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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC74900 BMS-817378 BMS-817378, also known as SCR-1481B1 is a potent and selective MET inhibitor. SCR-1481B1 inhibited MET kinase with IC50 = 1.7 nM.
DC74901 Naftifine HCl Naftifine is an allylamine antifungal drug for the topical treatment of tinea pedis, tinea cruris, and tinea corporis (fungal infections). Its precise mechanism of action is unknown, but may involve selectively blocking sterol biosynthesis via inhibition of the squalene 2,3-epoxidase enzyme. The half-life is approximately 2–3 days. The metabolites are excreted in the urine and feces.
DC74902 NTNCB HCl NTNCB is a selective, non-peptide competitive NPY Y5 antagonist. NTNCB potently antagonizes NPY inhibition of forskolin-stimulated cAMP. NTNCB Displays some affinity for cloned human D2 and α2C receptors (Ki values are 63 and 100 nM respectively).
DC74903 Atibeprone Atibeprone, also known as Lu 53439, is MAO-B inhibitor. The anticonvulsant activity of inhibitors of monoamine oxidase (MAO) was reported early after the development of irreversible MAO inhibitors such as tranylcypromine, but was never clinically used because of the adverse effects of these compounds. In contrast to esuprone and L-deprenyl, the selective MAO-B inhibitor LU 53439 was not effective in the kindling model; this substantiates the previous notion that the anticonvulsant activity of L-deprenyl is not related to MAO-B inhibition, but to other effects of this drug, such as inhibition of MAO-A.
DC74904 Cefovecin Sodium Cefovecin, also known as UK-287074, is an antibiotic of the cephalosporin class. Cefovecin interferes with the synthesis of bacterial cell walls, by binding to penicillin binding proteins. Due to high protein-binding, it is not effective against species of Pseudomonas or Enterococcus. The maximum anti-bacterial activity occurs approximately two days after cefovecin has been administered. It is used to treat skin infections caused by Pasteurella multocida in cats, and Staphylococcus intermedius and Streptococcus canis in dogs.
DC74905 Quizartinib free base Quizartinib, also known as AC220 and AC010220, is a highly potent FMS-like receptor tyrosine kinase-3 (FLT3) inhibitor. Quizartinib free base inhibits FLT3 activity and displays antitumor properties in a mouse MV4-11 tumor xenograft model.
DC74906 DOTA-TATE acetate DOTA-TATE (DOTATATE, DOTA-octreotate, oxodotreotide, DOTA-(Tyr3)-octreotate, and DOTA-0-Tyr3-Octreotate) is an eight amino acid long peptide, with a covalently bonded DOTA bifunctional chelator. DOTA-TATE can be reacted with the radionuclides gallium-68 (T1/2 = 68 min), lutetium-177 (T1/2 = 6.65 d) and copper-64 (T1/2 = 12.7 h) to form radiopharmaceuticals for positron emission tomography (PET) imaging or radionuclide therapy. DOTA-TATE is a compound containing tyrosine3-octreotate, an SSR agonist, and the bifunctional chelator DOTA (tetraxetan). SSRs are found with high density in numerous malignancies, including CNS, breast, lung, and lymphatics.
DC74907 Bimakalim Bimakalim, an ATP-sensitive potassium channel opener, mimics the effects of ischemic preconditioning to reduce infarct size, adenosine release, and neutrophil function in dogs
DC74908 CRD-733 CRD-733 is a PDE9A inhibitor. CRD-733 Reverses Pressure Overload-Induced Heart Failure. CRD-733 improves key hallmarks of HF including LV hypertrophy, LV dysfunction, left atrial dilation, and pulmonary edema after pressure overload in the mouse transverse aortic constriction HF model.
DC74909 KHS-101 free base KHS-101 is a selective inducer of neuronal differentiation. KHS101 induces neuronal differentiation in cultured hippocampal neural progenitor cells (NPCs) by interacting with TACC3 (EC50 ~1 μM). KHS101 disrupts energy metabolism in human glioblastoma cells and reduces tumor growth in mice. KHS101 promoted tumor cell death in diverse GBM cell models. KHS101 exerted cytotoxic effects by disrupting the mitochondrial chaperone heat shock protein family D member 1 (HSPD1). In GBM cells, KHS101 promoted aggregation of proteins regulating mitochondrial integrity and energy metabolism.
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.
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.

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