Phosphodiesterase (PDE) Inhibitor

K-252d is an indolocarbazole alkaloid found in Nocardiopsis. It is a PKC inhibitor that inhibits PKC isolated from rat brain (IC₅₀=350 nM). It also inhibits calcium- and calmodulin-dependent phosphodiesterase isolated from bovine heart (IC₅₀=46.2 μM).

PF-8380 (Standard) is the analytical standard of PF-8380. This product is intended for research and analytical applications. PF-8380 is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.

S32826 (disodium) (Standard) is the analytical standard of S32826 (disodium). This product is intended for research and analytical applications. S32826 disodium is a potent autotaxin inhibitor, with an IC50 of 8.8 nM. S32826 disodium shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 disodium inhibits LPA release from adipocytes.

Olprinone (Loprinone) Standard is the analytical standard of Olprinone (HY-14254A). This product is intended for research and analytical applications. Olprinone (Loprinone) is a potent and selective phosphodiesterase 3 (PDE3) inhibitor, with IC₅₀ values of 150, 100, 0.35, and 14 μM against PDE1, PDE2, PDE3, and PDE4, respectively. Olprinone exerts comprehensive protective effects including anti-inflammatory, antioxidant, and anti-apoptotic activities by elevating intracellular cAMP levels and inhibiting the NF-κB and MAPK signaling pathways. Olprinone can be used in studies related to lung injury, spinal cord injury, heart failure, myocardial ischemia-reperfusion injury, and cerebral ischemic injury.

Sudachitin is an orally active compound that potently inhibits mouse PDE1C and human PDE4B, with IC₅₀ values of 5.0 μM and 15.0 μM, respectively. Sudachitin upregulates Sirt1 and PGC‑1α expression in skeletal muscle to regulate energy metabolism and promote mitochondrial biogenesis. Sudachitin improves lipid metabolism, glucose tolerance, insulin sensitivity, energy expenditure, and fatty acid β‑oxidation. Sudachitin activates p38MAPK signaling, induces HSP27 phosphorylation and caspase‑dependent apoptosis, and blocks EGF‑driven keratinocyte migration and proliferation. Sudachitin suppresses LPS‑induced TNF‑α, NO, and iNOS expression in macrophages and shows potent anti‑inflammatory activity. Sudachitin can be used for the research of metabolic syndrome, type 2 diabetes, and psoriasis..

Lodenafil (Standard) is the analytical standard of Lodenafil. This product is intended for research and analytical applications. Lodenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).

Cipamfylline is a PDE4 inhibitor that can cause PDE4A4 to accumulate in specific areas of the cell through interaction with the ubiquitin scaffolding protein p62. Cipamfylline can be used in the research of atopic dermatitis.

Cilostazol-d₂ (OPC 13013-d₂) is deuterium labeled Cilostazol. Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC₅₀ of 0.2 μM.

OPB-171775 (Standard) is the analytical standard of OPB-171775 (HY-162730). This product is intended for research and analytical applications. OPB-171775 is an orally active molecular glue. OPB-171775 forms ternary complex with phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). OPB-171775 causes SLFN12 RNase-mediated cell death, activates SLFN12 RNase-associated GCN2 signaling pathway. OPB-171775 exhibits significant efficacy against gastrointestinal stromal tumor.

ONO-6126 is a PDE4 inhibitor that can be used in research for asthma and chronic obstructive pulmonary disease.

Leniquinsin is a phosphodiesterase inhibitor, which is used as a vasodilator.

OPC 3911 is a highly selective inhibitor of cGMP-inhibited cAMP phosphodiesterase (cGI-PDE/PDE3) and a vasodilator, with an IC₅₀ of 0.042 μM against rat cGI-PDE. OPC 3911 upregulates the expression of Osteopontin. OPC 3911 mediates vasodilation of arterial smooth muscle, induces vasodilatory responses in isolated rat arteriovenous tissues, and exhibits additive vasodilatory effects with Isoprenaline (HY-108353) and Forskolin (HY-15371). OPC 3911 can be used in studies related to congestive heart failure and insulin resistance.

Braylin, a coumarin, is a potent phosphodiesterase-4 (PDE4) inhibitor and is involved in anti-inflammatory and immunomodulation, which may serve as a potential target for the study of immunoinflammatory diseases.

RS-25344 hydrochloride (Standard) is the analytical standard of RS-25344 (hydrochloride) (HY-108621). This product is intended for research and analytical applications. RS-25344 hydrochloride is a selective cAMP-phosphodiesterase 4 (PDE 4; PDE IV) inhibitor with an IC₅₀ of 0.28 nM in human lymphocytes. RS-25344 hydrochloride has only weak inhibitory effects on PDE I, II, III (IC₅₀ of >100 μM, 160 μM, 330 μM, respectively). RS-25344 hydrochloride has anti-inflammatory, memory- and cognition enhancing, and antineoplastic effects.

MK-0952 (Standard) is the analytical standard of MK-0952 (HY-11070). This product is intended for research and analytical applications. MK-0952 is a selective and orally active PDE4 inhibitor, with an IC₅₀ of 0.53 nM. MK-0952 has the potential for Alzheimer’s disease study.

Furamidine (dihydrochloride) (Standard) is the analytical standard of Furamidine (dihydrochloride). This product is intended for research and analytical applications. Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent.

Desmethyl thiosildenafil is a phosphodiesterase type 5 (PDE5) inhibitor^[1].

JNJ-10258859 is a potent and selective phosphodiesterase type 5 inhibitor, with a K_i of 0.23 nM. JNJ-10258859 can be used for erectile dysfunction research.

Eurycomanone (Standard) is the analytical standard of Eurycomanone. This product is intended for research and analytical applications. Eurycomanone could increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis.

MMPX is a potent PDE1 inhibitor.