water solubility

Alginic acid (Snow acid algin G) 是一种从褐海藻中提取的天然多糖，具有抗过敏和抗炎活性。 Alginic acid 抑制组胺释放，可用于食品工业。

Caprylic acid天然存在于椰子和母乳中。它是一种油性液体，带有些许腐臭味，能用于酯类香料和染料的生产。

Hydroxypropyl Cellulose 是纤维素的衍生物，兼具水溶性和有机溶解性，用作食品添加剂和 DNA 分离的筛分基质。

4-[(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]benzoic acid 是一种合成化合物，具有强大的抗肿瘤活性，对肿瘤细胞有高效性和选择性，但其在水中的溶解性差且在高浓度下有潜在毒性。

Biotin-PEG3-acid 是一种属于 PEG 类的、生物素标记的 PROTAC linker，可用于 PROTAC 分子的合成。

8pyDTZ is a pyridyl diphenylterazine (DTZ) analog and an ATP-independent pyridyl substrate of LumiLuc luciferase. 8pyDTZ exhibits spectrally shifted emission and improved water solubility. It can be used for in vivo luminescence imaging.

SUN-597是一种选择性抑制剂，专门针对GSK-3α和β亚型，其抑制常数（Ki）分别为0.3 nM和0.05 nM。它干扰细胞增殖通路，特别影响与神经退行性疾病和多种癌症相关的细胞机制。尽管SUN-597在体内和体外研究中均表现出效力，但其水溶性较低，这在配方和给药方面带来了挑战。

HJ445A是一种高效选择性的MYOF抑制剂，具有良好的水溶性，用于治疗胃癌。在MGC803和MKN45胃癌细胞中，HJ445A具有强大的抗增殖能力，其IC50值分别为0.16 μM和0.14 μM。此外，HJ445A与MYOF-C2D结构域结合，其KD值为0.17 μM，且能够通过逆转上皮-间充质转化(EMT)过程阻止胃癌细胞的迁移，并以浓度依赖的方式抑制MKN45细胞的集落形成。值得注意的是，与化合物6y相比，HJ445A的水溶性得到了显著提高，增强了约170倍。此外，HJ445A在体内也显示出了卓越的抗肿瘤效果。

(S, R, S)-AHPC-PEG8-acid 是一种人工合成的PROTAC连接子，能够将E3连接酶配体与PEG8链结连，共同促进PROTAC药物研发。PEG8 提升了该化合物的水溶性，而酸基则与含胺分子发生反应。

Fenretinideglucuronide 是 Fenretinide 通过葡糖醛酸化代谢产生的代谢产物，其生成提高了 Fenretinide 的水溶性并促进其排泄。Fenretinideglucuronide 在癌症领域的研究中具有潜力。

(S,R,S)-AHPC-PEG2-NHS ester 是一种用于PROTAC药物的合成连接子，该化合物将 E3 连接酶配体与 PEG 接头连接，以改进药物化学特性。NHS ester 能够与胺基发生反应，并且亲水性的 PEG 连接物有助于提升其水溶性。

Thalidomide-5-(PEG2-amine) 是Thalidomide的一种类似物，含有一个E3连接酶配体并在末端带有胺基。此胺基可在EDC或HATU的存在下与NHS酯基或羧酸发生反应。PEG间隔物的加入则提高了其水溶性。

BMS-695735, a benzimidazole inhibitor of insulin-like growth factor-1 receptor, has broad-spectrum antitumor activity in vivo. It was found that BMS-695735 had strong inhibition of CYP3A4, induction of CYP3A4 mediated by PXR transactivation, poor water so

Epothilone F is a derivative or analogue of Epothilone D. Epothilone F is also an active metabolite of Epothilone D. In molecule of Epothilone F, a hydroxymethyl group is on the thiazole ring. Like taxanes, Epothilone F prevents cancer cells from dividing

NBI-30545 is a potent corticotropin-releasing factor-1 antagonist with sufficient lipophilicity and water solubility for the treatment of stress disorders.

para-amino-Blebbistatin is a more water-soluble form of (S)-4'-nitro-blebbistatin , which is a more stable and less phototoxic form of (-)-blebbistatin .1,2,3 (-)-Blebbistatin is a selective cell-permeable inhibitor of non-muscle myosin II ATPases that rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC50s = 0.5-5 μM), while poorly inhibiting smooth muscle myosin (IC50 = 80 μM).2,3,4 Through these effects, it blocks apoptosis-related bleb formation, directed cell migration, and cytokinesis in vertebrate cells. However, prolonged exposure to blue light (450-490 nm) results in degradation of blebbistatin to an inactive product via cytotoxic intermediates, which may be problematic for its use in fluorescent live cell imaging applications.5,6 The addition of a 4'-amino group increases its water solubility, decreases the inherent fluorescence, stabilizes the molecule to circumvent its degradation by prolonged blue light exposure, and decreases its phototoxicity while retaining the in vitro and in vivo activity of blebbistatin.7 para-amino-Blebbistatin has the same stereochemistry as the active (-)-blebbistatin enantiomer. |1. Várkuti, B.H., Képiró, M., Horváth, I.á., et al. A highly soluble, non-phototoxic, non-fluorescent blebbistatin derivative. Sci. Rep. 6:26141, (2016).|2. Straight, A.F., Cheung, A., Limouze, J., et al. Dissecting temporal and spatial control of cytokinesis with a myosin II inhibitor. Science 299(5613), 1743-1747 (2003).|3. Kovács, M., Tóth, J., Hetényi, C., et al. Mechanism of blebbistatin inhibition of myosin II. J. Biol. Chem. 279(34), 35557-35563 (2004).|4. Limouze, J., Straight, A.F., Mitchison, T., et al. Specificity of blebbistatin, an inhibitor of myosin II. J. Muscle Res. Cell Motil. 25(4-5), 337-341 (2004).|5. Kolega, J. Phototoxicity and photoinactivation of blebbistatin in UV and visible light. Biochem. Biophys. Res. Commun. 320(3), 1020-1025 (2004).|6. Sakamoto, T., Limouze, J., Combs, C.A., et al. Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light. Biochemistry 44(2), 584-588 (2005).|7. Verhasselt, S., Roman, B.I., Bracke, M.E., et al. Improved synthesis and comparative analysis of the tool properties of new and existing D-ring modified (S)-blebbistatin analogs. Eur. J. Med. Chem. 136, 85-103 (2017).

Propacetamol Hydrochloride (Propacetamol HCL) 是 paracetamol(acetaminophen) 的前药，具有改善的水溶性。当口服非甾体抗炎药不合适或矛盾时，丙帕西莫是一种静脉给药的镇痛药。

10-Deacetyl-7-xylosyl paclitaxel (7-Xylosyl-10-deacetyltaxol) 是一种紫杉醇衍生物，具有改进的药理特性和更高的水溶性，用于治疗癌症。

Antitubercular agent-32 是Benzothiazinone 衍生物，对结核分枝杆菌 M. tuberculosis 具有抑制作用，并表现出良好的代谢稳定性及水溶性。 Antitubercular agent-32 可以作用于 decaprenylphosphoryl-β-D-ribose 2'-氧化酶 (DprE1,IC50: 3.9 μM)，表现出抗结核效果。

OY-101为口服生效的特异性P-glycoprotein(P-gp)抑制剂。该化合物可增强耐药性肿瘤的敏感性，并有效逆转多药耐药现象。相较于Tetrandrine，OY-101在水溶性、细胞毒性以及逆转活性方面均表现出改进。

Iso-Fludelone is the third-generation epothilone B analogue with potential anti-mitotic and antineoplastic activites. Iso-fludelone binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2 M arrest, and apoptosis. Compared to other generations of epothilones, iso-fludelone exhibits increased stability, water solubility, potency, duration of action, tumor penetration as well as reduced toxicity. In addition, this agent is a not a substrate of the P-glycoprotein (P-gp), a multidrug resistance pump often overexpressed in cancer cells. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

TG11-77 HCl is a novel, Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist. TG11-77 HCl has a Schild KB of 9.7 nM on EP2, a water solubility of 2.5 mM, a brain-to-plasma ratio of 0.4, and a plasma half-life of 2.4 h in mice. TG11-77 HCl are representative second generation EP2 antagonists with improved pharmacodynamic and pharmacokinetic properties.

TG11-77 free base is a novel, Potent, Selective, Water Soluble, Brain-Permeable EP2 Receptor Antagonist. TG11-77 free base has a Schild KB of 9.7 nM on EP2, a water solubility of 2.5 mM, a brain-to-plasma ratio of 0.4, and a plasma half-life of 2.4 h in mice. TG11-77 free base are representative second generation EP2 antagonists with improved pharmacodynamic and pharmacokinetic properties.

KOS-1584 is a second-generation epothilone with potential antineoplastic activity. Epothilone KOS-1584 binds to tubulin and induces microtubule polymerization and stabilizes microtubules against depolymerization, which may result in the inhibition of cell division, the induction of G2 M arrest, and apoptosis. Compared to first-generation epothilones, this agent exhibits greater safety and efficacy with an enhanced pharmaceutical profile, including enhanced water solubility and tumor penetration, and reduced CNS exposure. In addition, epothilone KOS-1584 is a poor substrate for the P-glycoprotein (P-gp) drug efflux pump.