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Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclicnucleotidephosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
L-6355 is an Amiodarone (HY-14187) related compound, which inhibits Ca 2+/calmodulin activated cyclicnucleotidephosphodiesterase with an IC50 value of 0.65 μM. L-6355 is promising for research of antiarrhythmic and antianginal agent .
Apremilast-d5 is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclicnucleotidephosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1].
3′,5′-Cyclicnucleotidephosphodiesterase is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
Apremilast (Standard) is the analytical standard of Apremilast. This product is intended for research and analytical applications. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclicnucleotidephosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
2',3'-Cyclic NADP disodium (2',3'-cNADP+; β-Nicotinamide adenine dinucleotide-2',3'-cyclic phosphate) is a substrate for 2',3'-cyclicnucleotide3'-phosphodiesterase (CNP), an enzyme abundant in myelin. It has been used in a coupled enzyme assay to quantify CNP activity. 2',3'-Cyclic NADP disodium (5 μM) increases calcium overload-induced calcium release and prevents calcium-induced swelling in rat brain mitochondria.
Drotaverine hydrochloride is a type 4 cyclicnucleotidephosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine (hydrochloride) exhibits in vivo antispasmodic efficacy without anticholinergic effects.
Phosphodiesterase I (PDE) is an enzyme that can catalyze the hydrolysis of the 3' ring phosphate bond of cyclicnucleotides, and is often used in biochemical research. Phosphodiesterase I acts as an important regulator of signal transduction mediated by the second messenger molecules cAMP and cGMP. According to their specificity to cyclicnucleotides, they can also be divided into different types, such as PDE1-PDE11, which also have certain potential in various diseases .
Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclicnucleotidephosphodiesterase, with an IC50 value of 9 μM. Ophiobolin A antimicrobial and anticancer activity .
Drotaverine-d10 (hydrochloride) is the deuterium labeled Drotaverine hydrochloride. Drotaverine hydrochloride is a type 4 cyclicnucleotidephosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine hydrochloride exhibits in vivo antispasmodic efficacy without anticholinergic effects[1][2].
Amentoflavone hexaacetate is a 3,5-cyclicnucleotidephosphodiesterase inhibitor with antiplatelet aggregation activity. Amentoflavone hexaacetate can inhibit the aggregation of eluted human platelets induced by ADP or collagen. Amentoflavone hexaacetate can also inhibit the cAMP phosphodiesterase activity in human platelets. Amentoflavone hexaacetate can significantly increase the cAMP level of platelets in the presence of prostaglandin E1. Amentoflavone hexaacetate has anti-angiogenic and anti-metastatic effects .
8-OH-cAMP (8-Hydroxy-cAMP) is a polar, membrane-impermeable cyclic adenosine monophosphate analog that is resistant to mammalian cyclicnucleotide-dependent phosphodiesterases. As a polar PKA agonist, 8-OH-cAMP is used to study the role of cAMP in the development and progression of cardiovascular and metabolic diseases .
Phenacaine (Holocaine) is a local agent that can suppress or relieve pain. Phenacaine inhibits the specific calmodulin-dependent stimulation of erythrocyte Ca 2+-ATPase and cyclicnucleotidephosphodiesterases from brain and heart .
Diphylline (Diprophylline) is a potent A1/A2 adenosine receptor antagonist and cyclicnucleotidephosphodiesterase inhibitor. Diphylline, a xanthine derivative, is a bronchodilator and vasodilator agent and has the potential for chronic bronchitis and emphysema .
8-HA-cAMP is a membrane-permeable cAMP analogue and an activator of cAMP-dependent protein kinase and PKA I. 8-HA-cAMP exerts metabolic stability towards mammalian cyclicnucleotide-responsive phosphodiesterases .
Diphylline (Standard) is the analytical standard of Diphylline. This product is intended for research and analytical applications. Diphylline (Diprophylline) is a potent A1/A2 adenosine receptor antagonist and cyclicnucleotidephosphodiesterase inhibitor. Diphylline, a xanthine derivative, is a bronchodilator and vasodilator agent and has the potential for chronic bronchitis and emphysema .
Apremilast-d8 (CC-10004-d8) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclicnucleotidephosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
Apremilast-d3 (CC-10004-d3) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclicnucleotidephosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
CdnP-IN-1 (compound c82) is a potent and selective non-nucleotideMTB CDN PDE (CdnP; Mycobacterium tuberculosiscyclic dinucleotide phosphodiesterase) inhibitor with an IC50 of 18 μM. CdnP-IN-1 does not inhibit the enzymatic activities of three other bacterial CDN PDEs (Yybt, RocR, and GBS-CdnP), a viral CDN PDE (poxin) or mammalian ENPP1 .
EHNA is a potent and selective dual inhibitor of cyclicnucleotidephosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects .
EHNA hydrochloride is a potent and selective dual inhibitor of cyclicnucleotidephosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects .
Rp-8-Br-PET-cGMPS sodium (Rp-8-Bromo-PET-cGMPS) is an analog of cyclic GMP (cGMP). It is a cell permeable, competitive, and reversible inhibitor of cGMP-dependent protein kinases (cGKs) that blocks activation of cGKI and cGKII by cGMP (Kis=35 and 30 nM). It less potently inhibits protein kinase A (Ki=11 μM) and cGMP-induced activation of cyclicnucleotide-gated channels (IC50=25 μM). In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (Ki=1 μM). Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11.
Sp-8-Br-PET-cGMPS is a membrane-permeable PKG agonist and a membrane-permeable inhibitor of retinal-type cGMP-gated ion channels, as well as an activator of cGMP-dependent protein kinases I α and I β. Sp-8-Br-PET-cGMPS is resistant to mammalian cyclicnucleotide-dependent phosphodiesterases, has no metabolic side effects, and is more lipophilic and permeable than Sp-8-pCPT-cGMPS. Sp-8-Br-PET-cGMPS can be used to study the role of cGMP signaling pathways in the nervous system .
Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclicnucleotidephosphodiesterase, with an IC50 value of 9 μM. Ophiobolin A antimicrobial and anticancer activity .
Amentoflavone hexaacetate is a 3,5-cyclicnucleotidephosphodiesterase inhibitor with antiplatelet aggregation activity. Amentoflavone hexaacetate can inhibit the aggregation of eluted human platelets induced by ADP or collagen. Amentoflavone hexaacetate can also inhibit the cAMP phosphodiesterase activity in human platelets. Amentoflavone hexaacetate can significantly increase the cAMP level of platelets in the presence of prostaglandin E1. Amentoflavone hexaacetate has anti-angiogenic and anti-metastatic effects .
PDE1B protein, a cyclic nucleotide phosphodiesterase, displays dual specificity for cAMP and cGMP, essential second messengers in physiological processes. Preferring cGMP as a substrate, PDE1B fine-tunes cellular responses to cyclic nucleotide signaling. Its dual specificity underscores its regulatory role in diverse physiological pathways. PDE1B Protein, Human (sf9, His-GST) is the recombinant human-derived PDE1B protein, expressed by Sf9 insect cells , with N-His, N-GST labeled tag.
Apremilast-d5 is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclicnucleotidephosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM[1].
Drotaverine-d10 (hydrochloride) is the deuterium labeled Drotaverine hydrochloride. Drotaverine hydrochloride is a type 4 cyclicnucleotidephosphodiesterase (PDE4) inhibitor and an L-type voltage-dependent calcium channel (L-VDCC) blocker, blocks the degradation of 3',5'-cyclic adenosine monophosphate. Drotaverine hydrochloride exhibits in vivo antispasmodic efficacy without anticholinergic effects[1][2].
Apremilast-d8 (CC-10004-d8) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclicnucleotidephosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
Apremilast-d3 (CC-10004-d3) is deuterium labeled Apremilast. Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclicnucleotidephosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
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