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製品番号: 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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 2358754-27-3
分子式: C₂₃H₂₆N₂O₃
分子量:378.46

保管条件:

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

PDE4-IN-2 構造式

CAS 番号: 2358754-27-3

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target

^[1]

hPDE4D

0.24 μM (IC₅₀)

PDE10A

0.92 μM (IC₅₀)

PDE6C

3.3 μM (IC₅₀)

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示 :

TNF Receptor アイソフォーム固有の製品をすべて表示 :

Interleukin Related アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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 %

体内実験

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 :

化学情報

CAS 番号 2358754-27-3
分子量 378.46
分子式 C₂₃H₂₆N₂O₃
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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PDE4-IN-2

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示

TNF Receptor アイソフォーム固有の製品をすべて表示

Interleukin Related アイソフォーム固有の製品をすべて表示