1. Metabolic Enzyme/Protease
    Neuronal Signaling
  2. FAAH
  3. URB937

URB937 

Cat. No.: HY-116477 Purity: 99.86%
Handling Instructions

URB937 is an orally active and peripherally restricted FAAH inhibitor (IC50=26.8 nM) and increases anandamide levels. URB937 fails to affect FAAH activity in the brain (not penetrate the blood-brain barrier).

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

URB937 Chemical Structure

URB937 Chemical Structure

CAS No. : 1357160-72-5

Size Price Stock Quantity
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 170 In-stock
Estimated Time of Arrival: December 31
50 mg USD 510 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

URB937 is an orally active and peripherally restricted FAAH inhibitor (IC50=26.8 nM) and increases anandamide levels. URB937 fails to affect FAAH activity in the brain (not penetrate the blood-brain barrier)[1].

IC50 & Target

IC50: 26.8 nM (FAAH)[1].

In Vitro

URB937 is actively extruded from the CNS by the ATP-binding cassette (ABC) membrane transporter, Abcg2[3].

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

In Vivo

URB937 (1 mg/kg, i.p.) administrated in mice increases anandamide levels in peripheral tissues, but not forebrain or hypothalamus[1].
URB937 (1 mg/kg, s.c.) suppresses pain responses elicited by i.p. injections of acetic acid[1].
URB937 in male rats (an oral dose 3 mg/kg, F = 36%) is absorbed at a moderate rate and displays a peak plasma concentration (Cmax) of 159.47 ng/ml, which was achieved one hour after administration. URB937 exhibits T1/2 of 60 min by an oral dose of 3 mg/kg[2].
URB937 produces a high degree of antinociception in female mice and rats in models of visceral and inflammatory pain. Moreover, the compound displayed a restricted access to placental and fetal tissues in pregnant mice and rats[3].
URB937 (1 mg/kg, every 2 days for 30 days) attenuates radiation-induced lung injury and increased endocannabinoid concentration in lung tissue[4].

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

Animal Model: Swiss Webster mice[1].
Dosage: 1 mg/kg.
Administration: S.C.
Result: Suppressesd pain responses elicited by i.p. injections of acetic acid.
Animal Model: Adult Sprague Dawley male and female rats (250-300 g)[2].
Dosage: 0.3, 1, 3, 10 mg/kg (Pharmacokinetic Analysis).
Administration: Single oral dose.
Result: Inhibited liver FAAH activity with a median effective dose (ED50) of 0.9 mg/kg.
Inhibits FAAH in peripheral tissues and identify a possible biomarker for target engagement.
Molecular Weight

354.40

Formula

C₂₀H₂₂N₂O₄

CAS No.

1357160-72-5

SMILES

O=C(OC1=CC(C2=CC=CC(C(N)=O)=C2)=C(O)C=C1)NC3CCCCC3

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 (705.42 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8217 mL 14.1084 mL 28.2167 mL
5 mM 0.5643 mL 2.8217 mL 5.6433 mL
10 mM 0.2822 mL 1.4108 mL 2.8217 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 (5.87 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.87 mM); Clear solution

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

URB937URB 937URB-937FAAHFatty acid amide hydrolaselowtoxicityOEAInhibitorinhibitorinhibit

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Product Name:
URB937
Cat. No.:
HY-116477
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