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Novel inhibitors

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Cat. No. Product Name Field of Application Chemical Structure
DC9448 MK591
MK591(Quiflapon sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor.
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DC21286 MK-4074
MK-4074 is a potent, liver-specific, orally active inhibitor of acetyl-CoA carboxylase ACC1 and ACC2 with IC50 of ~3 nM.
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DC20454 MK-4074 sodium salt
MK-4074 is a potent, liver-specific, orally active inhibitor of acetyl-CoA carboxylase ACC1 and ACC2 with IC50 of ~3 nM.
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DC22731 MK-3901
MK-3901 is a potent, selective, orally active P2X3 antagonist with IC50 of 21 nM.
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DC7646 MK3697
MK-3697 is a third insomnia drug, currently being developed by Merck. MK-3697 is a potent and selective Orexin receptor antagonist with Ki = 0.95 nM.
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DC21297 MK-3281
MK-3281 is a potent and orally bioavailable inhibitor of HCV NS5B polymerase with IC50 of 6 nM.
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DC9397 MK-3207 (Hydrochloride)
MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC50= 0.12 nM; Ki value= 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3.
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DC24121 MK2-IN-1
MK2-IN-1 is a potent, selecitve, non-ATP competitive MAPKAPK2(MK2) inhibitor with IC50 of 0.11 uM.
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DC9607 MK-2894
MK-2894 is a highly potent and selective second generation EP4 antagonist.
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DC23099 MK-2048
MK-2048 is a potent inhibitor of HIV-1 integrase (IN) and IN mutant R263K with IC50 of 2.6 nM and 1.5 nM, respectively.
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DC21296 MK-204
MK-204 is a potent, selective AKR1B10 inhibitor with IC50 of 80 nM, shows high selective (270-fold) over AKR1B1.
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DC26086 MK-1925
MK-1925 is a selective, orally active, brain-penetrant opioid receptor-like 1 (ORL1.
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DC23650 MK-1832
MK-1832 is a potent, selective Kv1.5 inhibitor with IC50 of 86 nM, exhibits improved selectivity for IKur over IKs (>3000-fold) compares with MK-0448 (70-fold), also exhibits an improved preclinical pharmacokinetic profile..
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DC21293 MK-1
MK1 is a small molecule inducer of megakaryopoiesis (EC90=750 nM) that induces the differentiation of common myeloid progenitors (CMP) to megakaryocytes, does not adversely affect erythrocyte differentiation.
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DC9398 MK-0974
MK-0974(Telcagepant) is a highly potent, selective, and orally bioavailable CGRP receptor antagonist with Ki values of 0.77 nM and 1.2 nM for human and rhesus CGRP receptors respectively; displays >1500-fold lower affinity for the canine and rat receptors
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DC3167 MK0812
MK-0812 is chemokine receptor CCR-2 antagonist
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DC23343 MK-0731
MK-0731 is a potent, selective kinesin spindle protein (KSP) inhibitor with IC50 of 2.2 nM, cell EC50 of 5.3 nM.
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DC23665 MK-0674
MK-0674 is a potent, selective, reversible and orally active cathepsin K inhibitor with IC50 of 1 nM.
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DC21290 MK-0448
MK-0448 is a potent, specific I(Kur) current/Kv1.5 channel inhibitor with IC50 of 8.6 nM, potently inhibits IKur in human atrial myocytes with IC50 of 10.8 nM.
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DC21289 MK-0429
MK-0429 is a potent, selective, orally-active nonpeptide αvβ3 integrin inhibitor with IC50 of 0.08 nM in SPAV3 assay.
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DC9456 MK-0354
MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.
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DC23419 MK-0249
MK-0249 is a novel potent, selective histamine H3 inverse agonist for the treatment of cognitive impairment with schizophrenia..
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DC21283 MJN-228
MJN-228 is a selective ligand for the lipid-binding protein nucleobindin 1 (NUCB1) with IC50 of 3.3 uM (blocks AEA-DA probe labeling of NUCB1).
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DC9468 Mizolastine
Mizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions.
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DC22150 MIV-711
MIV-711 (MIV711, MV076159) is a potent, selective cathepsin K inhibitor with Ki of 0.98 nM, displays >1300-fold versus the other human cathepsins.
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DC21279 MIV-247
MIV-247 (MIV247) is a potent, selective, orally active inhibitor of cathepsin S with Ki of 2.1 nM (human cathepsin S).
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DC21651 miR544-IN-1
miR544-IN-1 (SID 3712249) is a selective small molecule inhibitor of miR-544 biogenesis.
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DC11045 miR-21 inhibitor 37
miR-21 inhibitor 37 is a novel inhibitor of miR-21 function with EC50 of 5.3 uM in HeLa-miR21-Luc assays, displays no inhibition of miR-122.
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DC21919 MIR17PTi
MIR17PTi is a novel LNA gapmeR antisense oligonucleotide (LNA-ASO), first-in-class inhibitor of pri-mir-17-92.
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DC11902 Minesapride
Minesapride (DSP-6952) is a novel potent, selective, orally active 5-HT4 receptor partial agonist with Ki of 50-100 nM for human 5-HT4a/4b/4c.
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