), 1438-1443 (2003). GLP-1 amide is a peptide hormone cleaved from proglucagon in the pancreas.1,2 Mice lacking the glucagon receptor (Gcgr- -) have approximately nine-fold higher levels of total GLP-1 amide, including GLP-1 (1-36) amide and truncated GLP-1 (7-36) amide , in pancreatic tissue compared to wild-type mice.2 References1. Schjoldager, B.T., Mortensen, P.E., Christiansen, J., et al. GLP-1 (glucagon-like peptide 1) and truncated GLP-1, fragments of human proglucagon, inhibit gastric acid secretion in humans. Dig. Dis. Sci. 34(5), 703-708 (1989).2. Gelling, R.W., Du, X.Q., Dichmann, D.S., et al. Lower blood glucose, hyperglucagonemia, and pancreatic α cell hyperplasia in glucagon receptor knockout mice. Proc. Natl. Acad. Sci. U.S.A. 100(3), 1438-1443 (2003).

Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, SK-N-MC, and T47D cells). In vivo, in newborn pigs, PACAP (6-27) (10 μM) inhibits vasodilation of pial arterioles induced by PACAP (1-27) and PACAP (1-38) . It also inhibits PACAP (1-27)-stimulated increases in plasma insulin and glucagon levels and pancreatic venous blood flow in dogs when administered locally to the pancreas at a dose of 500 μg.

PACAP-related peptide (PRP) is an endogenous 29-amino acid peptide that belongs to the secretin/glucagon superfamily of peptides, which includes secretin , glucagon , glucagon-like peptide-1 , GLP-2 , and pituitary adenylate cyclase-activating polypeptide . It is expressed in rat hypothalamus as well as within the nerves of the median eminence, the anterior pituitary, bed nucleus of the stria terminalis, cerebellum, cerebral cortex, and amygdala. PRP is also expressed in vaginal, uterine cervical, uterine horn, fallopian tube, and ovarian tissues from the rat female genital tract and is present in extracts of male testis tissue.

Tyr-α-CGRP (rat) is an N-terminally tyrosinated analog of the neuropeptide α-CGRP that induces a fall in resting tension of isolated opossum internal anal sphincter (IAS) with an EC50 value of 178 nM.

ζ-Stat trisodium (NSC37044 trisodium) is a potent and selective inhibitor of protein kinase C-ζ (PKC-ζ), exhibiting an IC50 of 5 μM. It effectively suppresses the proliferation of melanoma cell lines and promotes apoptosis. Moreover, ζ-Stat trisodium demonstrates notable antitumor activity in vitro.

TLR7 8 agonist 1是一种 toll 样受体 TLR7 TLR8 激动剂，具有抗癌抗病毒活性，可用于研究与免疫相关的疾病。

H-201-70 is a partial beta1 agonist with adrenoreceptor stimulatory effects.

Ninerafaxstat trihydrochloride 将细胞代谢由脂肪酸氧化转变为葡萄糖氧化。 Ninerafaxstat trihydrochloride 改善整体线粒体呼吸并减少脂肪酸氧化，从而抑制癌细胞的增殖和生长。

PITB是一种选择性且具口服活性的TTR聚集抑制剂，主要用于研究ATTR疾病。