lh 1

LH 1 is an immunostimulant used in antitumor treatment.

LH secretion antagonist 1 is an antagonist of luteinizing hormone secretion with analgesic activity.

[D-Leu6, Val7]-LH-RH (1-9) Ethyl Amide 是 LHRH 多肽类似物。

[D-Glp1,D-Phe2,D-Trp3,6]-LH-RH 是一种黄体激素释放激素 (LHRH) 类似物，可作为 GnRH 受体拮抗剂。

PLH1215 是一种有效地 AHR 抑制剂，可用于调节、限制或抑制 AVIL (advillin) 表达的化合物，能够用于预防和治疗肿瘤。

KPLH1130，一种选择性丙酮酸脱氢酶激酶(PDK)抑制剂，在高脂饮食(HFD)喂养的小鼠中提高了糖耐量。KPLH1130 抑制巨噬细胞极化并减轻了炎症反应。

LH1513 是 l-lysine 的二草酸 (dioxalate) 盐衍生物，能够抑制CaOx结晶，其效果优于柠檬酸盐和丙酮酸盐。在高草酸尿症模型中，LH1513 展示了预防活性的潜力，并且在 Agxt 敲除小鼠中能有效防止尿液中 CaOx 晶体形成。AGXT-1 是一种在线粒体中运作的蛋白质，参与代谢过程。

LH10 是一个基于 fexaramine 的FXR激动剂，EC50为0.14 μM。LH10 展现了肝脏保护作用，有助于减轻由 alpha naphthylisothiocyanate (ANIT) 导致的胆汁淤积、APAP 诱导的急性肝损伤以及非酒精性脂肪性肝炎 (NASH)。

Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal. Glycyl-H-1152 is a selective and potent ROCK inhibitor (IC50 = 11.8 nM for ROCK-II). It is a glycylated isoquinoline compound derived from the therapeutically-important ROCK inhibitor HA-1077 (Fasudil) and exhibits better specificity. Thus, it poorly inhibits Ca2+/calmodulin-dependent kinase type II, protein kinase (PK) G, and Aurora A (IC50 = 2.57, 2.35, and 3.26 μM, respectively) as well as PKA or PKC (IC50 ≥ 10 μM for each). The potency of Glycyl-H-1152 is superior to that of other ROCK inhibitors, including Y-27632 (Ki = 220 nM) and HA-1077 (IC50 = 158 nM).

LH1306 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 that has an IC50 value of 25 nM in a homologous time-resolved fluorescence (HTRF) assay.1 It increases the activation of Jurkat cells expressing PD-1 in co-culture with U2OS or CHO cells expressing PD-L1 (EC50s = 334 and 4,214 nM, respectively, in reporter assays). |1. Basu, S., Yang, J., Xu, B., et al. Design, synthesis, evaluation, and structural studies of C2-symmetric small molecule inhibitors of programmed cell death-1 programmed death-ligand 1 protein-protein interaction. J. Med. Chem. 62(15), 7250-7263 (2019).

LH1307 is an inhibitor of the interaction between programmed cell death 1 (PD-1) and its ligand PD-L1 that has an IC50 value of 3 nM in a homologous time-resolved fluorescence (HTRF) assay.1 It increases the activation of Jurkat cells expressing PD-1 in co-culture with U2OS or CHO cells expressing PD-L1 (EC50s = 79 and 763 nM, respectively, in reporter assays). |1. Basu, S., Yang, J., Xu, B., et al. Design, synthesis, evaluation, and structural studies of C2-symmetric small molecule inhibitors of programmed cell death-1/programmed death-ligand 1 protein-protein interaction. J. Med. Chem. 62(15), 7250-7263 (2019).

Esoxybutynin Free Base is (S)-enantiomer of oxybutynin. Esoxybutynin Free Base exerts antimuscarinic properties. Racemic oxybutynin is used clinically to treat urinary incontinence. Sepracor was developing (S)-oxybutynin, a single-isomer version of Alza's Ditropan (racemic oxybutynin), a muscarinic acetylcholine receptor antagonist, as a potential treatment for urinary incontinence.

ZEL-H16 is an agonist of the histamine H3 receptor.

LH1753 是一种口服活性的 L-胱氨酸结晶抑制剂，EC50 为 29.5 nM，并可用于研究半胱氨酸尿症。

Rosopatamab MMAE(罗索帕妥单抗 MMAE,HUJ-591 MMAE)是一种ADC，由PSMA定向抗体（人源化抗PSMA 的IgG1 单克隆抗体）和抗有丝分裂的细胞毒素MMAE组成，用于前列腺癌的研究。

BAY-298 是一种口服有效且选择性的促黄体生成激素受体(LH-R)拮抗剂，分别针对hLH(人LH)、rLH(大鼠LH)和cLH(食蟹猴LH)展现出96 nM、23 nM和78 nM的IC50。作为一种纳摩尔级别的hLH-R拮抗剂，BAY-298 能够有效降低体内性激素水平。

BAY-899 is an orally active and selective antagonist of the luteinizing hormone receptor (LH-R), exhibiting IC50 values of 185 nM and 46 nM for human LH (hLH) and rat LH (rLH) respectively. In vivo studies have demonstrated that BAY-899 effectively reduces sex hormone levels[1].

LH-21 是一种有效的体内中性大麻素 CB1受体拮抗剂。LH-21 会导致剂量依赖性进食抑制，减少肥胖 Zucker 大鼠的食物摄入和体重增加。

Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004). Kisspeptin-54 is a peptide ligand of the orphan G protein-coupled receptor GPR54 (Kis = 1.81 and 1.45 nM for rat and human receptors, respectively).1 It is a 54 amino acid peptide encoded by the metastasis suppressor gene KISS-1. Kisspeptin-54 induces calcium mobilization in CHO-K1 cells expressing rat and human receptors (EC50s = 1.39 and 5.47 nM, respectively). It also induces arachidonic acid release in CHO cells expressing rat and human GPR54 in a concentration-dependent manner. Kisspeptin-54 (10-1,000 nM) inhibits insulin secretion from isolated mouse pancreatic β-cells in the presence of 2.8 mM, but not 11.1 mM, glucose.2 Kisspeptin-54 (1-5 nmol, i.c.v.) increases serum levels of luteinizing hormone (LH) and follicular stimulating hormone (FSH) in mice, an effect which is reversed by the gonadotropin releasing hormone (GNRH) antagonist acycline.3 References1. Kotani, M., Detheux, M., Vandenbogaerde, A.L., et al. The metastasis suppressor gene KiSS-1 encodes kisspeptins, the natural ligands of the orphan G protein-coupled receptor GPR54. J. Biol. Chem. 276(37), 34631-34636 (2001).2. Vikman, J., and Ahrén, B. Inhibitory effect of kisspeptins on insulin secretion from isolated mouse islets. Diabetes Obes. Metab. 11(Suppl 4), 197-201 (2009).3. Gottsch, M.L., Cunningham, M.J., Smith, J.T., et al. A role for kisspeptins in the regulation of gonadotropin secretion in the mouse. Endocrinology 145(9), 4073-4077 (2004).

DCVC inhibits pathogen-stimulated TNF-α in human extra placental membranes in vitro.Target: TNF-αin vitro: DCVC inhibits pathogen stimulated cytokine release from tissue punch cultures. DCVC (5-50 μM) significantly inhibits LTA-, LPS-, and GBS-stimulated cytokine release from tissue cultures as early as 4 h (P ≤ 0.05). In contrast, TCA (up to 500 μM) does not inhibit LTA-stimulated cytokine release from tissue punches. DCVC effects on LTA-stimulated and LPS-stimulated TNF-α release from tissue punch cultures of extraplacental membranes. DCVC effects on GBS-stimulated release of pro-inflammatory cytokines from extraplacental membranes in transwell cultures. [1]. Boldenow E, et al. The trichloroethylene metabolite S-(1,2-dichlorovinyl)-l-cysteine but not trichloroacetate inhibits pathogen-stimulated TNF-α in human extraplacental membranes in vitro. Reprod Toxicol. 2015 Apr;52:1-6. [2]. Lash LH, et al. Multigenerational study of chemically induced cytotoxicity and proliferation in cultures of human proximal tubular cells. Int J Mol Sci. 2014 Nov 18;15(11):21348-65. [3]. Yoo HS, et al. Comparative analysis of the relationship between trichloroethylene metabolism and tissue-specific toxicity among inbred mouse strains: kidney effects. J Toxicol Environ Health A. 2015;78(1):32-49.

LUF5771 is a highly potent allosteric inhibitor of recombinant luteinizing hormone (recLH) and Org 43553. It exhibits partial activation of the LH receptor with low efficacy [1].

GnRH-R antagonist 1 (化合物 21a) 是GnRH-R拮抗剂，具有优良口服安全性及膜透性，高亲和力结合GnRH-R（IC50=0.57 nM），并展现出有效体外拮抗活性（IC50=2.18 nM）。该化合物适用于晚期前列腺癌治疗和预防过早LH峰出现的研究。

Ganirelix为一种竞争性且选择性的促性腺激素释放激素(GnRH)拮抗剂，其主要作用机制为抑制内源性GnRH，从而抑制黄体生成素(LH)及促卵泡激素的释放。

Spexin TFA, a potent agonist for galanin receptor 2 3 (GAL2 GAL3) with EC50 values of 45.7 and 112.2 nM respectively, shows no significant activity towards galanin receptor 1. As an endogenous peptide promoting satiety, it reduces long chain fatty acid uptake by adipocytes and lowers food consumption in diet-induced obese mice and rats. Additionally, it moderates LH secretion in goldfish and demonstrates anxiolytic effects in vivo.