m 130

PQM130是一种魏罗酮-多奈哌齐杂化化合物，能透过大脑。PQM130是多靶点的候选药物，可用于Aβ1-42低聚物引起的神经毒性，还具有抗炎活性。它是具有神经保护作用的、有潜力的抗 AD 药物。

UCM-1306 是具有口服活性的人多巴胺 D1 受体变构调节剂 (PAM)。UCM-1306 增加结合在人和小鼠 D1 受体的内源性多巴胺 (DA) 效应。UCM-1306可以改善运动症状，解决与长期帕金森病(PD) 相关的关键共病认知障碍。

SM-130,686 is a potent, orally-active agonist of the ghrelin growth hormone secretagogue receptor (GHSR) and growth hormone secretagogue. It has around half the potency of the endogenous agonist ghrelin as a stimulator of growth hormone release.

ORM-13070 is a selective antagonist radioligand for the α2C adrenoceptor subtype. ORM-13070 C-11 is under investigation in clinical trial.

ARQ 736 is a potent and selective BRAF inhibitor. ARQ 736 is selectively potent in killing cancer cell lines harboring at least one mutated BRAF allele. BRAF mutations were detected in over 60% of melanomas and may account for a significant proportion of colon cancer patients whose tumors are resistant to anti-EGFR therapy. The B-Raf protein is a key signaling molecule in the mitogen activated protein kinase (MAPK) signaling pathway and has been implicated in the pathogenesis of a variety of cancers.

S-Nitrosothiols (RSNOs) are a class of molecules that function as exogenous and endogenous nitric oxide (NO) donors. RSNOs found in vivo include proteins such as S-nitrosohemoglobin and S-nitrosoalbumin, as well as low molecular weight species such as S-nitrosoglutathione (GSNO) and S-nitrosocysteine (CysNO). CAY10565 is a member of a new class of S-nitrosothiol species that act as NO donors under acidic conditions. It decomposes with a half-life of 130 minutes in 0.1 M phosphate buffer, pH 5.0, at 37°C and relaxes phenylephrine-constricted rat aortic strips 71% and 44% at pH 6.0 and 7.4, respectively.

Epitalon is a synthetic tetrapeptide with anti-aging properties.1,2,3,4 Dietary administration of epitalon (0.00001% w w) reduces levels of lipid peroxidation products in aged D. melanogaster tissue homogenates.1 Epitalon (1 μg animal) delays age-related estrous shutdown and decreases the frequency of bone marrow cell chromosomal aberrations in female mice.2 It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice.3 Epitalon also stimulates melatonin synthesis and normalizes the circadian rhythm of cortisol secretion in senescent female M. mulatta monkeys.4References1. Khavinson, V.K., and Myl'nikov, S.V. Effect of epithalone on the age-specific changes in the time course of lipid peroxidation in Drosophila melanogaster. Bull. Exp. Biol. Med. 130(11), 1116-1119 (2000).2. Anisimov, V.N., Khavinson, V.K., Popovich, I.G., et al. Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice. Biogerontology 4(4), 193-202 (2003).3. Kossoy, G., Anisimov, V.N., Ben-Hur, H., et al. Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H He mice. In Vivo 20(2), 253-257 (2006).4. Khavinson, V., Goncharova, N., and Lapin, B. Synthetic tetrapeptide epitalon restores disturbed neuroendocrine regulation in senescent monkeys. Neuro. Endocrinol. Lett. 22(4), 251-254 (2001). Epitalon is a synthetic tetrapeptide with anti-aging properties.1,2,3,4 Dietary administration of epitalon (0.00001% w w) reduces levels of lipid peroxidation products in aged D. melanogaster tissue homogenates.1 Epitalon (1 μg animal) delays age-related estrous shutdown and decreases the frequency of bone marrow cell chromosomal aberrations in female mice.2 It decreases spontaneous mammary gland and ovarian tumor development and metastasis in aged female mice.3 Epitalon also stimulates melatonin synthesis and normalizes the circadian rhythm of cortisol secretion in senescent female M. mulatta monkeys.4 References1. Khavinson, V.K., and Myl'nikov, S.V. Effect of epithalone on the age-specific changes in the time course of lipid peroxidation in Drosophila melanogaster. Bull. Exp. Biol. Med. 130(11), 1116-1119 (2000).2. Anisimov, V.N., Khavinson, V.K., Popovich, I.G., et al. Effect of Epitalon on biomarkers of aging, life span and spontaneous tumor incidence in female Swiss-derived SHR mice. Biogerontology 4(4), 193-202 (2003).3. Kossoy, G., Anisimov, V.N., Ben-Hur, H., et al. Effect of the synthetic pineal peptide epitalon on spontaneous carcinogenesis in female C3H He mice. In Vivo 20(2), 253-257 (2006).4. Khavinson, V., Goncharova, N., and Lapin, B. Synthetic tetrapeptide epitalon restores disturbed neuroendocrine regulation in senescent monkeys. Neuro. Endocrinol. Lett. 22(4), 251-254 (2001).

OH-Chol is a cationic cholesterol derivative.1 OH-Chol, as a component of lipoplexes with DOPE , has been used for siRNA delivery and gene silencing in MCF-7 cells, as well as in mice via intravenous injection, resulting in lipoplex accumulation in the liver. It has also been used in cationic nanoparticles in combination with Tween 80 to transfect pDNA and siRNA into PC3 mouse xenografts via intratumoral injection and with Tween 80 and folate-PEG2000-DSPE in a KB mouse xenograft model for intratumoral gene delivery.2References1. Hattori, Y., Nakamura, M., Takeuchi, N., et al. Effect of cationic lipid in cationic liposomes on siRNA delivery into the lung by intravenous injection of cationic lipoplex. J. Drug. Target 27(2), 217-227 (2019).2. Hattori, Y. Development of non-viral vector for cancer gene therapy. Yakugaku Zasshi 130(7), 917-923 (2010). OH-Chol is a cationic cholesterol derivative.1 OH-Chol, as a component of lipoplexes with DOPE , has been used for siRNA delivery and gene silencing in MCF-7 cells, as well as in mice via intravenous injection, resulting in lipoplex accumulation in the liver. It has also been used in cationic nanoparticles in combination with Tween 80 to transfect pDNA and siRNA into PC3 mouse xenografts via intratumoral injection and with Tween 80 and folate-PEG2000-DSPE in a KB mouse xenograft model for intratumoral gene delivery.2 References1. Hattori, Y., Nakamura, M., Takeuchi, N., et al. Effect of cationic lipid in cationic liposomes on siRNA delivery into the lung by intravenous injection of cationic lipoplex. J. Drug. Target 27(2), 217-227 (2019).2. Hattori, Y. Development of non-viral vector for cancer gene therapy. Yakugaku Zasshi 130(7), 917-923 (2010).