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Cat. No.: HY-128620

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PDE4-IN-2

PDE4-IN-2 is an orally active and selective PDE4D inhibitor with a human IC₅₀ of 0.24 μM. PDE4-IN-2 blocks cAMP hydrolysis, elevates cAMP, and inhibits inflammatory cytokine release. PDE4-IN-2 exhibits higher selectivity for PDE4D over PDE1-3 and PDE5-11. PDE4-IN-2 shows high cell permeability and weak inhibitory effect on hERG. PDE4-IN-2 prevents Imiquimod (HY-B0180)-induced psoriasis-like skin lesions. PDE4-IN-2 can be used in psoriasis-related research.

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

CAS No.: 2358754-27-3
Formula: C₂₃H₂₆N₂O₃
Molecular Weight:378.46

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

PDE4-IN-2 Chemical Structure

CAS No.: 2358754-27-3

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

hPDE4D

0.24 μM (IC₅₀)

PDE10A

0.92 μM (IC₅₀)

PDE6C

3.3 μM (IC₅₀)

All Phosphodiesterase (PDE) Isoforms :

All TNF Receptor Isoforms :

All Interleukin Related Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	>40 μM Compound: 16	Inhibition of human ERG expressed in CHO cells at -80 mV holding potential measured after 3 mins by QPatch automated patch-clamp assay Inhibition of human ERG expressed in CHO cells at -80 mV holding potential measured after 3 mins by QPatch automated patch-clamp assay	[PMID: 31099559]
Sf9	IC₅₀	>50 μM Compound: 16	Inhibition of recombinant human full length N-terminal GST-tagged PDE11A4 expressed in baculovirus infected Sf9 insect cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay Inhibition of recombinant human full length N-terminal GST-tagged PDE11A4 expressed in baculovirus infected Sf9 insect cells using [3H]cAMP as substrate measured after 30 mins by scintillation proximity assay	[PMID: 31099559]
Sf9	IC₅₀	3.3 μM Compound: 16	Inhibition of recombinant human full length N-terminal GST-tagged PDE6C expressed in baculovirus infected Sf9 insect cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay Inhibition of recombinant human full length N-terminal GST-tagged PDE6C expressed in baculovirus infected Sf9 insect cells using [3H]cGMP as substrate measured after 30 mins by scintillation proximity assay	[PMID: 31099559]

In Vitro

Innate ImmunityCytokines & ChemokinesOthers

Innate Immunity

Cytokines & Chemokines

PDE4-IN-2 (compound 16) inhibits TNF-α release from LPS (HY-D1056)-stimulated hPBMCs with an IC₅₀ of 0.65 μM^[1].

Others

PDE4-IN-2 inhibits recombinant human PDE4D with an IC₅₀ of 0.24 μM; it also inhibits PDE10A and PDE6C with IC₅₀ values of 0.92 and 3.3 μM^[1].
PDE4-IN-2 is selective for PDE4D over most PDE subtypes tested and exhibits at least 4-fold selectivity over PDE3 and PDE10^[1].
PDE4-IN-2 (5400 s) exhibits high cellular permeability in vitro, with an efflux ratio of 1.1^[1].
PDE4-IN-2 inhibits hERG with an IC₅₀ > 40 μM^[1].

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

Parmacokinetics

Species	Dose	Route	AUC_0-t	AUC_0-∞	MRT	T_1/2	CL	V_ss	T_max	C_max	F
Rat^[1]	10 mg/kg	i.v.	6213 ng·h/mL	6276 ng·h/mL	0.92 h	0.60 h	1.70 L/h/kg	1.56 L/kg	/	/	/
Rat^[1]	25 mg/kg	p.o.	8388 ng·h/mL	8458 ng·h/mL	2.50 h	0.94 h	/	/	1.33 h	2447 ng/mL	68.3 %

In Vivo

Innate Immunity

PDE4-IN-2 (compound 16) (25 mg/kg; p.o.; once daily; 7 days) effectively prevents Imiquimod (HY-B0180)-induced psoriasis-like skin lesions in mice^[1].
PDE4-IN-2 (2% cream; topical administration; once daily; 7 days) is effective against Imiquimod-induced psoriasis-like skin lesions in mice^[1].

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

Animal Model:

BALB/c (female)^[1]
Dosage:

25 mg/kg
Administration:

p.o.; once daily; 7 days
Result:

An oral administration of this compound with a dose of 25 mg/kg once daily significantly attenuated skin lesion features, improving individual scores for scales, thickness, and erythema, and the cumulative score.

Animal Model:

BALB/c (female)^[1]
Dosage:

2% cream; 62.5 mg
Administration:

topical; once daily; 7 days
Result:

The topical application of this compound yielded significant efficacy in Imiquimod-induced skin inflammation, manifesting with scales, thickness, and erythema, similar to those resulting from oral administration of this compound.

Related Protocols :

Chemical Information

CAS No. 2358754-27-3
Molecular Weight 378.46
Formula C₂₃H₂₆N₂O₃
SMILES

CC1=CC2=C(C=C1)C(CC[C@H]3C(C=C4OC)=C(CCN3C=O)C=C4OC)=CN2
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

Handling Instructions (2659 KB)

References

[1]. Zhang X, et al. Structure-aided identification and optimization of tetrahydro-isoquinolines as novel PDE4 inhibitors leading to discovery of an effective antipsoriasis agent[J]. Journal of Medicinal Chemistry, 2019, 62(11): 5579-5593.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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PDE4-IN-2

All Phosphodiesterase (PDE) Isoforms

All TNF Receptor Isoforms

All Interleukin Related Isoforms