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trans-AUCB (Synonyms: t-AUCB)

Cat. No.: HY-113974 Purity: >95.0%
Handling Instructions

trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC50s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity.

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

trans-AUCB Chemical Structure

trans-AUCB Chemical Structure

CAS No. : 885012-33-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 109 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 200 In-stock
Estimated Time of Arrival: December 31
25 mg USD 400 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

trans-AUCB (t-AUCB) is a potent, orally active and selective soluble epoxide hydrolase (sEH) inhibitor with IC50s of 1.3 nM, 8 nM, 8 nM for hsEH, mouse sEH and rat sEH, respectively. trans-AUCB has anti-glioma activity[1][2].

IC50 & Target

IC50: 1.3 nM (hsEH), 8 nM (mouse sEH) and 8 nM (rat sEH)[2]

In Vitro

trans-AUCB (t-AUCB; 25-300 μM; 48 hours) suppresses U251 and U87 cell growth in a dose-dependent manner[1].
trans-AUCB (200 μM; 48 or 96 hours) induces cell-cycle G0/G1 phase arrest in U251 and U87 cells[1].
trans-AUCB (200 μM; 10 min-4 hours) can increase the phosphorylation levels of p65 after 10 min, reaching to peak after 30 min and lasting for at least 2 hours[1].
trans-AUCB (200 μM; 48 hours) suppresses U251 and U87 cell growth by activating NF-jB-p65[1].
trans-AUCB (10 μM; 30 min) efficiently inhibits sEH activities in human glioblastoma cell lines (U251, U87) and human hepatocellular carcinoma cell line (HepG2 cells)[1].

Cell Viability Assay[1]

Cell Line: U251, U87 cells
Concentration: 25, 50, 100, 200, or 300 μM
Incubation Time: 48 hours
Result: Suppressed U251 and U87 cell growth in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: U251, U87 cells
Concentration: 200 μM
Incubation Time: 48 or 96 hours
Result: Induced cell-cycle G0/G1 phase arrest in U251 and U87 cells.

Western Blot Analysis[1]

Cell Line: U251, U87 cells
Concentration: 200 μM
Incubation Time: 10 min, 30 min, 1 hour, 2 hours, or 4 hours
Result: Increased the phosphorylation levels of p65 after 10 min, reached to peak after 30 min and lasted for at least 2 hours.
In Vivo

trans-AUCB (t-AUCB; p.o.; 0.1, 0.5, 1 mg/kg) ameliorates the LPS-induced hypotension in a dose-dependent manner[2].
trans-AUCB (p.o.; 0.1, 0.5, 1 mg/kg) has t1/2 values of 20, 30, 15 min and Cmax values of 30, 100, 150 nmol/L for p.o. of 0.1, 0.5, 1 mg/kg[2].
trans-AUCB (s.c.; 1, 3, 10 mg/kg) has t1/2 values of 60, 85, 75 min and Cmax values of 245, 2700, 3600 nmol/L for s.c. of 1, 3, 10 mg/kg[2].
trans-AUCB (i.v.; 0.1 mg/kg) has t1/2 values of 70 min and 10 hours for distribution (α) and elimination (β) phases. trans-AUCB has a CL of 0.7 L/h•kg and a Vdss was 17 L/kg[2].

Animal Model: Mice (male CFW strain, 7 weeks old, 24-30 g; and male C57BL/6 strain, 8 weeks old, 22-25 g) [2]
Dosage: 0.1, 0.5, 1 mg/kg
Administration: PO
Result: Ameliorated the LPS-induced hypotension in a dose-dependent manner.
Animal Model: Mice (male CFW strain, 7 weeks old, 24-30 g; and male C57BL/6 strain, 8 weeks old, 22-25 g) [2]
Dosage: 0.1, 0.5, 1 mg/kg (Pharmacokinetic Analysis)
Administration: PO
Result: Had t1/2 values of 20, 30, 15 min and Cmax values of 30, 100, 150 nmol/L for p.o. of 0.1, 0.5, 1 mg/kg, respectively.
Molecular Weight

412.52

Formula

C₂₄H₃₂N₂O₄

CAS No.

885012-33-9

SMILES

OC(C(C=C1)=CC=C1O[[email protected]@H](CC2)CC[[email protected]]2NC(NC34C[[email protected]](C5)C[[email protected]](C[[email protected]]5C4)C3)=O)=O

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 : 250 mg/mL (606.03 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4241 mL 12.1206 mL 24.2412 mL
5 mM 0.4848 mL 2.4241 mL 4.8482 mL
10 mM 0.2424 mL 1.2121 mL 2.4241 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.04 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.04 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.04 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

trans-AUCBt-AUCBOthersorallyactivesolubleepoxidehydrolasesEHanti-gliomaactivityInhibitorinhibitorinhibit

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trans-AUCB
Cat. No.:
HY-113974
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