Verucerfont
Based on 1 Customer Validation
Verucerfont is a corticotropin-releasing factor receptor 1 (CRF1) antagonist with IC50s of ~6.1, >1000 and >1000?nM for CRF1, CRF2, and CRF-BP, respectively.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 885220-61-1
- Formula: C22H26N6O2
- Molecular Weight:406.48
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
|
CRFR1 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 885220-61-1
-
Appearance Solid
-
Molecular Weight 406.48
-
Formula C22H26N6O2
-
Color White to off-white
-
SMILES
CC[C@H](NC1=CC(C)=NC2=C(C3=CC=C(OC)C=C3C)C(C)=NN12)C4=NC(C)=NO4
-
Synonyms
GSK561679
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 83.33 mg/mL (205.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
Male Sprague-Dawley rats are received at 175 to 200 g and housed in a 12 to 12 light cycle for 1 week before adrenalectomy. Rats are adrenalectomized at Neurocrine Biosciences, and NaCl is replenished. Adrenalectomy is verified by plasma corticosterone measurements. Seven days after adrenalectomy, rats are implanted with femoral vein catheters. After ~4 days, rats are prepared for blood sampling by attaching their catheters to PE50 tubing and a syringe, and acclimated to individual opaque sampling cages for 1 h. These cages allow sampling to occur without disturbance to the rat. Blood samples (0.3 mL) are taken after acclimation and blood volumes are replaced with 5 U/mL heparinized saline. Blood samples are stored on ice with EDTA. After a baseline blood sample, rats receive oral doses of either vehicle at 5 mL/kg or the respective drug (including Verucerfont) in the same volume of vehicle. In each case, the dose is 10 mg/kg, based on prior pharmacokinetic studies showing that this dose results in adequate and comparable exposure. Blood samples are taken 1, 2, 3, 4, and 6 h later. Plasma is separated by centrifugation at 4°C and stored at -80 °C for subsequent measurement of ACTH by radioimmunoassay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (279 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4601 mL | 12.3007 mL | 24.6015 mL | 61.5036 mL |
| 5 mM | 0.4920 mL | 2.4601 mL | 4.9203 mL | 12.3007 mL | |
| 10 mM | 0.2460 mL | 1.2301 mL | 2.4601 mL | 6.1504 mL | |
| 15 mM | 0.1640 mL | 0.8200 mL | 1.6401 mL | 4.1002 mL | |
| 20 mM | 0.1230 mL | 0.6150 mL | 1.2301 mL | 3.0752 mL | |
| 25 mM | 0.0984 mL | 0.4920 mL | 0.9841 mL | 2.4601 mL | |
| 30 mM | 0.0820 mL | 0.4100 mL | 0.8200 mL | 2.0501 mL | |
| 40 mM | 0.0615 mL | 0.3075 mL | 0.6150 mL | 1.5376 mL | |
| 50 mM | 0.0492 mL | 0.2460 mL | 0.4920 mL | 1.2301 mL | |
| 60 mM | 0.0410 mL | 0.2050 mL | 0.4100 mL | 1.0251 mL | |
| 80 mM | 0.0308 mL | 0.1538 mL | 0.3075 mL | 0.7688 mL | |
| 100 mM | 0.0246 mL | 0.1230 mL | 0.2460 mL | 0.6150 mL |