| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
BIA 10-2474 is a novel, potent, long-acting and reversible inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions. In a recent clinical trial, the drug BIA 10-2474 was responsible for severe adverse events (SAEs), including one death. To date, there has been little reliable information divulged about the potency of BIA 10-2474 at FAAH in the central nervous system. BIA 10-2474 proved to be a potent FAAH inhibitor with IC50s of 50-70 µg/kg (i.p.) in various brain regions. This information may be useful for determining the cause of the SAEs.
| ln Vitro |
ExVivo: It was demonstrated that BIA 10-2474 is a strong FAAH inhibitor in several brain areas, with an IC50 of 50–70 mg/kg (ip). The corresponding IC50 values for the cerebellum, cortex, remainder of the brain, and hypothalamus are 52, 67, and 68 mg/kg, respectively [1].
|
|---|---|
| ln Vivo |
A Phase I clinical trial involving the medication BIA 10-2474 experienced a major adverse event (SAE) in January 2016, which resulted in one death. We'll look for potential reasons why a trial can fail, like off-target effects, dose estimations, unforeseen immunological reactions, species variance, and cumulative dose toxicity [2].
|
| References |
| Molecular Formula |
C16H20N4O2
|
|
|---|---|---|
| Molecular Weight |
300.36
|
|
| Exact Mass |
300.158
|
|
| CAS # |
1233855-46-3
|
|
| Related CAS # |
|
|
| PubChem CID |
46831476
|
|
| Appearance |
White to off-white solid powder
|
|
| Density |
1.3±0.1 g/cm3
|
|
| Boiling Point |
568.3±52.0 °C at 760 mmHg
|
|
| Flash Point |
297.5±30.7 °C
|
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
|
| Index of Refraction |
1.642
|
|
| LogP |
-0.41
|
|
| Hydrogen Bond Donor Count |
0
|
|
| Hydrogen Bond Acceptor Count |
3
|
|
| Rotatable Bond Count |
2
|
|
| Heavy Atom Count |
22
|
|
| Complexity |
386
|
|
| Defined Atom Stereocenter Count |
0
|
|
| InChi Key |
DOWVMJFBDGWVML-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C16H20N4O2/c1-18(14-7-3-2-4-8-14)16(21)19-11-15(17-12-19)13-6-5-9-20(22)10-13/h5-6,9-12,14H,2-4,7-8H2,1H3
|
|
| Chemical Name |
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | 0.3329 mL | 1.6647 mL | 3.3293 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Inhibition of [18F]-DOPP binding to FAAH in rat brain regions by pre-treatment with PF-04457845 (0.1 mg/kg) or BIA 10-2474.J Cereb Blood Flow Metab.2017 Nov;37(11):3635-3639. |
Brain regional inhibition of FAAH by doses of BIA 10-2474 as measured by inhibition of [18F]-DOPP.J Cereb Blood Flow Metab.2017 Nov;37(11):3635-3639. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
