Brinzolamide(AL 4862) is a potent carbonic anhydrase II inhibitor with IC50 of 3.19 nM.Target: carbonic anhydrase IIBrinzolamide (< 1 mg) ophthalmic suspension lowers intraocular pressure in Dutch-belted pigmented rabbits in a dose-dependent manner with an onset within 0.5 hour and a peak response by 1-2 hours. Brinzolamide (0.6 mg) ophthalmic suspension lowers intraocular pressure in laser-treated glaucomatous cynomolgus monkeys in a dose-dependent manner with an onset within 1 hour and a peak response by 3 hours. Brinzolamide dosages of 30 mg/kg, produces a 44% reduction in intestinal charcoal meal progression, but 1 and 10 mg/kg produced 8% and 18% decreases, respectively, in male CD-1 mice. Brinzolamide of 1 mg/kg, 10 mg/kg, and 30 mg/kg prolongs barbiturate sleep time by 57%, 15%, and 35%, respectively, in male CD-1 mice [1]. Brinzolamide (< 3%) produces significantly greater mean percent intraocular pressure reductions and mean intraocular pressure reductions compared with placebo in patients with primary, open-angle glaucoma or ocular hypertension. The optimal intraocular pressure-lowering concentration of brinzolamide is 1%, brinzolamide 1% is well tolerated by patients with primary open-angle glaucoma or ocular hypertension when administered twice daily [2].
(Rac)-Juvenile hormone III, a natural compound that can be isolated from farnesoic acid ,is the most widely distributed Juvenile hormone homologue[1].
IDO1-IN-22 (Compound 3) is a IDO1 inhibitor (biochemical hIDO1 IC50: 67.4 nM, HeLa hIDO1 IC50: 17.6 nM). IDO1-IN-22 has excellent antitumor efficacy in LLC xenograft model, as well as desirable pharmacokinetic (PK) profile[1].
Suc-Ala-Ala-Pro-Gly-Pna is a peptide. Suc-Ala-Ala-Pro-Gly-pNA can be used for the research of various biochemical[1].
Lumefantrine D18 is the deuterium labeled Lumefantrine, which is an antimalarial drug.
Tezepelumab (AMG 157) is human monoclonal antibody (IgG2λ) that binds specifically to TSLP, blocking it from interacting with its heterodimeric receptor. Tezepelumab can be used for the research of severe, uncontrolled asthma[1].
Lucenin-2 is a natural C-glucoside compound belonging to the flavonoid class[1].
Sevasemten is an allosteric inhibitor of skeletal muscle myosin. Sevasemten exhibits selectively myosin inhibition with IC50s of ≤10 μM (skeletal), >100 μM (cardiac), respectively[1][2].
Ceftizoxime is a bacterial inhibitor which acts by interfering with bacterial cell wall synthesis and inhibiting cross-linking of the peptidoglycan.
Ivabradine (hydrochloride) is a new If inhibitor with IC50 of 2.9 μM, and used as a pure heart rate lowering agent.
AZ-1355 is an effctive lipid-lowering compound, which also inhibits platelet aggregation in vivo and elevates the prostaglandin I2/thromboxane A2 ratio in vitro.
Z-Gly-Bt is a Glycine (HY-Y0966) derivative[1].
Tolmetin is an orally active and potent COX inhibitor with IC50s of 0.35 µM and 0.82 µM human COX-1 and COX-2, respectively. Tolmetin is a non-steroidal anti-inflammatory drug (NSAID)[1][2].
3,4,6-Tri-O-acetyl-D-glucal-13C is the 13C labeled 3,4,6-Tri-O-acetyl-D-glucal[1].
11-Oxomogroside II A2 (11-Dehydroxy-mogroside IIA2 O-rhamnoside) (compound 101) is a mogroside isolated from the fruit of Luo Han Guo[1].
2-Methylpiperazine-d10 is the deuterium labeled 2-Methylpiperazine[1].
Tislelizumab, a monoclonal antibody with high binding affinity to the PD-1 receptor, minimizes Fcγ receptor binding on macrophages, thereby abrogating antibody-dependent phagocytosis, a mechanism of T cell clearance and potential resistance to anti-PD-1 therapy. Tislelizumab can be used for the research of advanced squamous non-small-cell lung cancer[1].
AZ1729 is a novel direct, positive allosteric modulator of fatty acid receptor FFA2 (pEC50=6.9), selectively activates Gi signaling but lacks the capacity to activate FFA2 Gq/G11-mediated signaling pathways; produces stimulation of [35S]GTPγS binding with pEC50 7.23, inhibits β-adrenoreceptor agonist-promoted lipolysis in primary mouse adipocytes and promotes chemotaxis of isolated human neutrophils.
D-64131 is a novel inhibitor of Tubulin polymerization that competitively binds with [(3)H]colchicine to αβ-Tubulin. IC50 Value: N/ATarget: Microtubule/Tubulinin vitro: D-64131 is cytotoxic and inhibits tumor cell proliferation in vitro (IC50 = 74 nM). D-64131 prevents growth of tumor models in mice following oral administration in vivo. D-64131 has significant potential in cancer treatment. The proliferation of tumor cells from 12 of 14 different organs and tissues was inhibited with mean IC(50)s of 62 nM by D-64131.in vivo: In animal studies, no signs of systemic toxicity were observed after p.o. dosages of up to 400 mg/kg of D-64131. In xenograft experiments with the human amelanoic melanoma MEXF 989, D-64131 was highly active with treatment resulting in a growth delay of 23.4 days at 400 mg/kg. Therefore, D-64131 and analogues have the potential to be developed for cancer therapy, replacing or supplementing standard therapy regimens with tubulin-targeting drugs from natural sources.
Mefox is a degradation product of folic acid (HY-16637)[1].
Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties[1][2][3].
Ro5-3335, a benzodiazepine, acts as an inhibitor of core binding factor (CBF) leukemia. Ro5-3335 is a RUNX1-CBFβ interaction inhibitor that represses RUNX1/CBFB-dependent transactivation[1].
Azomycin is an antibiotic which can be active against aerobic Gram-positive and Gram-negative bacteria.
Antagonist G is a potent vasopressin antagonist. Antagonist G is also a weak antagonist of GRP and Bradykinin. Antagonist G induces AP-1 transcription and sensitizes cells to chemotherapy[1][2].
Bis(dihydrochelerythrinyl)amine possesses anti-bacteria activity[1].
Rocagloic acid is a racaglamide derivative isolated from the fruits of Amoora cucullata with potent cytotoxicity[1].
1,2-Di-O-acetyl-3-azido-3-deoxy-5-O-(4-methyl)benzoyl-D-ribofuranose is a purine nucleoside analog. Purine nucleoside analogs have broad antitumor activity targeting indolent lymphoid malignancies. Anticancer mechanisms in this process rely on inhibition of DNA synthesis, induction of apoptosis, etc[1].
Ramosetron Hydrochloride(YM060 Hydrochloride) is a serotonin 5-HT3 receptor antagonist for the treatment of nausea and vomiting.Target: 5-HT3 ReceptorRamosetron hydrochloride selectively blocks serotonin receptors (5-HT3). Serotonin plays a vital role in vomiting, serotonin-induced bradycardic reflex and peristalsis. The pharmacological action of Ramosetron hydrochloride is sustained and potent.
Desaminotyrosine is a microbially associated metabolite protecting from influenza through augmentation of type I interferon signaling.
SGLT1/2-IN-2 demonstrates potent dual inhibitory activities (IC50 = 96 nM for SGLT1 and IC50 = 1.3 nM for SGLT2).