2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. PDE7A-IN-1

PDE7A-IN-1 is an orally active and selective PDE7A inhibitor with an IC50 of 0.0037 μM against PDE7A. PDE7A-IN-1 shows excellent isozyme selectivity over PDE7B. PDE7A-IN-1 elevates intracellular cAMP levels, suppresses ECR5 enhancer activity and reduces sclerostin expression. PDE7A-IN-1 significantly increases bone mineral density in rats. PDE7A-IN-1 can be used for the study of osteoporosis.

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

PDE7A-IN-1

PDE7A-IN-1 Chemical Structure

CAS No. : 3074559-75-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

PDE7A-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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Description

PDE7A-IN-1 is an orally active and selective PDE7A inhibitor with an IC50 of 0.0037 μM against PDE7A. PDE7A-IN-1 shows excellent isozyme selectivity over PDE7B. PDE7A-IN-1 elevates intracellular cAMP levels, suppresses ECR5 enhancer activity and reduces sclerostin expression. PDE7A-IN-1 significantly increases bone mineral density in rats. PDE7A-IN-1 can be used for the study of osteoporosis[1].

IC50 & Target[1]

PDE7A

3.7 nM (IC50)

PDE7B

0.2 μM (IC50)

PDE4D

1.6 μM (IC50)

In Vitro

PDE7A-IN-1 (compound 26) potently inhibits recombinant PDE7A with an IC50 of 0.0037 μM, displays 54-fold selectivity over recombinant PDE7B, inhibits recombinant PDE4D with an IC50 of 1.6 μM, and also suppresses ECR5 enhancer activity in UMR106 cells with an IC50 of 0.39 μM[1].
PDE7A-IN-1 (10 min) shows 78% remaining compound in human liver microsomes and 28% remaining compound in rat liver microsomes[1].

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

PDE7A-IN-1 Related Antibodies
Parmacokinetics
Species Dose Route MRT CLtotal Vdss AUC T1/2 F
Rat[1] 0.3 mg/kg i.v. 1.0 h 1.4 L/h/kg 1.4 L/kg / / /
Rat[1] 3 mg/kg p.o. / / / 1.4 μM·h 2.3 h 30 %
In Vivo

PDE7A-IN-1 (compound 26) (3-30 mg/kg; p.o.; 1 month) dose-dependently suppresses serum sclerostin levels and increases bone mineral density in Sprague-Dawley rats[1].

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

463.96

Formula

C25H26ClN5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1N(CC)C(N[C@H]2CN(C(C3=NC=C(C4=CC=CC=C4)C=C3)=O)CC2)=NC(C5CC5)=C1Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (215.54 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1554 mL 10.7768 mL 21.5536 mL
5 mM 0.4311 mL 2.1554 mL 4.3107 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1554 mL 10.7768 mL 21.5536 mL 53.8840 mL
5 mM 0.4311 mL 2.1554 mL 4.3107 mL 10.7768 mL
10 mM 0.2155 mL 1.0777 mL 2.1554 mL 5.3884 mL
15 mM 0.1437 mL 0.7185 mL 1.4369 mL 3.5923 mL
20 mM 0.1078 mL 0.5388 mL 1.0777 mL 2.6942 mL
25 mM 0.0862 mL 0.4311 mL 0.8621 mL 2.1554 mL
30 mM 0.0718 mL 0.3592 mL 0.7185 mL 1.7961 mL
40 mM 0.0539 mL 0.2694 mL 0.5388 mL 1.3471 mL
50 mM 0.0431 mL 0.2155 mL 0.4311 mL 1.0777 mL
60 mM 0.0359 mL 0.1796 mL 0.3592 mL 0.8981 mL
80 mM 0.0269 mL 0.1347 mL 0.2694 mL 0.6735 mL
100 mM 0.0216 mL 0.1078 mL 0.2155 mL 0.5388 mL
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PDE7A-IN-1 Related Classifications

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:

PDE7A-IN-13074559-75-1Phosphodiesterase (PDE)sclerostinrat liver microsomesbone mineral densityPDE7Bhuman liver microsomesSprague-Dawley ratsPDE7AosteoporosisUMR106 cellsphosphodiesterase 7AInhibitorinhibitorinhibit

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