| DC74910 |
TRX-0237 mesylate |
Hydromethylthionine, also known as LMTM and Leucomethylene Blue, is a apotent tau aggregation inhibitor for the treatment of Alzheimer's disease (AD) and frontotemporal dementia. Hydromethylthionine showed pharmacological activity on brain structure and function as both monotherapy and as an add-on to symptomatic treatment in certain patients with Alzheimer’s disease. |
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| DC74911 |
Gramicidin S TFA |
Gramicidin S (GS), also known as Gramicidin soviet, is an antibiotic. GS reduces the cell number of planktonic cells within 20-40 min at a concentration of 40-80 μg/mL. GS kills the cells of pre-grown biofilms at concentrations of 100-200 μg/mL, such that no re-growth is possible. The translocation of the peptide into the cell interior and its complexation with intracellular nucleotides, including the alarmon ppGpp, can explain its anti-biofilm effect. The successful treatment of persistently infected root canals of two volunteers confirms the high effectiveness of GS. The broad GS activity towards resistant, biofilm-forming E. faecalis suggests its applications for approval in root canal medication. |
|
| DC74912 |
Tirofiban HCl hydrate |
Tirofiban is an antiplatelet drug. It belongs to a class of antiplatelet named glycoprotein IIb/IIIa inhibitors. Tirofiban is the first drug candidate whose origins can be traced to a pharmacophore-based virtual screening lead. Tirofiban is indicated to reduce the rate of thrombotic cardiovascular events (combined endpoint of death, myocardial infarction, or refractory ischemia/repeat cardiac procedure) in patients with non-ST elevation acute coronary syndrome (NSTE-ACS). |
|
| DC74913 |
BMS-223131 |
BMS-223131 is a novel opener of large conductance Ca2+-activated K+ (maxi-K) channels. BMS-223131 effectively reduced stress-induced colonic motility and visceral nociception supporting the potential utility of maxi-K channel openers for the treatment of bowel disorders involving dysfunctional motility and visceral sensitivity. |
|
| DC74914 |
Terbutaline |
Terbutaline is a β2 adrenergic receptor agonist, used as a "reliever" inhaler in the management of asthma symptoms and as a tocolytic (anti-contraction medication) to delay preterm labor for up to 48 hours. This time can then be used to administer steroid injections to the mother which help fetal lung maturity and reduce complications of prematurity. It should not be used to prevent preterm labor or delay labor more than 48–72 hours. |
|
| DC74915 |
Bromofosfamide |
Bromofosfamide, alkso known KM-135, is an alkylating agent with antitumor activity. |
|
| DC74916 |
Giredestrant tartrate |
Giredestrant, also known as GDC-9545 and RG6171, is a SERD. GDC-9545 is an orally available selective estrogen receptor degrader/downregulator (SERD), with potential antineoplastic activity. Upon oral administration, SERD GDC-9545 specifically targets and binds to the estrogen receptor (ER) and induces a conformational change that promotes ER degradation. |
|
| DC74917 |
Elacestrant free base |
Elacestrant, also known as RAD1901, is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities. Upon oral administration of higher doses of RAD1901, this agent acts as a SERD, which binds to the estrogen receptor (ER) and induces a conformational change that results in the degradation of the receptor. This may inhibit the growth and survival of ER-expressing cancer cells. At lower doses of this agent, RAD1901 acts as a SERM and has estrogen-like effects in certain tissues, which can both reduce hot flashes and protect against bone loss. In addition, RAD1901 is able to cross the blood-brain barrier (BBB). |
|
| DC74918 |
Pramipexole HCl |
Pramipexole hydrochloride is an agonist of the Gαi-linked dopamine receptors D2, D3, and D4. It is relatively inactive at the Gαs-linked dopamine receptors D1 and D5, as well as at serotonin and adrenergic receptors. This narrow profile of receptor binding distinguishes pramipexole from other compounds, particularly those derived from ergot fungi, which can be associated with adverse events when used for treating Parkinson’s disease and other disorders. |
|
| DC74919 |
Adekalant tartrate |
Adekalant, also known as H 345/52. is a new antiarrhythmic compound with low proarrhythmic activity. Adekalant concentration-dependently blocked HERG-carried currents with an IC50 of 230 nM. Adekalant preferentially bound to the open channel with unusually rapid kinetics and was trapped by channel closure. Voltage-independent behavior of Adekalant was observed during both square-pulse and action potential clamp protocols. It is proposed that block of I(Kr) is the principal mechanism by which Adekalant delays repolarization in human myocardium. Adekalant blocks I(Kr) with high potency and I(Ca) with somewhat lower potency and was found to delay ventricular repolarization without substantially increasing temporal or spatial dispersion and without inducing early after-depolarizations or TdP. |
|
| DC74920 |
Tirabrutinib HCl |
Tirabrutinib HCl, also known as ONO-4059 HCl, is a potent and orally active Bruton agammaglobulinemia tyrosine kinase (BTK) in hibitor. Upon administration, ONO-4059 covalently binds to BTK within B cells, thereby preventing B-cell receptor signaling and impeding B-cell development. As a result, this agent may inhibit the proliferation of B-cell malignancies. BTK, a cytoplasmic tyrosine kinase and member of the Tec family of kinases, plays an important role in B lymphocyte development, activation, signaling, proliferation and survival. |
|
| DC74921 |
OG-488 SE |
OG 488 SE is a Green fluorescent dye; supplied as NHS ester. OG-488 SE is a potential fluorescein precursor for live bacteria detection. |
|
| DC74922 |
BU-226 HCl |
BU-226 is a Potent, highly selective I2 ligand. |
|
| DC74923 |
Nitrocaramiphen HCl |
Nitrocaramiphen is a muscarinic antagonist with 71-fold selectivity for M1 over M2. |
|
| DC74924 |
Y-39983 HCl |
Y-39983, also known as Y-33075, is a potent and selective inhibitor of ROCK family with IC50 value of 3.6nM for ROCK. Y-39983 attenuates experimental autoimmune encephalomyelitis via inhibition of demyelination. Y-39983 downregulates RhoA/Rho-associated kinase expression during its promotion of axonal regeneration. Y-39983, promotes regeneration of crushed axons of retinal ganglion cells into the optic nerve of adult cats. |
|
| DC74925 |
Batanopride HCl |
Batanopride is an antiemetic 5-HT3 receptor antagonist. |
|
| DC74926 |
Bisphosphocin Nu-3 |
NU-3, also known as Bisphosphocin NU-3, is a protonated modified nucleotide with antimicrobial activity. Nu-3 had a wide antibacterial spectrum to Gram-positive, Gram-negative and some resistant bacteria. The MIC values of Nu-3 against all tested MRSA and MSSA were roughly in a same range while MICs of Oxacillin and Vancomycin varied between the bacteria tested. In the mouse model of skin wound infection study, the treatment with 5% Nu-3 glycerine solution also showed comparable therapeutic effects to Ciprofloxacin Hydrochloride Ointment. Nu-3 represents a new class of antibacterial agents for treating topical infections and acts via a different mechanism from conventional antibiotics. |
|
| DC74927 |
OD36 free base |
OD36 is a cell permeable, highly potent, selective, and ATP-competitive inhibitor of receptor-interacting protein 2 (RIPK2, IC₅₀ = 5.3 nM). |
|
| DC74928 |
HM43239 |
HM43239 is an orally active small molecule inhibitor of FLT3 that selectively inhibits not only FLT3 wild type, ITD mutants or TKD mutations, but also FLT3 ITD/TKD double mutations. HM43239 directly inhibits the kinase activity of FLT3 as a reversible Type I inhibitor and effectively modulates downstream p-STAT5 and p-ERK. HM43239 also demonstrated inhibition of SYK, JAK1/2 and TAK1, known to be involved in tumor cell proliferation and/or differentiation HM43239 monotherapy induced dose-dependent regression of tumor growth in FLT3 wild-type and FLT3 mutated leukemia cancer cell line. |
|
| DC74929 |
Vaneprim |
Vaneprim is an antibacterial agent. |
|
| DC74930 |
A33903 |
A33903 is a 1,4-benzodiazepine analog that is being studied as a potential inhibitor of respiratory syncytial virus. This molecule was moderately active and demonstrated good pharmacokinetic properties. |
|
| DC74931 |
TM-5275 sodium |
TM 5275 sodium salt is an orally bioavailable plasminogen activator inhibitor-1 (PAI-1) inhibitor. |
|
| DC74932 |
Anecortave Acetate |
Anecortave Acetate is an angiostatic steroid used for proteomics research. Anecortave acetate possesses a mechanism of action that decreases CNV growth irrespective of the inciting angiogenic stimulus, has a dosing-interval that allows its use as prophylactic therapy, and is safe. |
|
| DC74933 |
Trelagliptin succinate |
Trelagliptin, also known as SYR-472, is a long acting dipeptidyl peptidase-4 (DPP-4) inhibitor that is being developed by Takeda for the treatment of type 2 diabetes (T2D). Once-weekly SYR-472 treatment produced clinically and statistically significant improvements in glycaemic control in patients with type 2 diabetes. It was well tolerated and might be a new treatment option for patients with this disease. Trelagliptin (Zafatek(®)) was approved in Japan for the treatment of type 2 diabetes mellitus. |
|
| DC74934 |
Bosutinib hydrate |
Bosutinib, also known as SKI-606, is a synthetic quinolone derivative and dual kinase inhibitor that targets both Abl and Src kinases with potential antineoplastic activity. Unlike imatinib, bosutinib inhibits the autophosphorylation of both Abl and Src kinases, resulting in inhibition of cell growth and apoptosis. Because of the dual mechanism of action, this agent may have activity in resistant CML disease, other myeloid malignancies and solid tumors. Abl kinase is upregulated in the presence of the abnormal Bcr-abl fusion protein which is commonly associated with chronic myeloid leukemia (CML). Overexpression of specific Src kinases is also associated with the imatinib-resistant CML phenotype. Bosutinib was approved in 2012 |
|
| DC74935 |
Phentolamine Mesylate |
Phentolamine is a reversible antagonist of α-adrenergic receptors, non-specifically binding all α1- and α2-adrenoceptors with nanomolar affinities. When given intravenously, phentolamine rapidly and transiently increases local blood flow, which has proven useful for the management of hypertensive emergencies. Phentolamine also has applications in controlling chronic and emergent pain. |
|
| DC74937 |
Moxifloxacin HCl |
Moxifloxacin is a fourth-generation synthetic fluoroquinolone antibacterial agent. Its antibacterial spectrum includes enteric Gram-(−) rods (Escherichia coli, Proteus species, Klebsiella species), Haemophilus influenzae, atypical bacteria (Mycoplasma, Chlamydia, Legionella), and Streptococcus pneumoniae, and anaerobic bacteria. It differs from earlier antibacterials of the fluoroquinolone class such as levofloxacin and ciprofloxacin in having greater activity against Gram-positive bacteria and anaerobes. Because of its potent activity against the common respiratory pathogen Streptococcus pneumoniae, it is considered a "respiratory quinolone." |
|
| DC74938 |
Budiodarone HCl |
Budiodarone, also known as ATI-2042, is an antiarrhythmic agent and chemical analog of amiodarone. Budiodarone has a half life of 7 h. It is electrophysiologically similar to amiodarone, but may not have metabolic and interaction side effects. ATI-2042 effectively reduced AFB over all doses studied by reducing mean episode duration. Budiodarone holds much promise as an antiarrhythmic drug to prevent fibrillation. As a drug that spans over many of antiarrhythmic drug classes, the electrophysiological activity of budiodarone includes. |
|
| DC74939 |
R1487 HCl |
R-1487 is an orally bioavailable and highly selective inhibitors of p38α mitogen-activated protein kinase. Pyruvate dehydrogenase (PDH) plays an important role in regulating carbohydrate oxidation in skeletal muscle. PDH is deactivated by a set of PDH kinases (PDK1, PDK2, PDK3, PDK4), with PDK2 and PDK4 being the most predominant isoforms in skeletal muscle. |
|
| DC74940 |
Bemnifosbuvir hemisulfate |
Bemnifosbuvir hemisulfate, also known as AT-527 and RG 6422, a hemisulfate salt of AT-511, a guanosine nucleotide prodrug, is a potent and orally active HCV viral replication inhibitor. AT-511 is a prodrug form of the antiviral nucleoside analog AT-9010. It reduces the infectious virus yield in cells infected with Middle East respiratory syndrome coronavirus (MERS-CoV), severe acute respiratory syndrome CoV (SARS-CoV), SARS-CoV-2, human CoV 229E (HCoV-229E), and HCoV-OC43 (EC90s = 37, 0.47, 2.8, 1.2, and 0.5 µM, respectively). |
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