water solubility

Alginic acid (Snow acid algin G) is a natural polysaccharide extracted from brown seaweeds with anti-anaphylactic and anti-inflammatory activities. Alginic acid inhibits histamine release and can be used in the food industry.

Octanoic acid (Caprylic acid), found naturally in coconuts and breast milk, is an oily liquid with a slightly unpleasant rancid taste and minimal solubility in water. It is commercially utilized in the production of esters for perfumery and in dye manufacturing.

Hydroxypropyl cellulose (HPC) is a derivative of cellulose with both water solubility and organic solubility, it is used as food additive and sieving matrix for DNA separations.

4-[(2,4-dioxo-1,3-thiazolidin-5-ylidene)methyl]benzoic acid is a synthetic compound with potent antitumor activity, high efficiency and selectivity against tumor cells. However, it has poor solubility in water and is potentially toxic at high concentrations.

Biotin-PEG3-acid is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs. This heterobiofunctional biotin PEG derivative contains a carboxylic acid group. The hydrophilic PEG spacer arm imparts water solubility to the biotinylated molecule. [PEG Linkers] may be useful in the development of antibody-drug conjugates and drug delivery methods.

8pyDTZ is a pyridyl diphenylterazine (DTZ) analog and an ATP-independent pyridyl substrate of LumiLuc luciferase, exhibiting spectrally shifted emission and improved water solubility, suitable for in vivo luminescence imaging.

SUN-597 is a selective inhibitor targeting GSK-3α and β isoforms, showcasing inhibition constants (Ki) of 0.3 nM and 0.05 nM, respectively. It disrupts the proliferation pathways of cells, particularly impacting cellular mechanisms implicated in neurodegenerative diseases and various forms of cancer. While demonstrating efficacy in both in vivo and in vitro studies, SUN-597 has limited water solubility, which poses challenges regarding its formulation and administration.

HJ445A is a highly efficient and selective MYOF inhibitor with excellent water solubility, utilized for the treatment of gastric cancer. In gastric cancer cells MGC803 and MKN45, HJ445A exhibits significant antiproliferative properties with IC50 values of 0.16 μM and 0.14 μM, respectively. The compound binds to the MYOF-C2D domain with a KD value of 0.17 μM and hinders the migration of gastric cancer cells by reversing the epithelial-mesenchymal transition (EMT) process. It also inhibits colony formation in MKN45 cells in a concentration-dependent manner. Remarkably, compared to compound 6y, HJ445A's water solubility is improved by approximately 170 times. Moreover, HJ445A demonstrates superior antitumor effects in vivo.

(S, R, S)-AHPC-PEG8-acid is a synthetic PROTAC linker that binds an E3 ligase ligand with a PEG8 linker to facilitate PROTAC drug development. The PEG8 component enhances the compound's water solubility, and the acid group reacts with amine-containing molecules.

Fenretinide glucuronide is a metabolite formed through the glucuronidation of Fenretinide. This process enhances the water solubility of Fenretinide and facilitates its excretion. Fenretinide glucuronide shows potential for research in the field of cancer.

(S,R,S)-AHPC-PEG2-NHS ester is a synthetic PROTAC linker that combines the E3 ligase ligand with a PEG linker to enhance PROTAC pharmacology. The NHS ester reacts with amine groups, and the hydrophilic PEG spacer increases water solubility.

Thalidomide-5-(PEG2-amine) is a Thalidomide analogue that includes an E3 ligase ligand substituted with a terminal amine group. The amine group can react with NHS esters or carboxylic acids in the presence of EDC or HATU. The PEG spacer enhances water solubility.

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) is a prodrug of paracetamol (acetaminophen) with improved water solubility. Propacetamol Hydrochloride is an analgesic drug delivered by IV when the oral application of NSAID is not appropriate or contradicted.

10-Deacetyl-7-xylosyl paclitaxel (7-Xylosyl-10-deacetyltaxol) is a Paclitaxel derivative with improved pharmacological features and higher water solubility,used in Chinese clinics to treat cancer.

Antitubercular agent-32 is a Benzothiazinone derivative that inhibits Mycobacterium tuberculosis and exhibits good metabolic stability and water solubility. Antitubercular agent-32 can act on decaprenylphosphoryl-β-D-ribose 2'-oxidase (DprE1, IC50: 3.9 μM) and exhibits antitubercular effects.

OY-101, an orally active compound, serves as a potent and specific inhibitor of P-glycoprotein (P-gp). It has the capability to sensitize drug-resistant tumors and counteract tumor multidrug resistance efficiently. Compared to Tetrandrine [1], OY-101 demonstrates enhanced water-solubility, cytotoxicity, and reversal activity.

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.