distribution

4-Hydroxyantipyrine 是在氨基比林的氧化脱氨过程中形成的。

UK-101 是一种强效且具有选择性的免疫蛋白酶体 LMP2 的抑制剂 ，对 β1i (LMP2) 、 β1c (LMP2) 和 β5 (LMP2) 具有抑制作用，IC50 为 104nM 、15 μM 和 1 μM 。UK-101 对 β1i 的亲和力比β1c 和 β5 亚基分布高的 144 倍和 10 倍。UK-101 可诱导细胞凋亡且可用于研究前列腺癌的相关疾病。

Theophylline monohydrate (Quibron) 似乎抑制磷酸二酯酶和前列腺素的产生，调节钙通量和细胞内钙分布，并拮抗腺苷。茶碱是黄嘌呤的天然生物碱衍生物，从植物山茶花和小粒咖啡中分离出来。在生理上，该药剂可放松支气管平滑肌，产生血管舒张（脑血管除外），刺激中枢神经系统，刺激心肌，利尿，增加胃酸分泌；它还可以抑制炎症并改善横膈膜的收缩性。

7-Methoxy-1-naphthaleneacetic acid 是植物生长素作用的抑制剂。 7-Methoxy-1-naphthaleneacetic acid 抑制与拟南芥和玉米中生长素不对称分布相关的极性生长素转运和热带反应。 7-Methoxy-1-naphthaleneacetic acid 抑制由酵母中表达的 AUX1、PIN 和 ABCB 蛋白介导的生长素转运。

Inosinic acid (IMP) 是内源性代谢产物。

Recilisib, also known as ON 01210.Na, is a radioprotectant, which modifys cell cycle distribution patterns in cancer cells subjected to radiation therapy, and it has been identified as a potential candidate for radiation protection studies. It appears tha

MK-8245 trifluoroacetate is a liver-targeting inhibitor of stearoyl-CoA desaturase (SCD) with IC50 of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with anti-diabetic and anti-dyslipidemic efficacy. IC50 value: 1 nM (hSCD1) Target: SCD1 in vitro: MK-8245, a phenoxy piperidine isoxazole derivative, has been identified as a potent and liver-specific SCD inhibitor. It contains a tetrazole acetic acid moiety, which is the key molecule for OATPs recognition and liver-targeting. MK-8245 displays similar potencies against human, rat and mouse SCD1 with IC50 values of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1. MK-8245 exhibits a significant SCD inhibition in the rat hepatocyte assay which contains functional, active OATPs with IC50 of 68 nM, while being only weakly active in the HepG2 cell assay which is devoid of active OATPs with IC50 of ~1 μM. MK-8245 displays highly selective activity for the Δ-5 and Δ-6 desaturases (i.e., >100000 μM vs rat and human Δ5D and Δ6D as assessed in the HepG assay. in vivo: Administration of MK-8245 at 10 mg kg in mice exhibits a tissue distribution profile concentrated in the liver. It shows a liver-to-Harderian gland ratio of 21, suggesting a high degree of liver-targeting compared to a systemically distributed compound with liver-to-Harderian gland ratio of 1.5. Oral dosing of MK-8245 in mice, rats, dogs, and rhesus monkeys demonstrates that MK-8245 is distributed mainly to the liver, with low exposure in tissues associated with potential adverse events. The liver-to-skin ratios are >30:1 in all four species. Administration of MK-8245 to eDIO mice before the glucose challenge improves glucose clearance in a dose-dependent manner with ED50 of 7 mg kg.

OPC-167832 is a potent and orally active dprE1 Inhibitor with an IC50 of 0.258 μM. OPC-167832 has antituberculosis activity and can be used for the research of tuberculosis caused by Mycobacterium tuberculosis[1]. OPC-167832 exhibits very low MICs against laboratory strains of M. tuberculosis H37Rv (MIC: 0.0005 μg ml) and Kurono (MIC: 0.0005 μg ml) and strains with monoresistance to rifampin (RIF), isoniazid (INH), ethambutol (EMB), streptomycin (STR), and pyrazinamide (PZA) (MIC: 0.00024-0.001 μg ml). However, OPC-167832 has minimal or no activity against standard strains of nonmycobacterial aerobic and anaerobic bacteria[1].The IC90 values of OPC-167832 against intracellular M. tuberculosis strains H37Rv and Kurono are 0.0048 and 0.0027 μg ml, respectively. OPC-167832 shows bactericidal activity against intracellular M. tuberculosis at a low concentration, and the bactericidal activity is saturated at concentrations of 0.004 μg ml or higher[1]. OPC-167832 (oral administration; 0.625-10 mg kg) exhibits a good pharmacokinetic characteristic. The plasma reaches peak at 0.5 h to 1.0 h (tmax) and is eliminated with a half-life (t1 2) of 1.3 h to 2.1 h OPC-167832 distribution in the lungs is approximately 2 times higher than that in plasma, and the Cmax and AUCt of OPC-167832 in plasma and the lungs shows dose dependency[1].OPC-167832 (oral administration; 0.625-10 mg kg; 4 weeks) significantly reduces lung CFU compared to the vehicle group. The dose-dependent decrease of lung CFU is observed from 0.625 mg kg to 2.5 mg kg. In a M. tuberculosis Kurono-infected ICR female mice model. OPC-167832 combines with DMD, BDQ, or LVX via oral gavage exhibits significantly higher efficacies than each single agent alone[1].[1].OPC-167832 (oral gavage; 2.5 mg kg; combination with DCMB; 12 weeks) demonstrates the most potent efficacy when compares with DC, DCB. The lung CFU count after 6 weeks of treatment is below the detection limit, and at the end of just 8 weeks of treatment, the bacteria in the lungs of all the evaluated mice had already been eradicate[1]. [1]. Norimitsu Hariguchi, et al. OPC-167832, a Novel Carbostyril Derivative with Potent Antituberculosis Activity as a DprE1 Inhibitor.Antimicrob Agents Chemother. 2020 May 21;64(6):e02020-19.

Resolvin D3 methyl ester is a methyl ester version of the free acid that may act as a lipophilic prodrug form that will alter its distribution and pharmacokinetic properties. The methyl ester moiety is susceptible to cleavage by intracellular esterases, leaving the free acid.

Heteroatom-substituted fatty acids have been observed to modulate the extension and desaturating of fatty acids, and to influence their distribution within phospholipids pools. 10-Thiastearic acid inhibits desaturation of radiolabeled stearate to oleate in rat hepatocytes and hepatoma cells by more than 80% at a concentration of 25 μM. This activity is associated with a hypolipidemic effect, making this 10-thiastearic acid a useful tool for evaluating new anti-obesity therapeutics.

Advanced glycation end products (AGEs) are compounds formed by non-enzymatic chemical reactions following the bonding of sugars to proteins or lipids during diabetes, uremia, aging, rheumatic arthritis, and other conditions. A receptor for the AGEs (RAGE) binds certain members of this class to initiate cell signaling.[1][2] Pentosidine is a well-characterized natural AGE that is often used as a biomarker for the production of all AGEs. While pentosidine can be measured in urine, the majority of this AGE is catabolized before excretion.[3] Reference：[1]. Neeper, M., Schmidt, A.M., Brett, J., et al. Cloning and expression of a cell surface receptor for advanced glycosylation end products of proteins. The Journal of Biological Chemisty 267(21), 14998-15004 (1992).[2]. Brett, J., Schmidt, A.M., Yan, S.D., et al. Survey of the distribution of a newly characterized receptor for advanced glycation end products in tissues. American Journal of Pathology 143(6), 1699-1712 (1993).[3]. Miyata, T., Ueda, Y., Horie, K., et al. Renal catabolism of advanced glycation end products: The fate of pentosidine. Kidney International 53, 416-422 (1998).

'(Met(O)35)-Amyloid β-Protein (1-42)，Aβ42的一种氧化形态，位于Met35。该化合物可形成与Aβ40具有相似大小和分布特征的寡聚体，适用于阿尔茨海默病（AD）研究。'

CEDAEVFKDSMVPGEK 为大鼠辣椒素受体亚型 1 (VR1) 的多肽序列片段，适用于探测 VR1 的存在、分布及分子形态。

Pinoresinol ((+)-Pinoresinol) 是一种植物来源的木质素，具有抗炎、保肝和杀真菌活性。它导致 CDK 抑制剂 p21(WAF1 Cip1) 在 mRNA 和蛋白质水平上调，抑制 NF-kappaB 和激活蛋白 1 。

Clinodiside A 是来自中草药Clinopodium chinensis 中。

1-Palmitoyl-2-cholesterylcarbonoyl-sn-glycero-3-phosphocholine是一种甾醇修饰磷脂，能够稳定膜双层结构并提升脂质体介导的化合物传递活性。它广泛应用于生物医学领域，以提高化合物的传递效率，同时改善化合物在细胞内的释放和分布。

GR65630是一种高效且具有选择性的5-羟色胺（5-HT）3型受体拮抗剂。该化合物常用于研究5-HT3受体在多个脑区的分布及其在中枢神经系统的潜在功能。通过使用GR65630及其同位素标记的[3H]GR65630，研究人员能够探索受体的分布情况、密度和亲和性。

1-1(Z)-Octadecenyl-2-docosahexaenoyl-sn-glycero-3-PE (18:0p 22:6-PE) 为一种通过质谱成像技术在大鼠脑组织中确认的独特结构脂质，此方法可准确识别其不同脂肪酸链的异构体及其分布。

Stilbamidine dihydrochloride is a blocker of neuromuscular transmission and axonal conduction used to study the distribution of the drug in the organs and tissues of rats following intravenous injection.

Taribavirin is an orally active inosine monophosphate dehydrogenase inhibitor. Taribavirin is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of he

CAY10704 is a potent inhibitor of hepatitis C virus (HCV) infection (EC50 = 17 nM) that displays low cytotoxicity of virally-infected human hepatoma Huh7.5.1 cells (CC50 = 21.3 μM). It displays good pharmacokinetics in mice when delivered intraperitoneally, with preferential liver distribution without significant hepatotoxicity. CAY10704 is selective for HCV over dengue virus (EC50 = 4.62 μM).

DMHAPC-Chol is a cationic cholesterol. Liposomes containing DMHAPC-chol have been used for DNA plasmid delivery in vitro and in vivo in a B16-F10 mouse xenograft model. Liposomes containing DMHAPC-chol are cytotoxic to B16-F10 cells when used at lipid concentrations greater than 20 μM. DMHAPC-Chol, as part of a lipoplex with DOPE , has also been used to deliver DNA into mouse lung via intratracheal injection, resulting in a heterogeneous distribution in the bronchi and bronchioles, and to deliver VEGF siRNA into A431 and MDA-MB-231 cells, which secrete VEGF.

Sphingomyelins (SMs) are bioactive sphingolipids found in mammalian cell membranes.1SMs make up 2-15% of the total organ phospholipid population but are found at higher concentrations in the brain and myelin sheaths surrounding peripheral nerves. They interact with cholesterol to control its distribution within cellular membranes and maintain cholesterol homeostasis in cells. SMs undergo hydrolysis by sphingomyelinase to form ceramides, which are sphingolipid mediators of intracellular signaling.2This product is a mixture of SMs, with variable fatty acyl chain lengths, isolated from buttermilk. [Matreya, LLC. Catalog No. 1329] 1.Slotte, J.P., and Ramstedt, B.The functional role of sphingomyelin in cell membranesEur. J. Lipid Sci. Technol.109(10)977-981(2007) 2.Shayman, J.A.SphingolipidsKidney Int.58(1)11-26(2000)

Anguizole, a small molecule, effectively inhibits Hepatitis C Virus (HCV) replication by modifying the subcellular distribution of NS4B. It demonstrates its potency with an IC50 value, highlighting its specific target action against HCV.