country

Change Language

EN - English
FR - Français
DE - Deutsch
ES - Español
JA - 日本語
KO - 한국어

Country or Region:

United States

Product Name	Size / Unit Price	Qty

Total: USD 0.00 Checkout

製品番号: HY-187425

Copy Link Print Information

PROTAC sEH degrader-5

PROTAC sEH degrader-5 is a highly efficient PROTAC degrader that targets and degrades soluble epoxide hydrolase (sEH) by recruiting cereblon. PROTAC sEH degrader-5 directly inhibits the hydrolase activity of human and mouse sEH, with pIC50 values of 10.36 and 8.41, respectively. PROTAC sEH degrader-5 alleviates LPS (HY-D1056)-induced acute inflammation in vivo. PROTAC sEH degrader-5 can be used in studies related to LPS-induced acute inflammation.
(Pink: Epoxide Hydrolase ligand (HY-113974); Blue: Cereblon ligand (HY-103596); Black: linker).

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: 3123230-60-1
分子式: C₅₃H₇₀N₈O₁₀
分子量:979.17

保管条件:

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

PROTAC sEH degrader-5 構造式

CAS 番号: 3123230-60-1

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
- 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

PROTAC sEH degrader-5 is a highly efficient PROTAC degrader that targets and degrades soluble epoxide hydrolase (sEH) by recruiting cereblon. PROTAC sEH degrader-5 directly inhibits the hydrolase activity of human and mouse sEH, with pIC50 values of 10.36 and 8.41, respectively. PROTAC sEH degrader-5 alleviates LPS (HY-D1056)-induced acute inflammation in vivo. PROTAC sEH degrader-5 can be used in studies related to LPS-induced acute inflammation^[1]. (Pink: Epoxide Hydrolase ligand (HY-113974); Blue: Cereblon ligand (HY-103596); Black: linker).

PROTACs 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
HepG2	DC₅₀	2.9 nM	Degradation of sEH protein in human HepG2 cells assessed via immunoblot after 6 hrs of treatment. Degradation of sEH protein in human HepG2 cells assessed via immunoblot after 6 hrs of treatment.	42469598

体外実験

PROTAC sEH degrader-5 (compound 1d) (0.1-1000 nM; 6-24 h) potently degrades sEH in HepG2 cells via the proteasome pathway, with a DC₅₀ of 2.9 nM, and its activity depends on intact CRBN binding^[1].
PROTAC sEH degrader-5 potently inhibits the hydrolase activity of recombinantly purified human sEH (pIC₅₀ = 10.36) and mouse sEH (pIC₅₀ = 8.41)^[1].
PROTAC sEH degrader-5 (1 μM; 24 h) induces 61.3 ± 4.7% degradation of sEH in HepG2 cells^[1].
sEH degradation induced by PROTAC sEH degrader-5 (100 nM; 24 h) is significantly attenuated by MG132 (HY-13259) (5 μM), whereas Chloroquine (HY-17589A) (5 μM) exerts no obvious effect, indicating that sEH degradation is mediated via the proteasome pathway^[1].
The methylated derivative of PROTAC sEH degrader-5 (100 nM; 6 h) with a modified CRBN-binding moiety fails to effectively reduce sEH protein levels, indicating that an intact CRBN-binding moiety is essential for its sEH-degrading activity^[1].
PROTAC sEH degrader-5 (100 nM; 6 h) significantly degrades sEH in the cytoplasmic fraction of HepG2 cells, while the level of sEH in the peroxisomal fraction shows no obvious change^[1].

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

Western Blot Analysis^[1]

Cell Line:

HepG2 cells
Concentration:

0.1-1000 nM (6 h); 1 μM (24 h); 100 nM (6 h, 24 h with 5 μM MG132 or 5 μM Chloroquine)
Incubation Time:

6 h; 24 h
Result:

Achieved 61.3% degradation of sEH at 1 μM for 24 h.
Significantly reduced sEH protein levels at 100 nM for 6 h.
Showed maximal sEH degradation of 73% with a DC₅₀ value of 2.9 nM in concentration-dependent testing over 6 h.
Attenuated sEH degradation when co-treated with 5 μM MG132, but no impact when co-treated with 5 μM chloroquine.
Methylated derivative with disrupted CRBN binding had no effect on sEH abundance.

Cell Cytotoxicity Assay^[1]

Cell Line:

HepG2 cells
Concentration:

1 μM
Incubation Time:

24 h; 48 h; 72 h
Result:

Showed no evident cytotoxicity.

Real Time qPCR^[1]

Cell Line:

HepG2 cells
Concentration:

1 μM
Incubation Time:

24 h
Result:

Showed no significant difference in relative EPHX2 mRNA expression compared to control or DMSO-treated groups.

Western Blot Analysis^[1]

Cell Line:

HepG2 cells (cytosolic S10 and peroxisomal P10 fractions)
Concentration:

100 nM
Incubation Time:

6 h
Result:

Reduced sEH protein levels in cytosolic (S10) fraction compared to control groups.
Reduced sEH protein levels in peroxisomal (P10) fraction compared to control groups.

Parmacokinetics

Species	Dose	Route	T_max	V_d/F	T_1/2	C_max	AUC_0-∞	MRT
Mice^[1]	10 mg/kg	i.p.	0.50 h	212.2 L	17.9 h	206.1 nM	1271.4 nM·h	10.2 h
Mice^[1]	10 mg/kg	p.o.	1 h	421 L	19 h	89.6 nM	667.8 nM·h	17.4 h

体内実験

PROTAC sEH degrader-5 (compound 1d) (10 mg/kg; i.p.) significantly reduces hepatic sEH protein levels in LPS-induced acute inflammation mouse models^[1].
PROTAC sEH degrader-5 (10 mg/kg; i.p.) reduces LPS-induced inflammatory cell infiltration and focal necrosis in the liver^[1].
PROTAC sEH degrader-5 (10 mg/kg; i.p.) increases plasma levels of sEH upstream epoxy lipid substrates 9 (10)-EpOME, 12 (13)-EpOME, 11 (12)-EET, 14 (15)-EET and 8 (9)-EET, and elevates the ratios of EpOMEs/DiHOMEs and EETs/DiHETs^[1].
PROTAC sEH degrader-5 (10 mg/kg; i.p.) significantly attenuates the LPS-induced upregulation of Il-6, Mcp-1 and Il-10 mRNA expression in the liver^[1].

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

Animal Model:

LPS-induced acute inflammation^[1]
Dosage:

10 mg/kg
Administration:

i.p.; 12 h before LPS; samples collected 6 h after LPS
Result:

Reduced hepatic sEH protein levels.
Attenuated LPS-induced Il-6, Mcp-1, and Il-10 mRNA elevation.
Attenuated hepatic inflammatory cell infiltration and focal necrosis.
Increased plasma epoxy lipid substrates and EpOMEs/DiHOMEs and EETs/DiHETs ratios.

化学情報

CAS 番号 3123230-60-1
分子量 979.17
分子式 C₅₃H₇₀N₈O₁₀
SMILES

O=C(NC12C[C@H](C[C@H](C2)C3)C[C@H]3C1)N[C@H]4CC[C@@H](CC4)OC5=CC=C(C=C5)C(N6CCN(CC6)CC(NCCCCCCCCNC(COC7=CC=CC(C(N8C9C(NC(CC9)=O)=O)=O)=C7C8=O)=O)=O)=O
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]. Yin C, et al. Modular Access to Diverse Soluble Epoxide Hydrolase Degraders as Potential Agents for Alleviating LPS-Induced Acute Inflammation. Journal of medicinal chemistry. 2026 Jul 17.

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

お問い合わせ在庫あり

Other size

お問い合わせ

Amount: USD 0.00

生物活性
- 製品説明
- 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

製品名:
製品番号:
数量:
日本の代理先をお選びください:

製品名:
CAS 番号:
生物種:
純度:
数量:

PROTAC sEH degrader-5

PROTACs アイソフォーム固有の製品をすべて表示