PDE
| 货号 | 产品名 | CAS号 | 信息 |
|---|---|---|---|
| FB12414 | YM 976 | 191219-80-4 | YM976 is an orally active PDE4 inhibitor (IC50 = 2.2 nM). YM976 has low emetogenic activity, suggested to be due to poor brain penetration. |
| FB17213 | THPP-1 | 1257051-63-0 | THPP-1 is a potent and selective PDE10A inhibitor with IC50 value of 1-1.3nM. It demonstrates excellent pharmacokinetic properties in multiple preclinical animal species. It has the potential to impact multiple symptomatic domains of schizophrenia including positive symptoms and cognitive impairment. |
| FB12711 | TC-E 5005 | 959705-64-7 | TC-E 5005 is a selective PDE10A inhibitor. |
| FB11274 | TAK-915 | 1476727-50-0 | TAK-915 is a highly potent, selective, and brain-penetrating phosphodiesterase 2A inhibitor with an IC50 of 0.61 nM, potential for the treatment of cognitive disorders. |
| FB12698 | T 0156 HCl | 324572-93-2 | T 0156 hydrochloride is a potent and selective inhibitor of phosphodiesterase type 5 (PDE5). It is more selective than sildenafil (IC50 values are 0.23, 56 and > 63000 nM for T 0156 and 3.6, 29 and > 270 nM for sildenafil at PDE5, PDE6 and PDEs 1 - 4 respectively). T 0156 hydrochloride is selective over 30 other enzymes and receptors (IC50 > 10 mM) and potentiates electrical field stimulation-induced relaxation of isolated rabbit corpus cavernosum. |
| FB12657 | Siguazodan | 115344-47-3 | Siguazodan is a selective phosphodiesterase inhibitor with anti-platelet action properties. |
| FB11208 | Roflupram | 1093412-18-0 | Roflupram is a phosphodiesterase 4 inhibitior which suppresses inflammasome activation through autophagy in microglial cells. |
| FB13148 | Roflumilast N-oxide | 292135-78-5 | Roflumilast N-oxide, an active metabolite of roflumilast, is an inhibitor of phosphodiesterase 4 (PDE4). It can be combined with formoterol to enhance the antiinflammatory effect of dexamethasone. |
| FB12635 | Ro 20-1724 | 29925-17-5 | Ro20-1724 is a widely used inhibitor of cyclic nucleotide phosphodiesterase, selective for PDE4 (IC50 = 2.0 μM) |
| FB20355 | Quazinone | 70018-51-8 | Quazinone, is a phosphodiesterase 3 (PDE3) inhibitor and novel cardiotonic agent with vasodilating properties. |
| FB12631 | RS 25344 HCl | 152815-28-6 | Potent PDE4 inhibitor |
| FB12391 | Piclamilast | 144035-83-6 | Piclamilast is a potent and selective inhibitor of phosphodiesterase (PDE) 4. |
| FB11178 | PF-05085727 | 1415637-72-7 | PF-05085727 is a potent, selective, and brain penetrant phosphodiesterase 2A inhibitor to potentiate NMDA signaling and their further development for clinical cognition indications. |
| FB12504 | PF 05180999 | 1394033-54-5 | PF 05180999 is a potent and selective PDE2A inhibitor with IC50 of 1 nM. |
| FB12502 | PF 04449613 | 1236858-52-8 | PF 04449613 is a potent PDE9 inhibitor IC50 of 22 nM. |
| FB10809 | PDE5 Inhibitor C2 | 2109805-65-2 | PDE5 inhibitor C2, a chromeno[2,3-c]pyrrol-9(2H)-one derivate, is a selective and orally bioavailable phosphodiesterase 5 inhibitor for the treatment of pulmonary arterial hypertension. |
| FB12069 | PAT-505 | 1782070-22-7 | PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouse plasma. |
| FB17745 | Oglemilast (sodium) | 778576-63-9 | Oglemilast is a potent and orally active PDE4 inhibitor with IC50 value of 0.5nM for PDE4D3. |
| FB17942 | N-Methylbenzamide | 613-93-4 | N-Methylbenzamide is a potent phosphodiesterase 10A (PDE10A) inhibitor. N-Methylbenzamide has anti-cancer activity. |
| FB12410 | MY-5445 | 78351-75-4 | MY-5445 is a specific inhibitor of cyclic GMP phosphodiesterase 5 with IC50 of 0.5 μM. |
| FB12469 | MMPX | 78033-08-6 | MMPX is a specific inhibitor of calmodulin-sensitive cyclic GMP phosphodiesterase 1 with IC50 of 5.2 μM. |
| FB16045 | Lotamilast | 947620-48-6 | Lotamilast (RVT-501; E6005) is a selective phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.8 nM. |
| FB17744 | K-Ras-PDEδ-IN-1 | 1841464-21-8 | K-Ras-PDEδ-IN-1 is a potent K-Ras-PDEδ inhibitor. It can bind to the farnesyl binding pocket of PDEδ with a low nanomolar Kd of 8 nM. |
| FB12530 | ICI 63197 | 27277-00-5 | ICI 63197 is a potent phosphodiesterase (PDE) 4 inhibitor with antidepressant effects. |
| FB11781 | ICI 153110 | 87164-90-7 | ICI 153110 is an orally active phosphodiesterase inhibitor with both vasodilating and inotropic properties which is designed for the treatment of congestive cardiac failure. |
| FB07587 | Hesperetin | 520-33-2 | Hesperetin is a flavanone extracted from the peel of citrus that exhibits inhibition of PDE4 and UGT. Hesperetin has antioxidative and anti-inflammatory effects as well. Hesperetin dose-dependently inhibited cleavage activity of the 3CLpro with IC50 value of 8.3μM in the cell-based assay. |
| FB10910 | GW4869 2HCl | 6823-69-4 | GW4869 2HCl is a cell permeable, selective and non-competitve inhibitor of N-SMase (neutral sphingomyelinase), which is important in the metabolism of sphingomyelin producing ceramide and phosphocholine and in cell signaling and regulation. GW4869 is an exosome inhibitor. |
| FB10941 | GLPG1690 | 1628260-79-6 | GLPG1690, a first-in-class autotaxin (ATX) inhibitor with IC50 of 131 nM and Ki of 15 nMl, is able to cause a sustained reduction of LPA levels in plasma in vivo and was shown to be efficacious in a bleomycin-induced pulmonary fibrosis model in mice, and in reducing extra-cellular matrix deposition in the lung whilst also reducing LPA 18:2 content in bronchoalveolar lavage fluid and may be a possible effectvie compound in treating idiopathic pulmonary fibrosis. |
| FB12181 | Gisadenafil Besylate | 334827-98-4 | Gisadenafil Besylate is a potent PDE5 inhibitor with IC50 of 1.23 nM. |
| FB12329 | Etazolate HCl | 35838-58-5 | Etazolate HCl is an inhibitor of Phosphodiesterase 4 with IC50 of 2.0 μM. |
| FB12159 | Enoximone | 77671-31-9 | Enoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibits PDE4 inhibitory effect with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects. |
| FB12304 | Eggmanone | 505068-32-6 | Eggmanone is a potent and selective phosphodiesterase (PDE) 4 inhibitor with IC50 of 72 nM. |
| FB17546 | DSR-141562 | 2007975-22-4 | DSR-141562 is a novel orally available and brain-penetrant PDE 1 inhibitor. It has preferential selectivity for predominantly brain-expressed PDE1B over other PDE1 family members, and high selectivity for the PDE1 family over other PDE families and 65 other tested biologic targets. |
| FB15396 | D 159687 | 1155877-97-6 | D 159687 is selective inhibitor of PDE4B and PDE4D with brain permeability. |
| FB17561 | CP-671,305 | 445295-04-5 | CP-671,305 is a potent and selective PDE4D inhibitor. |
| FB12236 | CP 80633 | 135637-46-6 | CP 80633 is a selective inhibitor of phosphodiesterase type 4 with IC50 of 1.9 μM for human lung PDE4. |
| FB04330 | Citreorosein | 481-73-2 | Citreorosein, a cAMP phosphodiesterase inhibitor isolated and purified from the root and rhizome of Rheum palmatum L., has anti-inflammatory effect, inhibits proinflammatory cytokines production through the inhibition of both MAPKs and AKT-mediated IκB kinase (IKK) phosphorylation and subsequent inhibition of transcription factor NF-κB activation. |
| FB12576 | Cilostamide | 68550-75-4 | Cilostamide is a selective inhibitor of type III phosphodiesterase (PDE3). |
| FB11822 | CI-1044 | 197894-84-1 | CI-1044 is an orally active PDE4 inhibitor with IC50s of 0.29, 0.08, 0.56, 0.09 μM for PDE4A5, PDE4B2, PDE4C2 and PDE4D3, respectively. |
| FB11199 | CHF-6001 | 1239278-59-1 | CHF-6001 is a PDE4 inhibitor designed for treating pulmonary inflammatory diseases via inhaled administration. |
| FB12222 | CDP 840 HCl | 162542-90-7 | CDP 840 HCl is a potent and selective inhibitor of phosphodiesterase (PDE) 4 with IC50 of 12 nM. |
| FB08668 | BRL50481 | 433695-36-4 | BRL-50481 is an inhibitor of PDE7 with IC50 of 0.15 μM and can also inihibt PDE7A, PDE7B, PDE4 and PDE3. BRL-50481 has been shown to increase mineralisation activity in osteoblasts thus has the potential treatment of osteoporosis. |
| FB16552 | BIO-32546 | 1548743-66-3 | BIO-32546 is a novel modulator of the activity of the autotaxin (ATX) enzyme. |
| FB16776 | BI-409306 | 1189767-28-9 | BI-409306 is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM, and shows weak activity against other PDEs, such as PDE1A (IC50, 1.4 µM), PDE1C (IC50, 1.0 µM), PDE2A, PDE3A, PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC50 all > 10 μM). BI-409306 can be used in the research of memory enhancement in CNS disorders. It is currently being investigated in clinical trials. |
| FB12218 | BC 11-38 | 686770-80-9 | BC 11-38 is a selective phosphodiesterase (PDE) 11 inhibitor with IC50 of 0.28 μM. |
| FB15528 | BAY 73-6691 | 794568-92-6 | BAY 73-6691 is a potent, selective brain penetrant PDE9A inhibitor. |
| FB18213 | ATX inhibitor 1 | 2225892-70-4 | ATX inhibitor 1 is a potent Autotaxin (ATX) with IC50 values of 1.23nM, 2.18nM and 135nM for FS-3, bis-pNPP, human plasma and LPC cell assays, respectively. |
| FB01238 | AN2898 | 906673-33-4 | AN-2898 is a potent and selective PDE4 inhibitor potentially for the treatment of fungal infection. |
| FB11957 | AMG 579 | 1227067-61-9 | AMG 579 is a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A) with an IC50 of 0.1 nM. |
| FB12213 | (S)-C33 | 2066488-39-7 | (S)-C33 is a potent PDE9 inhibitor with IC50 of 11 nM. |