| 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. |
| M28113 | VP3.15 | VP3.15 is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS). |
| M28112 | VP3.15 dihydrobromide | VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 dihydrobromide has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS). |
| M28069 | THPP-1 | THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species. |
| M28059 | Mufemilast | Mufemilast is a phosphodiesterase 4 (PDE4) inhibitor. |
| M27983 | AMG 579 | AMG 579 is a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A) with an IC50 of 0.1 nM. |
| M27861 | Siguazodan | Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM. |
| M27648 | Zardaverine | Zardaverine is an orally active and selective PDE3/4 inhibitor (IC50)=0.58 uM/0.17 uM) with potent bronchodilator activity. Zardaverine also selectively inhibits the proliferation of HCC cells and induces apoptosis and cycle arrest (G0/G1 phase). Zardaverine has good antitumor potential and is effective in both bronchial relaxation and reduction of inflammation in asthma. |
| M25442 | Drotaverine | Drotaverine is a type 4 cyclic nucleotide phosphodiesterase (PDE4) inhibitor, and it is also an L-type voltage-dependent calcium channel (L-VDCC) blocker, Drotaverine blocks the degradation of 3',5'-cyclic adenosine monophosphate. |
| M21352 | Dovramilast | Dovramilast (CC-11050) is a phosphodiesterase 4 (PDE4) inhibitor with oral activity that reduces the inflammatory response and improves Isoniazid-mediated clearance of bacteria from the lung. Dovramilast is used as an adjuvant in tuberculosis studies. |
| M21314 | LEO 39652 | LEO 39652 is a dual-soft PDE4 inhibitor with IC50 values of 1.2 nM for PDE4A, 1.2 nM for PDE4B, 3.0 nM for PDE4C, and 3.8 nM for PDE4D. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used in topical studies of atopic dermatitis. |
| M21275 | ONO-8430506 | ONO-8430506 is a potent autotaxin phosphodiesterase inhibitor with significant oral exposure and low clearance in higher species. |
| M20723 | 3-Methylxanthine | 3-Methylxanthine (3-MX), a 3-alkylxanthine, is an inhibitor of cyclic guanosine monophosphate (GMP) phosphodiesterase (PDE) with IC50 of 920 μM on guinea-pig isolated trachealis muscle. |
| M20701 | BPN14770 | BPN14770 is a selective allosteric inhibitor of phosphodiesterase 4D (PDE4D) with IC50 of 7.8 nM and 7.4 nM for PDE4D7 and PDE4D3, respectively. |
| M20590 | BW-A78U | BW-A78U, an adenine derivative PDE inhibitor, has anticonvulsant activity. |
| M20402 | Mardepodect (PF-2545920) | PF-2545920 is a potent and selective PDE10A inhibitor with IC50 of 0.37 nM, with >1000-fold selectivity over the PDE. |
| M20179 | WAY-388796 | WAY-388796 is a PDE5 inhibitor |
| M19327 | Moracin M | Moracin M is a potent phosphodiesterase-4 (PDE4) inhibitor with IC50 values of 2.9, 4.5, >40, and >100 μM for PDE4D2, PDE4B2, PDE5A1, and PDE9A2, respectively. Moracin M has anti-inflammatory activity. |
| M18283 | Eurycomanone | Eurycomanone could increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis. |
| M14507 | Vardenafil | Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. |
| M14504 | ML-030 | ML-030 is a potent PDE4 inhibitor, with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM for PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2, respectively. |
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