acid values

Sodium Tartrate is a pH regulator with antioxidant activity that is effective in delaying hydrolysis during high temperature heating and increasing the acidity of vegetable oils.

Aspirin is an orally active, selective, and irreversible inhibitor of COX-1 and COX-2 with IC₅₀ values of 5 and 210 μg/mL, respectively. It induces apoptosis, inhibits NF-κB activation and platelet prostaglandin synthesis, thereby preventing thrombosis. Additionally, it acts as a histone deacetylase inhibitor that upregulates p21, exhibiting anti-inflammatory, antipyretic, analgesic, and anti-platelet aggregation activities. Aspirin is commonly used to induce gastric ulcer models.

AMI-1 free acid is a potent, cell-permeable, and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with inhibitory concentration 50 (IC50) values of 8.8 μM for human PRMT1 and 3.0 μM for yeast-Hmt1p. It achieves its PRMTs inhibitory activity by obstructing peptide-substrate binding [1].

Sodium dichloroacetate (BCA) , a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.

Pemetrexed disodium heptahydrate (LY231514) is an antifolate that inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinyl-adenosine 5'-monophosphate (GARMT) with K_i values of 1.3 nM, 7.2 nM, and 65 nM respectively. This inhibits the formation of precursor purine and pyrimidine nucleotides and cancer cell proliferation, making it suitable for research into pleural mesothelioma and non-small cell lung cancer (NSCLC).

Atraric acid derivatives as a new chemical lead structure for novel therapeutic compounds as AR antagonists, that can be used for prophylaxis or treatment of prostatic diseases. It inhibits PTP1B activity in a dose-dependent manner with IC50 values of 51.5 uM, suggest that atraric acid has potential to treat diabetes.

AGN 205327 is a potent synthetic agonist of retinoic acid receptors (RARs), with EC50 values of 3766 nM for RARα, 734 nM for RARβ, and 32 nM for RARγ, and AGN 205327 demonstrates no inhibitory activity against retinoid X receptors (RXRs), thereby exhibiting selective receptor subtype targeting that makes AGN 205327 an important tool for probing retinoid signaling pathways and investigating therapeutic applications of RAR activation.

1-Linoleoyl Glycerol (Monolinolein) is fatty acid glycerol that has been isolated from Saururus Chinensis roots. The (R)-1-Linoleoyl Glycerol and (S)-1-Linoleoyl Glycerol exhibit Lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitory activities with IC50 values of 45.0 and 52.0 μM, respectively.

AM095 (free acid) is a potent LPA1 receptor antagonist with IC50 values of 0.98 μM for recombinant human LPA1 and 0.73 μM for recombinant mouse LPA1.

Avibactam (NXL-104) free acid is a covalent, reversible inhibitor of non-β-lactam β-lactamase, with IC50 values of 8 nM for β-lactamase TEM-1 and 5 nM for CTX-M-15.

FAAH-IN-1 is a fatty acid amide hydrolase (FAAH) inhibitor with IC50 values of 145 nM for rat FAAH and 650 nM for human FAAH.

Ganoderic acid F exhibits antitumor and antimetastatic activities through inhibition of angiogenesis and alteration of proteins involving cell proliferation and/or cell death, carcinogenesis, oxidative stress, calcium signaling, and endoplasmic reticulum

Ganoderic acid TR is a broad-spectrum inhibitor of influenza neuraminidases (NAs), particularly H1N1 and H5N1 neuraminidases, with IC50 values of 4.6 and 10.9 μM, respectively.

LtaS-IN-1 is an effective inhibitor of Lipoteichoic acid synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 is against Enterococcus spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 inhibits strain E1630 and E1590 with MIC values of 0.5 μg/mL.

PDGFRα kinase inhibitor 1 is a highly selective inhibitor of type II PDGFRα kinase (PDGFRα and PDGFRβ) with IC50 values of 132 nM and 6115 nM, respectively.

Perhexiline maleate is an orally active inhibitor of CPT1 and CPT2, reducing fatty acid metabolism, with IC50 values of 77 μM and 148 μM against rat heart and liver CPT1, respectively.

Sapienic acid, a fatty acid commonly found on the skin and in the mucosa, is active against Streptococcus sanguinis, Streptococcus mitis, and Fusobacterium nucleatum, with MBC values of 31.3 μg/mL, 375.0 μg/mL, and 93.8 μg/mL, respectively.

AGN 194310 (VTP-194310) is a pan-antagonist for retinoic acid receptors (RARs), with Kd values of 3 nM, 2 nM, and 5 nM for RARα, RARβ, and RARγ, respectively[1][2].

YM022 is a highly effective and selective gastrin/cholecystokinin (CCK)-B receptor antagonist. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively.

Compound 27b, also known as hURAT1 inhibitor 1, is an isomarine-derived, orally active inhibitor that targets both hURAT1 and GLUT9 with IC50 values of 0.16 μM and 4.47 μM, respectively. This compound exhibits significant anti-hyperuricemia effects and has demonstrated potent uric acid-lowering activity in a hyperuricemia mouse model at a dose of 10 mg kg. Importantly, Compound 27b displays no notable in vitro cytotoxicity or in vivo hepatotoxicity, and possesses favorable pharmacokinetic (PK) characteristics.

AubipyOMe serves as an effective inhibitor of Tartrate-resistant Acid Phosphatase (TRAP ACP5), a metalloenzyme identified in activated osteoclasts and macrophages. It exhibits inhibitory IC50 values of 1.3 μM against TRAP5a and 1.8 μM against TRAP5b. Additionally, it effectively suppresses TRAP activity in extracts from mouse macrophages and human lung tissues.

(R)-AS-1 is a selective positive allosteric modulator of excitatory amino acid transporter 2 (EAAT2), with an EC50 of 11 nM. At doses of 60 and 90 mg kg, (R)-AS-1 enhances spontaneous locomotor activity in mice. It demonstrates anticonvulsant properties in mouse seizure models induced by maximal electroshock (MES), pentylenetetrazole (PTZ), or electric current stimulation (32 or 44 mA), with ED50 values of 66.3, 36.3, 15.6, and 41.6 mg kg, respectively. This compound is applicable in neurological disease research.

Lucidenic acid O is a terpene compound that acts as an inhibitor of DNA polymerases. Lucidenic lactone inhibits calf DNA polymerase-α, rat DNA polymerase-β, and HIV-1 reverse transcriptase, with IC50 values of 42 μM, 99 μM, and 69 μM, respectively.

L-657926 is a stereoselective antagonist of the thromboxane A2 (TxA2) receptor, composed of (-)-9-chlorobenzyl-6-fluoro-1,2,3,4-tetrahydrocarbazol-1-yl acetic acid and (+)-9-chlorobenzyl-6-fluoro-1,2,3,4-tetrahydrocarbazol-1-yl acetic acid. The IC50 values for the (-) and (+) configurations against TxA2 are 0.27 nM and 124 nM, respectively.