(s)-3-hydroxybutyric acid is a normal human metabolite that has been found elevated in geriatric patients remitting from depression. 3-hydroxybutyric acid is synthesized in the liver from acetyl-coa in humans, and can be used as an energy source by the br
tadalafil is a carboline-based compound with vasodilatory activity. tadalafil selectively inhibits the cyclic guanosine monophosphate (cgmp)-specific type 5 phosphodiesterase- (pde-5)-mediated degradation of cgmp, which is found in the smooth muscle of th
demeclocycline hydrochloride is a tetracycline analog having a 7-chloro and a 6-methyl. because it is excreted more slowly than tetracycline, it maintains effective blood levels for longer periods of time.
11-beta-hydroxyandrostenedione is a steroid mainly found in the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue), which is a 11β-hydroxysteroid dehydrogenase isozymes inhibitor. measuring plasma 11-beta-hydroxyan
2,2,5,7,8-pentamethyl-6-chromanol is the anti-oxidant moiety of vitamin e (α-tocopherol), which has potent androgen receptor (ar) signaling modulation and anti-cancer activity against prostate cancer cell lines.
ay 9944 is a specific cholesterol biosynthesis inhibitor. ay 9944 inhibits the 7-dehydro cholesterol δ7-reductase (dhcr7) enzyme (ic50=13 nm). at high doses, ay 9944 inhibits also in cultured embryos sterol δ7-δ8 isomerase, which causes the accumulation o
az pfkfb3 26 is an effective and selective pfkfb3 inhibitor with an ic50 of 23 nm. the ic50s for pfkfb1 and pfkfb2 are 2.06 and 0.384 μm, respectively.
az10606120 dihydrochloride has anti-depressant effects and reduces tumour growth[1]. az10606120 dihydrochloride is a selective, high affinity antagonist for p2x7 receptor (p2x7r) at human and rat with an ic50 of ~10 nm and it is little or no effect at oth
az1495 is an oral active inhibitor of interleukin-1 receptor associated kinase 4 (irak4), with ic50 values of 5 nm and 23 nm for irak4 and irak1, respectively. which shows activity in treatment of mutant myd88l265p diffuse large b-cell lymphoma (dlbcl).
azd-0284 is an inverse agonist of the nuclear receptor rorγ. in development for the treatment of plaque psoriasis vulgaris and respiratory tract disorders[1].
dexpanthenol is an alcoholic analogue of d-pantothenic acid and cholinergic agent. dexpanthenol acts as a precursor of coenzyme a necessary for acetylation reactions and is involved in the synthesis of acetylcholine. although the exact mechanism of the ac
azd4320 is an inhibitor of bh3-mimicking dual bcl2/bclxl. for kpum-ms3, kpum-uh1, and str-428 cells, the ic50s values are 26 nm, 17 nm, and 170 nm , respectively.
azd5423 is an inhaled, potent, selective, and non-steroidal modulator of glucocorticoid receptor (gr) and it effectively reduces allergen-induced responses in subjects with mild allergic asthma.
azd5582 acetate is an inhibitor of iaps, which binds to the bir3 domains ciap1, ciap2, and xiap with ic50s of 15, 21, and 15 nm, respectively. azd5582 induces apoptosis.
butoconazole nitrate is the nitrate salt form of butoconazole, a synthetic imidazole derivative with fungistatic properties. butoconazole nitrate interferes with steroid biosynthesis by inhibiting the conversion of lanosterol to ergosterol, thereby changi
lacidipine is a lipophilic dihydropyridine calcium antagonist with an intrinsically slow onset of activity. due to its long duration of action, lacidipine does not lead to reflex tachycardia. it displays specificity in the vascular smooth muscle, where it
pizotifen is a strong serotonin and tryptamine antagonist, with weak anticholinergic, anti-histaminic and anti-kinin effects. it also possesses sedative and appetite-stimulating properties. pizotifen hydrochloride is an active ingredient in sandomigran, w
memantine hydrochloride is an amantadine derivative that has some dopaminergic effects. memantine hydrochloride has been proposed as an antiparkinson agent.
agomelatine is structurally closely related to melatonin. agomelatine is a potent agonist at melatonin receptors and an antagonist at serotonin-2c (5-ht2c) receptors, tested in an animal model of depression.
fenclonine is a selective and irreversible inhibitor of tryptophan hydroxylase, a rate-limiting enzyme in the biosynthesis of serotonin (5-hydroxytryptamine). fenclonine acts pharmacologically to deplete endogenous levels of serotonin.
azvudine is a potent nucleoside reverse transcriptase inhibitor (nrti), with antiviral activity on hiv, hbv and hcv. azvudine inhibits nrti-resistant viral strains. azvudine exerts highly potent inhibition on hiv-1 (ec50s ranging from 0.03 to 6.92 nm) and
dasatinib is an orally bioavailable synthetic small molecule-inhibitor of src-family protein-tyrosine kinases. dasatinib binds to and inhibits the growth-promoting activities of these kinases. apparently, because of its less stringent binding affinity for
talipexole dihydrochloride is a dopamine d2 receptor agonist, α2-adrenoceptor agonist, and 5-ht3 receptor antagonist in both rat cortical and intestinal membrane fractions with ki values of 0.35 μm and 0.22 μm, respectively. it displays antiparkinsonian a
balovaptan is a highly potent and selective brain-penetrant vasopressin 1a (hv1a) receptor antagonist, with kis of 1 and 39 nm for human (hv1a) and mouse (mv1a) receptors. it is used for the research of autism.
bamb-4 is a highly membrane-permeable inhibitor of inositol-1,4,5-trisphosphate-3-kinase a (itpka). it acts by suppressing the metastasis-promoting effect of itpka in lung tumor cells(with ic50 of 37 μm in adp-glo assay).
bay-2402234 is an inhibitor of dihydroorotate dehydrogenase (dhodh) for the treatment of myeloid malignancies.bay 2402234 is a selective low-nanomolar inhibitor of human dhodh enzymatic activity.
levofloxacin is a broad-spectrum, third-generation fluoroquinolone antibiotic and optically active l-isomer of ofloxacin with antibacterial activity. levofloxacin diffuses through the bacterial cell wall and acts by inhibiting dna gyrase (bacterial topois
bay1082439 is highly effective in inhibiting pten-null prostate cancer growth[1][2] and it is an orally bioavailable, selective pi3kα/β/δ inhibitor. bay1082439 also inhibits mutated forms of pik3ca.
axitinib is an orally bioavailable tyrosine kinase inhibitor with ic50s of 0.1, 0.2, 0.1-0.3, 1.7, 1.6 nm for vegfr1, vegfr2, vegfr3, c-kit, and pdgfrβ, respectively.