Pexacerfont
Based on 1 Customer Validation
Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1±0.6 nM for human CRF1 receptor.
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 459856-18-9
- Formula: C18H24N6O
- Molecular Weight:340.42
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
IC50: 6.1±0.6 nM (human CRF1 receptor)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| IMR-32 | IC50 |
4.5 nM
Compound: 13-15
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Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cells
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cells
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[PMID: 19361209] |
| IMR-32 | IC50 |
6.1 nM
Compound: 6, BMS-562086
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Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
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[PMID: 21618986] |
| Pituitary gland cell | IC50 |
129 nM
Compound: 13-15
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Antagonist activity at CRF1 receptor in rat pituitary cells assessed as inhibition of CRF-mediated ACTH production
Antagonist activity at CRF1 receptor in rat pituitary cells assessed as inhibition of CRF-mediated ACTH production
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[PMID: 19361209] |
Pexacerfont demonstrates a potent and specific inhibitory effect (IC50=6.1 ± 0.6 nM) toward human CRF1 receptor and has greater than 1000-fold lower affinity (IC50>1000 nM) for the CRF-binding protein and biogenic amine receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 459856-18-9
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Appearance Solid
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Molecular Weight 340.42
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Formula C18H24N6O
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Color White to off-white
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SMILES
CC[C@H](NC1=NC(C)=NC2=C(C3=CC=C(OC)N=C3C)C(C)=NN21)C
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Synonyms
BMS-562086
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 50 mg/mL (146.88 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.34 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Caco-2 cells at passage 50 to 60 are seeded on polycarbonate membranes of 24 well Transwell plates at a density of 60,000 cells/cm2. The cells are cultured for 21 to 25 days in culture medium consisting of Dulbecco's modified Eagle's medium supplemented with 10% fetal bovine serum, 0.5 mM HEPES, 1% nonessential amino acids, 1% L-glutamine, 100 U/mL penicillin-G, and 100 μg/mL streptomycin. Before the permeability studies, apical (AP) and basolateral (BL) media are replaced with transport buffer (Hanks' balanced salt solution supplemented with 2% N, N-dimethylacetamide, pH 7.4). AP to BL permeability study is initiated by replacing the AP medium with the transport buffer containing 25 μM BMS-562086. All permeability experiments are performed at 37°C.Transepithelial electrical resistance (TEER) values are measured to assess cell monolayer integrity. TEER values are obtained both at the beginning and at the end of each experiment. Only wells with TEER values between 400 and 500 Ω/cm2 throughout the experiment are used in the studies. Mannitol (25 or 100 μM) transport experiments are performed in the same manner as other transport experiments. Mannitol served as a probe of the Caco-2 cell monolayer integrity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats[1]
One group of male Sprague-Dawley rats (n=3, 0.34-0.35 kg b.wt.) instrumented with single jugular vein cannulas are designated for oral administration, and a second group of male Sprague-Dawley rats (n=3, 0.34-0.35 kg b.wt.) instrumented with dual jugular vein cannulas are designated for intravenous administration. All rats are fasted for approximately 18 h before use and for 4 h after dosing. Water is provided ad libitum. Pexacerfont (BMS-562086) is administered orally by gavage to three rats at a single dose of 5 mg/kg in 0.5% aqueous methylcellulose. A single intravenous bolus dose of Pexacerfont is administered to three rats at 1 mg/kg in 20% ethanol in saline via the jugular vein cannula. Blood samples (0.2 mL/time point per animal) are collected via the jugular vein cannula for analysis of Pexacerfont at 0, 0.08 (intravenous dose only), 0.17 (intravenous dose only), 0.25, 0.5, 0.75, 1, 2, 4, 8, 12, 24, 48, 72, and 96 h postdose. Plasma is prepared from the blood samples by centrifuging for 10 min at 1000g and 5°C.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9375 mL | 14.6877 mL | 29.3755 mL | 73.4387 mL |
| 5 mM | 0.5875 mL | 2.9375 mL | 5.8751 mL | 14.6877 mL | |
| 10 mM | 0.2938 mL | 1.4688 mL | 2.9375 mL | 7.3439 mL | |
| 15 mM | 0.1958 mL | 0.9792 mL | 1.9584 mL | 4.8959 mL | |
| 20 mM | 0.1469 mL | 0.7344 mL | 1.4688 mL | 3.6719 mL | |
| 25 mM | 0.1175 mL | 0.5875 mL | 1.1750 mL | 2.9375 mL | |
| 30 mM | 0.0979 mL | 0.4896 mL | 0.9792 mL | 2.4480 mL | |
| 40 mM | 0.0734 mL | 0.3672 mL | 0.7344 mL | 1.8360 mL | |
| 50 mM | 0.0588 mL | 0.2938 mL | 0.5875 mL | 1.4688 mL | |
| 60 mM | 0.0490 mL | 0.2448 mL | 0.4896 mL | 1.2240 mL | |
| 80 mM | 0.0367 mL | 0.1836 mL | 0.3672 mL | 0.9180 mL | |
| 100 mM | 0.0294 mL | 0.1469 mL | 0.2938 mL | 0.7344 mL |
Pexacerfont Related Classifications
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