MK-2894 sodium salt is a highly potent and selective second generation EP4 antagonist.IC50 value:Target: EP4MK-2894 exhibits favorable pharmacokinetic profile in a number of preclinical species and potent anti-inflammatory activity in several animal models of pain/inflammation. MK-2894 also shows favorable GI tolerability profile in rats when compared to traditional NSAID indomethacin.
Isoliquiritin, isolated from Licorice Root, inhibits angiogenesis and tube formation. Isoliquiritin also exhibits antidepressant-like effects and antifungal activity[1][2][3].
Fluocinolone Acetonide is a glucocorticoid derivative used topically in the treatment of various skin disorders.Target: Glucocorticoid ReceptorFluocinolone acetonide is a corticosteroid primarily used in dermatology to reduce skin inflammation and relieve itching. It is a synthetic hydrocortisone derivative. The fluorine substitution at position 9 in the steroid nucleus greatly enhances its activity. A typical dosage strength used in dermatology is 0.01-0.025%. One such cream is sold under the brand name Flucort-N and includes the antibiotic neomycin. The Glucocorticoid Receptor(GR) binding affinity (IC50) for Fluocinolone Acetonide(FA) was 2.0 nM, respectively. The values is similar to the GR transactivation EC50 of 0.7 nM for FA, respectively [1, 2].
Cromakalim is a potassium channel opener. Cromakalim can be used as a bronchodilator in asthma. Cromakalim inhibits the spontaneous tone of human isolated bronchi in a concentration-related manner being nearly as effective as isoprenaline or theophylline[1].
ROCK-IN-6 is a potent and selectiveROCK2 inhibitor with an IC50 of 2.19 nM. ROCK-IN-6 is extracted from patent WO2021164351 A1, example 7, has the potential for glaucoma and retinal diseases research[1].
Neohesperidin dihydrochalcone is a synthetic glycoside chalcone, is added to various foods and beverages as a low caloric artificial sweetener.
Monoethylglycinexylidide (MEGX) hydrochloride is a metabolite of Lidocain (HY-B0185) via oxidative N-deethylation of Lignocaine by liver cytochrome P-450 enzymes in the liver. Monoethylglycinexylidide has proven to be a highly sensitive indicator of hepatic dysfunction, especially in the field of liver transplantation[1][2].
Suprofen is a non-steroidal anti-inflammatory drug (NSAID). Target: PGE synthaseSuprofen is an NSAID.Suprofen is an ibuprofen-type anti-inflammatory analgesic and antipyretic. It inhibits prostaglandin synthesis and has been proposed as an anti-arthritic. suprofen was clinically effective but the differential suppression of prostanoids favors 200mg which spares 6-keto PGF1a [1, 2].
Hexahydrofarnesyl acetone (6,10,14-Trimethyl-2-pentadecanone), a sesquiterpene isolated from Launaea mucronata, is the major constituents of the essential oil. Hexahydrofarnesyl acetone has antibacterial, anti-nociceptive and anti-inflammation activities[1][2].
Carboxy-PTIO potassium is a potent nitric oxide (NO) inhibitor that can make a quick reaction with NO to produce NO2. Carboxy-PTIO can prevent hypotension and endotoxic shock through the direct scavenging action against NO in lipopolysaccharide-stimulated rat model[1][2][3].
Evocarpine, a quinolone alkaloid that could be isolated from Evodiae fructus, inhibitss Ca2+ influx through voltage-dependent calcium channels. Antimycobacterial activity[1][2].
Bis-PEG1-PFP ester is a non-cleavable (1 unit PEG) ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[1].
Kalii Dehydrographolidi Succinas (Potassium dehydroandrographolide succinate), extracted from herbal medicine Andrographis paniculata (Burm f) Nees, is widely used for the treatment of viral pneumonia and viral upper respiratory tract infections because of its immunostimulatory, anti-infective and anti-inflammatory effect[1][2].
Liquiritin apioside, a main flavonoid component of licorice, possesses antitussive effects[1].
Pivalylbenzhydrazine (Pivhydrazine) is a potent monoamine oxidase (MAO) inhibitor. Pivalylbenzhydrazine decreases cartilage growth in normal rats. Pivalylbenzhydrazine can be used in research of depression[1].
Endokinin D is a human tachykinin and consist of 14 amino acid residues[1].
4-O-Cinnamoylquinic acid could inhibit superoxide anion generation in human neutrophils[1].
Cevidoplenib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities[1][2].
Beclometasone dipropionate is a potent glucocorticoid agonist; it is a prodrug of the free form, beclometasone. IC50 Value: 0.2 nM (Inhibiting thymidine incorporation) [1]Target: glucocorticoid receptorin vitro: Cortisol and beclomethasone dipropionate were more potent than salbutamol in inhibiting thymidine incorporation with IC50 values of 5 nM and 0.2 nM respectively. Cortisol 100 nM led to a 16.6 +/- 6.5% reduction and beclomethasone dipropionate 3 nM led to a 17.8 +/- 5.8% reduction in cell number [1]. in vivo: Controlled trials involving 497 adults and children demonstrated similar clinical efficacy between nebulized BDP and either nebulized fluticasone propionate or nebulized budesonide. Meta-analyses show that BDP, like other inhaled corticosteroids, has no major influence on patient height, urinary cortisol concentration, or bone metabolism [2]. Beclometasone dipropionate (BDP) 800 microgday(-1) suspension for nebulization and budesonide (BUD) 750 microg day(-1) given by nebulization in a twice-daily regimen, and when used in addition to the usual maintenance therapy, resulted in comparable clinical efficacy across all parameters [3]. Clinical trial: Efficacy and Tolerability of Beclometasone/Formoterol Single Inhaler in Patients With Moderate to Severe Persistent Asthma. Phase 3
Mogamulizumab (KW-0761) is a defucosylated humanized recombinant anti-CCR4 monoclonal antibody (MAb). Mogamulizumab can eliminate tumor cells by antibody-dependent cellular cytotoxicity (ADCC). Mogamulizumab can be used in the research of cancers, adult T-cell leukemia/lymphoma (ATLL), cutaneous T-cell lymphoma (CTCL)[1][2][3].
Allopurinol-d2 is deuterium labeled Allopurinol. Allopurinol is a potent xanthine oxidase inhibitor (IC50 values of 0.2 to 50 μM). Allopurinol can be used for the research of hyperuricemia and gout. Antileishmanial effect[1][2].
GW 766994 is a specific and oral chemokine receptor-3 (CCR3) antagonist, which has entered clinical trial for asthma and eosinophilic bronchitis.
Ginsenoside F3, a component of PPTGs (an minor saponin in the leaves of Panax ginseng), has immunoenhancing activity by regulating production and gene expression of type 1 cytokines (IL-2, IFN-gamma) and type 2 cytokines (IL-4 and IL-10)[1].
Interphotoreceptor retinoid-binding protein(668-687), the amino acid residues 668 to 687 of human interphotoreceptor retinoid binding protein (IRBP), induces uveitis[1].
(R)-(+)-Tetrahydroberberine is the inactive isomer of (S)-(-)-Tetrahydroberberine (HY-N1418), and can be used as an experimental control. (S)-(-)-Tetrahydroberberine is an alkaloid and intermediate in the biosynthesis of berberine with insecticidal activity[1].
D-Ribose-d2 is the deuterium labeled D-Ribose. D-Ribose is an energy enhancer, and acts as a sugar moiety of ATP, and widely used as a metabolic therapy supplement for chronic fatigue syndrome or cardiac energy metabolism. D-Ribose is active in protein gl
Basiliximab (CHI 621) is a recombinant chimeric murine/human IgG1 monoclonal anti-interleukin-2 receptor antibody. Basiliximab can be used for the research of renal transplantation[1].
FXb is an immunizing and functionalized hapten and can be used for protein bioconjugates preparation[1].
(R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
Norisoboldine hydrochloride is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine hydrochloride, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis[1][2].