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PDE1-IN-2 is a PDE1 inhibitor extracted from patent WO2016/55618 A1, example 31. PDE1-IN-2 has IC50 values of 6 nM, 140 nM and 164 nM for PDE1C, PDE1B and PDE1A, respectvely. PDE1-IN-2 is developed for the research of neurodegenerative disorders and psychiatric disorders [1].
PDE1-IN-6 (compound 6c) is a selectivity PDE1 inhibitor with the IC50 of 7.5 nM. PDE1-IN-6 significantly inhibits the proliferation and induced cell apoptosis in Acute myelogenous leukemia cells [1].
PDE1-IN-3, compound 4 (WO2019156861), is a selective human phosphodiesterase 1(PDE1) inhibitor. PDE1-IN-3 inhibits PDE4D and PDE6AB with IC50 values of 23.99 μM and 10 μM, respectively [1].
PDE1-IN-4 (compound 2g) is a potent and selective PDE1 (phosphodiesterase-1) inhibitor, with IC50 values of 10, 145, and 354 nM for PDE1C, PDE1A, and PDE1B, respectively. PDE1-IN-4 inhibits myofibroblast differentiation of human lung fibroblasts induced by TGF-β1. PDE1-IN-4 shows anti-fibrosis effects through the regulation of cAMP (3′,5′-cyclic adenosine monophosphate) and cGMP (3′,5′-cyclic guanosine monophosphate). PDE1-IN-4 can be used for idiopathic pulmonary fibrosis (IPF) research [1].
PDE1-IN-5 (Compound 10c) is a selective PDE1C inhibitor (IC50: 15 nM). PDE1-IN-5 has anti- inflammatory activity, and inhibits expression of iNOS, TNF-α, IL-1α, IL-1β, and IL-6 induced by LPS. PDE1-IN-5 has anti-inflammatory bowel disease (IBD) effects in the dextran sodium sulfate (DSS)-Induced colitis mice model. PDE1-IN-5 can be used for research of IBD [1].
PDE11A4-IN-1 (compound 23b) is a potent and selective PDE11A4 inhibitor with an IC50 of 12 nM. PDE11A4-IN-1 show high selectivity for PDE11A4 over PDE1, PDE2, PDE7, PDE8, and PDE9 [1].
PDE1A Human Pre-designed siRNA Set A contains three designed siRNAs for PDE1A gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Pde1a Mouse Pre-designed siRNA Set A contains three designed siRNAs for Pde1a gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
PDE1A Rat Pre-designed siRNA Set A contains three designed siRNAs for PDE1A gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
PDE1B Human Pre-designed siRNA Set A contains three designed siRNAs for PDE1B gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
PDE1C Human Pre-designed siRNA Set A contains three designed siRNAs for PDE1C gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
T-0156 is a potent and selective phosphodiesterase type 5 (PDE5) inhibitor. T-0156 specifically inhibits the hydrolysis of cyclic guanosine monophosphate (cGMP) by PDE5 in a competitive manner (IC50=0.23 nM). T-0156 inhibits PDE6 (IC50=56 nM) and has low potencies against PDE1, PDE2, PDE3, and PDE4 (IC50>10 μM). T-0156 enhances the nitric oxide (NO)/cGMP pathway [1].
ICI-63197 is a phosphodiesterase 3 (PDE3) and PDE4 inhibitor with Ki values of 9 µM and 10 µM, respectively. ICI-63197 is selectivity against PDE1 and PDE2. ICI-63197 has antidepressant effects [1] .
PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11 [1].
DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1(PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia [1] .
Phosphodiesterase (PDE) is an enzyme that can catalyze the hydrolysis of the 3' ring phosphate bond of cyclic nucleotides, and is often used in biochemical research. Phosphodiesterase acts as an important regulator of signal transduction mediated by the second messenger molecules cAMP and cGMP. According to their specificity to cyclic nucleotides, they can also be divided into different types, such as PDE1-PDE11, which also have certain potential in various diseases [1].
Olprinone (Loprinone) is a potent phosphodiesterase (PDE) 3 inhibitor, with IC50s of 150, 100, 0.35 and 14 μM for PDE1, PDE2, PDE3 and PDE4, respectively. Olprinone is used for the research of heart failure due to its positive inotropic and vasodilative effects. Anti-inflammatory activity [1] .
Olprinone (Loprinone) Hydrochloride is a potent phosphodiesterase (PDE) 3 inhibitor, with IC50s of 150, 100, 0.35 and 14 μM for PDE1, PDE2, PDE3 and PDE4, respectively. Olprinone Hydrochloride is used for the research of heart failure due to its positive inotropic and vasodilative effects. Anti-inflammatory activity [1] .
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions [1] .
Roflumilast (APTA-2217) is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions [1] .
BC11-38 is a potent, selective, and biologically active PDE11 inhibitor, with IC50s of 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively. BC11-38 elevates cAMP levels, PKA-mediated ATF-1 phosphorylation, and cortisol production in H295R cells [1].
Roflumilast-d3 is deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
Roflumilast-d4 is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells[1][2].
3-O-Methylquercetin (3-MQ) is a major component from the plant Rhamnus nakaharai and has antiviral activity and potential antiasthmatic efficacy. 3-O-Methylquercetin inhibits total cAMP and cGMP-phosphodiesterase (PDE). The IC50 values of 3-O-Methylquercetin (3-MQ) against PDE1-PDE5 are in the range of 1.6-86.9 μM. 3-O-Methylquercetin is a non-competitive inhibitor of PDE2 and a competitive inhibitor of PDE4 [1].
Roflumilast-d4 N-Oxide is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells[1][2].
Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5(PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 [1]. Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5(PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 [1]. Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
FCPR03 is a potent and selective phosphodiesterase 4 (PDE4) inhibitor with IC50 values of 60 nM, 31 nM and 47 nM for PDE4 catalytic domain, PDE4B1 and PDE4D7, respectively. FCPR03 displays at least 2100-fold selectivity over other PDEs (PDE1-3 and PDE5-11). FCPR03 has anti-inflammatory, neuroprotective and antidepressant-like effects [1] .
Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction[1][2].
Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5(PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]- .
Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5(PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 [1]. Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
Cilomilast (SB-207499) is a potent, selective and orally active inhibitor of Phosphodiesterase 4 (PDE4), with IC50s of ~100 and 120 nM for LPDE4 and HPDE4, respectively. Cilomilast shows selectivity for PDE4 over PDE1, PDE2, PDE3 and PDE5 (IC50=74, 65, >100, and 83 µM, respectively). Cilomilast has anti-inflammatory and immunomodulatory effects and can be used for thr research of asthma and chronic obstructive pulmonary disease (COPD) [1] .
Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis [1] .
Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis [1] .
Mangostanol ((+)-Mangostanol) is a polyoxygenated xanthone mangostanol, which can be isolated from the shell of Garcinia mangostana, and has inhibitory effect on cAMP phosphodiesterase(PDE) .
Osoresnontrine (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); Osoresnontrine can be used in the research of memory enhancement in CNS disorders.
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 [1] .
MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ lacks inhibitory activity toward other PDE isozymes (all IC50s>100 μM). MBCQ dilates coronary arteries via specific inhibition of cGMP-PDE .
Phosphodiesterase (PDE) is an enzyme that can catalyze the hydrolysis of the 3' ring phosphate bond of cyclic nucleotides, and is often used in biochemical research. Phosphodiesterase acts as an important regulator of signal transduction mediated by the second messenger molecules cAMP and cGMP. According to their specificity to cyclic nucleotides, they can also be divided into different types, such as PDE1-PDE11, which also have certain potential in various diseases [1].
Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5(PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 [1]. Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5(PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 [1]. Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
Avanafil (TA-1790) is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis [1] .
Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5(PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]- .
Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis [1] .
Mangostanol ((+)-Mangostanol) is a polyoxygenated xanthone mangostanol, which can be isolated from the shell of Garcinia mangostana, and has inhibitory effect on cAMP phosphodiesterase(PDE) .
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. The total length of PDE1B Protein, Human (sf9, His-GST) is 536 a.a., with molecular weight of ~75 kDa.
Roflumilast-d4 N-Oxide is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells[1][2].
Roflumilast-d3 is deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
Roflumilast-d4 is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells[1][2].
Vardenafil-d5 is deuterium labeled Vardenafil. Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction[1][2].
