2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. PDE5-IN-13

PDE5-IN-13 inhibits phosphodiesterase 5 (PDE5A) with an IC50 of 3 nM. PDE5-IN-13 is a potential candidate for the treatment of PAH (pulmonary arterial hypertension). PDE5-IN-13 has high selectivity for targets over PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11. PDE5-IN-13 has reasonable drug-like profiles.

For research use only. We do not sell to patients.

PDE5-IN-13 Chemical Structure

PDE5-IN-13 Chemical Structure

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PDE5-IN-13 Related Antibodies

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Description

PDE5-IN-13 inhibits phosphodiesterase 5 (PDE5A) with an IC50 of 3 nM. PDE5-IN-13 is a potential candidate for the treatment of PAH (pulmonary arterial hypertension). PDE5-IN-13 has high selectivity for targets over PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11. PDE5-IN-13 has reasonable drug-like profiles[1].

IC50 & Target[1]

PDE5A

3 nM (IC50)

PDE1C

10478 nM (IC50)

PDE2A

3378 nM (IC50)

PDE3A

>100000 nM (IC50)

PDE4D2

53294 nM (IC50)

PDE6C

20 nM (IC50)

PDE7A

25746 nM (IC50)

PDE8A1

>100000 nM (IC50)

PDE9A2

>100000 nM (IC50)

PDE10A2

21160 nM (IC50)

PDE11A

>100000 nM (IC50)

In Vitro

The C3-cyanide group of PDE5-IN-13 forms hydrogen bond bridges with D764 and H613 through water molecules, which stabilizes the binding conformation of PDE5-IN-13[1].
The [1-(pyridin-2-yl)ethyl] amino side chain at C8-position of PDE5-IN-13 is located near the solvent-exposed region, and the hydrophilic pyridine ring can interact with the solvent region, enhancing inhibitory affinity of PDE5-IN-13[1].
PDE5-IN-13 inhibitor displays weak inhibition against the CYP1A2, CYP2D6, and CYP3A4 with IC50s above 50 μM, and for CYP2C19 and CYP2C9 is 4.63 and 9.76 μM, respectively[1].
PDE5-IN-13 exhibits much weaker inhibitory activity toward hERG channel with an IC50 above 30 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PDE5-IN-13 Related Antibodies
In Vivo

PDE5-IN-13 (1500 mg/kg, p.o.) has no acute toxicity in rice[1].
PDE5-IN-13 (5.0 mg/kg, p.o., daily, 21 days) shows a remarkable increase in mPAP (pulmonary arterial pressure) and decrease in RVHI (right ventricular hypertrophy index) than Sildenafil citrate (HY-15025A) (10.0 mg/kg) in a Monocrotaline (HY-N0750)-induced PAH rat model[1].
In Vivo Pharmacokinetic Properties of PDE5-IN-13.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PK parameters i.v. administration (2 mg/kg) p.o. administration (10mg/kg)
AUC(0-t)(ng/mL・h) 398.9 338.8
AUC (0−∞)(ng/mL・h) 399.0 340.5
AUC (0−t)(h) 0.75 6.3
AUC (0−∞)(h) 0.76 6.4
t1/2 (h) 2.25 2.79
Tmax (h) 0.083 4.0
CL (L/h/kg) 5.0 31.5
Vz (L/kg) 16.3 126.6
Cmax (ng/mL) 985.2 58.4
F (%) 16.8
Molecular Weight

486.56

Formula

C31H26N4O2
SMILES

C[C@@H](NC1=CC=CC(C(C2=CC=C(OC)C=C2)=C3C#N)=C1N(CC4=CC=CC=C4)C3=O)C5=CC=CC=N5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PDE5-IN-13 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PDE5-IN-13Phosphodiesterase (PDE)pulmonary arterial hypertension (PAH)inhibitory activitypharmacodynamicInhibitorinhibitorinhibit

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