Cat.No. | Name | Information |
---|---|---|
M2030 | Apremilast | Apremilast is a novel, orally available small molecule inhibitor of PDE4 with IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM. |
M6804 | IBMX | IBMX is a pDE inhibitor (non-selective) with IC50 values of 6.5±1.2, 26.3±3.9 and 31.7±5.3 μM for PDE3, 4 and 5 respectively. |
M30131 | NPD-001 | NPD-001 is a potent Trypanosoma brucei phosphodiesterases TbrPDEB1 and TbrPDEB2 inhibitor, with IC50 values of 4 and 3 nM, respectively. NPD-001 also inhibits human PDEs (phosphodiesterases). NPD-001 shows good anti trypanosomal activity, with an IC50 of 80 nM. |
M30119 | Ophiobolin A | Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase, with an IC50 value of 9 μM. Ophiobolin A antimicrobial and anticancer activity. |
M30028 | Amino Tadalafil | Amino Tadalafil is an analog of Tadalafil. Tadalafil is a potent inhibitor of phosphodiesterase 5 (PDE5) with applications in several conditions, including erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction. |
M29740 | Enpp-1-IN-12 | Enpp-1-IN-12 (compound 43) is a potent and orally active ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor, with a Ki of 41 nM. Enpp-1-IN-12 exhibits anti-tumor activity. |
M29620 | PF-07038124 | PF-07038124 is a PDE4 inhibitor with an IC50 of 0.5 nM for PDE4B2. PF-07038124 shows inhibitory activities against IL-13, IL4, and IFNγ (IC50=125, 4.1 1.06 nM, respectively). |
M29544 | TMX-4100 | TMX-4100 is a selective phosphodiesterase 6D (PDE6D) degrader. TMX-4100 shows a high degradation preference for PDE6D with the DC50 values less than 200 nM in MOLT4, Jurkat, and MM.1S cells. TMX-4100 can be used for the research of multiple myeloma. |
M29313 | BI-2545 | BI-2545 is a potent autotaxin (ATX) inhibitor that significantly reduces LPA, with IC50s of 2.2 nM and 3.4 nM for human ATX and rat ATX, respectively. |
M29161 | Mardepodect hydrochloride | Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect hydrochloride can cross the blood-brain barrier. |
M29156 | (S)-C33 | (S)-C33 is a potent and selective PDE9 (phosphodiesterase-9) inhibitor, with an IC50 of 11 nM. (S)-C33 can be used for central nervous system diseases and diabetes research. |
M29145 | PF-06445974 | PF-06445974, a promising positron emission tomography (PET) lead, has exquisite potency at PDE4B with an IC50 <1 nM. The IC50 values are 36, 4.7 and 17 nM for PDE4D, PDE4A and PDE4C, respectively. PF-06445974 has good selectivity over PDE4D, excellent brain permeability, and a high level of specific binding in the "cold tracer" study. |
M29000 | K134 | K134 is a phosphodiesterase 3 (PDE3) inhibitor. The IC50s of K134 toward PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 µM, respectively. |
M28973 | CM-675 | CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer’s disease. |
M28830 | Nortadalafil | Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension. IC50 value: Target: |
M28698 | Autotaxin-IN-1 | Autotaxin-IN-1 is a potent autotaxin inhibitor, which has favorable potency (IC50=2.2 nM), PK properties, and a robust PK/PD relationship. Autotaxin-IN-1 is used in treatment of osteoarthritis pain. |
M28520 | TAK-915 | TAK-915 is a potent, selective, brain-penetrant and orally active phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 0.61 nM. TAK-915 is >4100-fold more selectivity for PDE2A than PDE1A. TAK-915 has the potential for neuropsychiatric and neurodegenerative disorders treatment. |
M28395 | MK-8189 | MK-8189 is a potent, orally active and selective PDE10A inhibitor with a Ki value of 29 pM. MK-8189 can be used in research of schizophrenia. |
M28318 | PF-05180999 | PF-05180999 (PF-999) is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM. |
M28290 | Gemlapodect | Gemlapodect (RO554965) is an inhibitor of phosphodiesterase 10A (PDE10A). Gemlapodect can be used for researching schizophrenia. |
M28251 | Arofylline | Arofylline is a PDE4 inhibitor as a potential research for asthma. |
M28193 | JNJ-42314415 | JNJ-42314415 is a centrally active phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 35 nM and 64 nM for human recombinant PDE10A and rPDE10A, respectively. |
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