1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. Pyributicarb

Pyributicarb (Synonyms: TSH-888)

Cat. No.: HY-111202 Purity: 99.99%
Handling Instructions

Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).

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

Pyributicarb Chemical Structure

Pyributicarb Chemical Structure

CAS No. : 88678-67-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
50 mg USD 90 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR).

IC50 & Target

CYP3A4[1], hPXR[2]

In Vitro

Pyributicarb, a carbamate-type herbicide, is a potent activator of both CYP3A4 gene and human pregnane X receptor (hPXR). Pyributicarb is found to increase the CYP3A4 reporter activity at 0.1 to 1 μM more strongly than typical CYP3A4 inducer rifampicin. Expression of hPXR-siRNA clearly diminishes the Pyributicarb-stimulated CYP3A4 reporter activity in 3-1-10 cells and decreases the endogenous CYP3A4 mRNA levels in HepG2 cells[1]. Pyributicarb induces luciferase transcription via hPXR at low concentrations in the order of 10 nM. The relative potency of Pyributicarb for hPXR is 8.6-fold that of rifampicin (RIF)[2].

In Vivo

Pyributicarb causes enhancement of CYP3A4-derived reporter activity in mouse livers introduced with hPXR by adenovirus[1].

Molecular Weight

330.44

Formula

C₁₈H₂₂N₂O₂S

CAS No.

88678-67-5

SMILES

S=C(OC1=CC=CC(C(C)(C)C)=C1)N(C2=NC(OC)=CC=C2)C

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 (302.63 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0263 mL 15.1313 mL 30.2627 mL
5 mM 0.6053 mL 3.0263 mL 6.0525 mL
10 mM 0.3026 mL 1.5131 mL 3.0263 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: ≥ 2.5 mg/mL (7.57 mM); Clear solution

  • 2.

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

    Solubility: 2.5 mg/mL (7.57 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (7.57 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

HepG2-derived cells stably expressing the CYP3A4 reporter gene (3-1-10 cells) are used in this experiment. The cells are treated with 0.3 to 30 μM Pyributicarb for 48 h. Then reporter activities are determined[1].

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

Animal Administration
[1]

Male ICR mice (5 weeks old) are used and fed standard rodent chow. After 18-h fasting, mice are injected i.v. with adenovirus [4.0 ×109 50% titer culture infectious dose (TCID50)/mouse]. Three days after the infection, vehicle (0.5% methyl cellulose/saline) or Pyributicarb (100 mg/kg/day) is administered p.o. for 2 consecutive days. Animals are killed 20 h after the last dose[1].

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

References
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Product Name:
Pyributicarb
Cat. No.:
HY-111202
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