turnover

Alendronic Acid (alendronate) 是法呢基二磷酸合酶(FDPS)抑制剂，是一种双膦酸盐。它能够抑制破骨细胞介导的骨吸收，对绝经后骨质疏松症，恶性高钙血症和 Paget 病具有疗效。

β-Gentiobiose 是一种能够促进果实成熟天的然寡糖。

Balicatib (AAE581) 是组织蛋白酶K 抑制剂，其对组织蛋白酶K 的抑制作用是组织蛋白酶B、L 和S 的抑制性的10到100倍。

L-692429 (MK-0751) 是一种有效的非肽基生长激素促分泌素 (GHS) 激动剂，是一种苯并内酰胺的衍生物，可逆转糖皮质激素对 GH 分泌的抑制。L-692429 对 G 蛋白偶联受体 (G protein-coupled receptor)具有很高的亲和力，可用于研究肢端肥大症和肥胖。

Etidronic acid (HEDP) 是一种影响钙代谢的二膦酸盐，抑制异位钙化并减缓骨吸收和骨转换，可应用于洗涤，水处理，化妆品和制药业。

Pentabromophenol (NSC-5717) 通过加速 TGF-β 受体的转换率来抑制 TGF-β 反应。

Cholestenone 是胆固醇的中间氧化产物，主要在肝脏中代谢。它能够会导致细胞长期功能缺陷。它在膜中具有很高的流动性，会影响胆固醇的翻转和外排。

β-Anhydroicaritin 是从乳香提取的一种天然产物，具有重要的生物学和药理学作用，如抗骨质疏松症，雌激素调节和抗肿瘤特性。它改善牙周组织的降解，抑制糖尿病大鼠 TNF-α 和 MMP-3 的合成和分泌。它抑制细胞内 Ca2+的升高，并显著降低 iNOS 蛋白的表达。

KM02894 是一种谷氨酸释放抑制剂。癌细胞释放高水平的谷氨酸，能够破坏正常的骨转换，这可能导致癌症引起的骨痛。KM02894 可用于研究肿瘤相关疾病。

CLP257 是有效的 K+-Cl- 协同转运蛋白 KCC2 选择性激活剂 (EC50: 616 nM)。它可减轻神经性疼痛大鼠的超敏反应，并在翻译后调节质膜 KCC2 蛋白周转。它在 KCC2 活性降低的神经元中恢复受损的 Cl- 转运。

RGH-5526是一种新型的抗高血压药。它引起下丘脑去甲肾上腺素（NA）周转（利用）增加，下丘脑去甲肾上腺素能神经元活性的增加可能导致外周交感神经活性的降低，从而显著降低血压。

Lactacystin是一种天然的非肽类蛋白酶体抑制剂和高特异性的抗癌药物，控制细胞蛋白周转的UPS并抑制碱性细胞增殖，能够作为研究痴呆症的模型，诱导神经突生长和cAMP水平短暂升高，抑制血管生成，引发胶质瘤细胞凋亡，能穿透血脑屏障（BBB）。

Sulbactam (CP45899) 是一种竞争性、不可逆的 β-内酰胺酶抑制剂，抑制耐多药不动杆菌-鲍曼不动杆菌复合物。它具有抗菌活性。

PF-06273340 是一种口服具有活力的、具有选择性的外周限制性Trk 泛抑制剂。

Dehydroindapamide是Indapamide的一种吲哚化合物，主要用于定量分析Indapamide在CYP3A4中的代谢速率。该化合物的代谢速率比Indoline高出约10倍，并且对CYP3A4的亲和力略有提高。

L-654284为一种α2-肾上腺素受体拮抗剂，展现出较高的选择性。该化合物在体外实验中与3H-clonidine及3H-rauwolscine的结合发生竞争，展示Ki值分别为0.8 nM和1.1 nM。在体内实验中，L-654284能显著提升大鼠脑皮层中的去甲肾上腺素周转率，表明其在中枢神经系统中对α2-肾上腺素受体具有阻断作用。此外，L-654284还能阻断克隆尼定在大鼠孤立输精管中的作用，其pA2值达到9.1。在α2与α1肾上腺素受体的选择性上，L-654284对3H-prazosin的结合抑制表现出Ki值为110 nM。

BNN27 是 TrkA 受体 (TrkA receptor) 和 p75NTR 受体 (p75NTR receptor) 的激动剂，具备神经营养和抗凋亡特性。该化合物能够提升大鼠海马和前额叶皮质中的谷氨酸、GABA 和谷氨酰胺水平，同时改善谷氨酸的代谢。在小鼠肌萎缩侧索硬化症 (ALS) 模型中，BNN27 展示了神经保护效果；在实验性自身免疫性脑脊髓炎 (EAE) 模型中显示出抗炎能力，并在大鼠糖尿病模型中具有视网膜保护功能。此外，BNN27 还能透过血脑屏障。

Glycitin (Glycitein 7-O-β-glucoside) 是一种从豆类中分离出来的天然异黄酮，有抗菌，抗病毒和雌激素作用，还有促进骨髓基质细胞和成骨细胞的增殖和抑制骨转换的生物学功能。

Glucosylgalactosylhydroxylysine is a bone formation and bone resorption marker that is related to bone turnover processes during growth and development as well as metabolic bone diseases.

Ganglioside GQ1b is a tetrasialoganglioside that contains two sialic acid residues linked to an inner galactose unit. It stimulates phosphorylation of several ecto-type protein kinase substrates on the surface of GOTO human neuroblastoma cells when used at a concentration of 5 nM. Ganglioside GQ1b promotes differentiation of murine embryonic stem cells (mESCs) to neuronal precursor and glial cells via activation of the ERK1/2 pathway. It also induces differentiation of murine keratinocytes through phosphoinositide turnover. Ganglioside GQ1b mixture contains ganglioside GQ1b molecular species with C18:1 and C20:1 sphingoid backbones.

Osteocalcin (1-49) is a non-collagenous peptide that is secreted by osteoblasts and odontoblasts and comprises 1-2% of the total protein in bone. Secretion of osteocalcin (1-49) is stimulated by 1,25-dihydroxy vitamin D and plasma levels increase in diseases that induce dysregulated bone turnover such as osteoporosis, Paget's disease, and primary hyperparathyroidism. Osteocalcin (1-49) is positively correlated with insulin sensitivity and negatively correlated with high blood glucose levels in women. In vitro, osteocalcin induces chemotaxis of MDA-MB-231 breast cancer cells, human peripheral blood monocytes, and rat osteosarcoma cells with osteoblast-like characteristics. It is also expressed by vascular smooth muscle cells (VSMCs) displaying an osteoblast-like phenotype and has been positively associated with calcification of aortic tissue and heart valves in humans.

Inactivation of the tumor suppressor p53 commonly coincides with increased signaling through NF-κB in cancer. CAY10681 is a dual modulator of p53-MDM2 interaction and NF-κB signaling. It potently binds MDM2 (Ki = 250 nM), reducing MDM2-mediated turnover of p53. CAY10681 also inhibits phosphorylation of IκBα and dose-dependently reduces nuclear accumulation of p65. It blocks the proliferation of cancer cell lines (IC50s range from 33 to 37 μM). CAY10681 exhibits excellent oral bioavailability and inhibits tumor growth in A549 xenografts in nude mice.

5-Ethynyluridine 可用于标记新合成的 RNA。这种方法称为使用点击化学 (RICK) 捕获新转录的 RNA 相互作用组，系统地捕获与多种 RNA 结合的蛋白质，包括新生 RNA 和传统上被忽视的非多腺苷酸化 RNA。

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg kg, respectively). Zonisamide (40 mg kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy. |1. Masuda, Y., Ishizaki, M., and Shimizu, M. Zonisamide: Pharmacology and clinical efficacy in epilepsy. CNS Drug Rev. 4(4), 341-360 (1998).|2. Rock, D.M., Macdonald, R.L., and Taylor, C.P. Blockade of sustained repetitive action potentials in cultured spinal cord neurons by zonisamide (AD 810, CI 912), a novel anticonvulsant. Epilepsy Res. 3(2), 138-143 (1989).|3. Suzuki, S., Kawakami, K., Nishimura, S., et al. Zonisamide blocks T-type calcium channel in cultured neurons of rat cerebral cortex. Epilepsy Res. 12(1), 21-27 (1992).|4. Nishimori, I., Vullo, D., Minakuchi, T., et al. Carbonic anhydrase inhibitors: Cloning and sulfonamide inhibition studies of a carboxyterminal truncated α-carbonic anhydrase from Helicobacter pylori. Bioorg. Med. Chem. Lett. 16(8), 2182-2188 (2006).|5. De Simone, G., Di Fiore, A., Menchise, V., et al. Carbonic anhydrase inhibitors. Zonisamide is an effective inhibitor of the cytosolic isozyme II and mitochondrial isozyme V: Solution and X-ray crystallographic studies. Bioorg. Med. Chem. Lett. 15(9), 2315-2320 (2005).|6. Yabe, H., Choudhury, M.E., Kubo, M., et al. Zonisamide increases dopamine turnover in the striatum of mice and common marmosets treated with MPTP. J. Pharmacol. Sci. 110(1), 64-68 (2009).