1. Metabolic Enzyme/Protease
    Neuronal Signaling
    Autophagy
  2. FAAH
    Autophagy
    Mitophagy
  3. URB-597

URB-597 (Synonyms: KDS-4103)

Cat. No.: HY-10864 Purity: 99.01%
Handling Instructions

URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity.

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

URB-597 Chemical Structure

URB-597 Chemical Structure

CAS No. : 546141-08-6

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Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 77 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 70 In-stock
Estimated Time of Arrival: December 31
25 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 400 In-stock
Estimated Time of Arrival: December 31
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Description

URB-597 (KDS-4103) is an orally bioavailable and selective FAAH inhibitor. URB-597 inhibits FAAH activity with an IC50s of approximately 5 nM in rat brain membranes, 0.5 nM in intact rat neurons, 3 nM in human liver microsomes. Antidepressant-like effects. Analgesic activity[1].

In Vitro

URB-597 (KDS-4103) prevents the FAAH-catalyzed hydrolysis of [3H]anandamide by primary cultures of rat cortical neurons with an IC50 value of ~0.50 nM[1].

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

In Vivo

URB-597 (KDS-4103) inhibits rat brain FAAH activity after intraperitoneal (i.p.) administration with a median inhibitory dose (ID50) of 0.15 mg/kg in wild-type mice (+/+) or FAAH-null mice (-/-)[1].
KDS-4103 (0.1-0.3 mg/kg, i.p.) elicits significant, anxiolytic-like, antidepressant-like and analgesic effects, which are prevented by treatment with CB1 receptor antagonists in rats and mice[1].
KDS-4103 is orally available in rats and cynomolgus monkeys[1].
URB-597 inhibits FAAH in the brain rapidly (1 h), sustains at >90% through 12 h and >60% through 24 h after an oral dose of 10 mg/kg.

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

Animal Model: Wistar rats[1]
Dosage: 250, 500, 750, 1000, 1250 mg/kg (Pharmacokinetic Analysis)
Administration: Oral administration
Result: Absorbed at a moderate rate with peak plasma concentrations (Cmax) achieved at 1.2 h after treatment. The oral elimination half-life was approximately 2 h.
Clinical Trial
Molecular Weight

338.40

Formula

C₂₀H₂₂N₂O₃

CAS No.
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 (295.51 mM)

H2O : 0.1 mg/mL (0.30 mM; ultrasonic and warming and heat to 50°C)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9551 mL 14.7754 mL 29.5508 mL
5 mM 0.5910 mL 2.9551 mL 5.9102 mL
10 mM 0.2955 mL 1.4775 mL 2.9551 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: 10 mg/mL (29.55 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (7.39 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (7.39 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
URB-597
Cat. No.:
HY-10864
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