| Cat. No. | Product Name | Field of Application | Chemical Structure |
|---|---|---|---|
| DC21573 | Ro 5212773 Featured | EPPTB is a selective antagonist of the trace amine-associated receptor 1 (TAAR1). |
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| DC24163 | XEN-907 | A potent, selective NaV1.7 blocker with IC50 of 3 nM. |
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| DC23603 | Traxoprodil mesylate Featured | A potent, selective N-methyl-D-aspartate (NMDA) antagonist with selectivity for the NR2B subunit. |
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| DC20771 | Faldaprevir | A potent, selective noncovalent competitive inhibitor of HCV NS3/4A protease with Ki of 2.6 and 2.0 nM for GT1a and 1b NS3-NS4A protease, respectively. |
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| DC22726 | SB 290157 | A potent, selective nonpeptide antagonist of anaphylatoxin C3a receptor (C3aR) with IC50 of 200 nM. |
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| DC22672 | SB-612111 hydrochloride | A potent, selective opiate receptor-like orphan receptor (ORL-1, NOP) antagonist with Ki of 0.33 nM. |
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| DC22947 | RN-9893 hydrochloride | A potent, selective orally-bioavailable TRPV4 antagonist with IC50 of 320, 420 and 660 nM for mouse, human and rat TRPV4 channels, respectively. |
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| DC22951 | RN-9893 | A potent, selective orally-bioavailable TRPV4 antagonist with IC50 of 320, 420 and 660 nM for mouse, human and rat TRPV4 channels, respectively. |
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| DC24064 | SB-408124 hydrochloride Featured | A potent, selective OX1 receptor antagonist with Ki of 57 nM (whole cell assay), and 27 nM (cell membrane-based SPA assay). |
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| DC11849 | DSM421 | A potent, selective P. falciparum dihydroorotate dehydrogenase (PfDHODH) with IC50 of 53 nM. |
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| DC23213 | SCIO-469 | A potent, selective p38α MAPK inhibitor with IC50 of 9 nM. |
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| DC22577 | Revizinone | A potent, selective PDE3 inhibitor with IC50 of 36 nM, displays >20,000-fold selectivity over PDE1.. |
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| DC22963 | Org-9935 | A potent, selective PDE3 inhibitor with IC50 of 50 nM. |
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| DC22942 | BeKm-1 | A potent, selective peptide inhibitor of hERG channel with IC50 of 3.3 nM for hERG1 channels. |
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| DC22767 | UK-500001 | A potent, selective phosphodiesterase 4 (PDE4) inhibitor with IC50 of 26.1, 22.8, 21 and 0.28 nM for PDE4A4, PDE4B2, PDE4C2 and PDE4D3, respectively.. |
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| DC11635 | Poloxin-2 | A potent, selective PLK1 PBD inhibitor with IC50 of 1.36 uM. |
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| DC22535 | CGP-25454A | A potent, selective presynaptic dopamine autoreceptor antagonist. |
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| DC21587 | RR 601 | A potent, selective protein tyrosine phosphatase DUSP5, PTP1B and SHP-2 inhibitor with IC50 of 36 uM, 2.1 and 1.1 uM respectively, 8-fold selectivity for PTP1B versus DUSP5. |
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| DC26105 | AGN-195183 | A potent, selective RARα agonist. |
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| DC22996 | LE-540 | A potent, selective RARβ antagonist that inhibits RA-induced transcriptional activation of RARβ, but not RARα, RARγ or RXRα on a variety of RA response elements. |
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| DC22547 | RIPK2-IN-2 | A potent, selective receptor interacting protein-2 (RIP2) kinase inhibitor.. |
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| DC11942 | VU591 | A potent, selective renal outer medullary potassium channel (ROMK, Kir1.1) inhibitor with IC50 of 0.24 uM in T1+ flux assays. |
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| DC22701 | SEW2871 | A potent, selective S1P1 receptor full agonist with EC50 of 13.8 nM, with no activites at the S1P2-5 receptors. |
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| DC11560 | SPM-242 | A potent, selective S1P3 antagonist with Ki of 0.25 nM. |
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| DC11561 | SPM-242 racemate | A potent, selective S1P3 antagonist with Ki of 0.25 nM. |
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| DC22702 | PD144418 | A potent, selective sigma 1 ligand with Ki of 0.08 nM, >3000-fold selectivity over sigma 2 (Ki=1377 nM). |
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| DC22663 | CB-64D | A potent, selective sigma-2 receptor agonist with Ki of 16.5 nM, 200-fold selectivity over sigma 1 (Ki=3063 nM). |
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| DC22703 | CM 764 | A potent, selective sigma-2 receptor agonist with Ki of 3.5 nM, 25-fold selectivity over sigma-1 receptors (Ki=86.6 nM). |
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| DC21700 | Stafib-1 Featured | A potent, selective small molecule inhibitor of transcription factor STAT5b with Ki of 44 nM, >50-fold selectivity over STAT5a.. |
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| DC23946 | PAP-1 Featured | PAP-1 is a selective inhibitor of Kv1.3, voltage-gated K+ channel. PAP-1 (EC50=2 nM) potently inhibits human T effector memory cell proliferation and delayed hypersensitivity. IC50 value: 2 nM (EC50) [1]in vitro: blocks Kv1.3 in a use-dependent manner, with a Hill coefficient of 2 and an EC50 of 2 nM, by preferentially binding to the C-type inactivated state of the channel. PAP-1 is 23-fold selective over Kv1.5, 33- to 125-fold selective over other Kv1-family channels, and 500- to 7500-fold selective over Kv2.1, Kv3.1, Kv3.2, Kv4.2, HERG, calcium-activated K+ channels, Na+,Ca2+, and Cl- channels [1]. The blockade of Kv1.3 results in membrane depolarization and inhibition of TEM proliferation and function. In this study, the in vitro effects of PAP-1 on T cells and the in vivo toxicity and pharmacokinetics (PK) were examined in rhesus macaques (RM) with the ultimate aim of utilizing PAP-1 to define the role of TEMs in RM infected with simian immunodeficiency virus (SIV). Electrophysiologic studies on T cells in RM revealed a Kv1.3 expression pattern similar to that in human T cells. Thus, PAP-1 effectively suppressed TEM proliferation in RM [2].in vivo: PAP-1 does not exhibit cytotoxic or phototoxic effects, is negative in the Ames test, and affects cytochrome P450-dependent enzymes only at micromolar concentrations. PAP-1 potently inhibits the proliferation of human TEM cells and suppresses delayed type hypersensitivity, a TEM cell-mediated reaction, in rats [1]. When administered intravenously, PAP-1 showed a half-life of 6.4 hrs; the volume of distribution suggested extensive distribution into extravascular compartments. When orally administered, PAP-1 was efficiently absorbed. Plasma concentrations in RM undergoing a 30-day, chronic dosing study indicated that PAP-1 levels suppressive to TEMs in vitro can be achieved and maintained in vivo at a non-toxic dose [2]. |
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