1. Metabolic Enzyme/Protease
    Neuronal Signaling
    Autophagy
  2. FAAH
    Autophagy
  3. BIA 10-2474

BIA 10-2474 

Cat. No.: HY-19740 Purity: 98.41%
Handling Instructions

BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions.

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

BIA 10-2474 Chemical Structure

BIA 10-2474 Chemical Structure

CAS No. : 1233855-46-3

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Estimated Time of Arrival: December 31
10 mg USD 105 In-stock
Estimated Time of Arrival: December 31
50 mg USD 375 In-stock
Estimated Time of Arrival: December 31
100 mg USD 580 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

BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions.

IC50 & Target

IC50: 50-70mg/kg (FAAH, rat brain regions)[1]

In Vitro

ExVivo: BIA 10-2474 proves to be a potent FAAH inhibitor with IC50s of 50-70mg/kg (i.p.) in various brain regions. IC50 values for brain regions are 52 (cerebellum), 67 (rest of brain), 68 (cortex), and 71 mg/kg (hypothalamus)[1].

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

In Vivo

In January 2016, severe adverse events (SAE) occurs in the Phase I clinical trial using the drug BIA 10-2474 including one death. The possibilities for failure of trials such as off-target effect, dose calculation, unexpected immune response, species variation, and cumulative dose toxicity would be sought[2].

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

Molecular Weight

300.36

Formula

C₁₆H₂₀N₄O₂

CAS No.

1233855-46-3

SMILES

O=C(N1C=C(C2=C[N+]([O-])=CC=C2)N=C1)N(C3CCCCC3)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 : 2.2 mg/mL (7.32 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.3293 mL 16.6467 mL 33.2934 mL
5 mM 0.6659 mL 3.3293 mL 6.6587 mL
10 mM --- --- ---
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Rats: Groups of rats (n=4) are pre-treated with BIA 10-2474 (2 mL/kg in 5% Tween 80 in saline i.p.) or with vehicle 40 min prior to radiotracer injection. Rats, in a restraining box, receives 3–4 MBq of high-specific activity [18F]-DOPP in 0.3mL of 10% ethanol in citrate buffer (pH 6) via the tail vein which has been vasodilated in a warm water bath. They are sacrificed by decapitation at 40 min after radiotracer administration, the brain is surgically removed from the skull and stored on ice. Brain regions are excised, blotted, and weighed while blood is collected. Radioactivity in tissues is assayed[1].

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

References
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Keywords:

BIA 10-2474FAAHAutophagyFatty acid amide hydrolaseInhibitorinhibitorinhibit

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BIA 10-2474
Cat. No.:
HY-19740
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