4-Bromopyrazole
Based on 1 Customer Validation
4-Bromopyrazole is an orally active alcohol dehydrogenase inhibitor that crosses the blood-brain barrier, with an IC50 of 1 μM. 4-Bromopyrazole inhibits Src, VEGFR2 Y1175, and ERK1/2 phosphorylation, and competitively inhibits octanol oxidation. 4-Bromopyrazole is used in research on alcoholism, triple-negative breast cancer, trichomoniasis, and Meloidogyne incognita infection.
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- Pureza : 99.79%
- No. CAS: 2075-45-8
- Fòrmula: C3H3BrN2
- Peso molecular:146.97
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
|
alcohol dehydrogenase 1 μM (IC50) |
Src |
VEGFR2 |
ERK1 |
ERK2 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
4-Bromopyrazole (11.5 μmoles/mL; administered via drinking water; 11-41 days) decreases hepatic AldDH activity while increasing ADH activity in mice[1].
4-Bromopyrazole (50-400 mg/kg; intraperitoneal injection; once daily for 4 consecutive days or single administration) does not affect brain norepinephrine, dopamine, or 5-hydroxytryptamine levels at any dose or time point tested, but at higher doses produces severe dose-dependent central nervous system depression accompanied by hypothermia and loss of the righting reflex[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Swiss albino male mice (CD Charles River, Massachusetts; 19-27 g)[1]
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Dosage:1.5 m-moles/kg
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Administration:i.p.; single dose
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Result:At 1 hr, hepatic AldDH activity was 87 ± 10% of control and ADH activity was 25 ± 11% of control.
At 3 hr, AldDH was 93 ± 13% and ADH was 20 ± 4% of control.
At 6 hr, AldDH was 78 ± 15% and ADH was 26 ± 6% of control.
At 17 hr, AldDH was 82 ± 23% and ADH was 156 ± 7% of control, indicating apparent elevation of ADH activity.
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Animal Model:C57BL/Cum male mice (20-33 g; Cumberland View Farms, Clinton, Tenn.)[1]
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Dosage:11.5 μmoles/mL
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Administration:ad lib.; 11, 18, or 41 days
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Result:After 11 days, hepatic AldDH activity was 71 ± 10% of control and ADH was 112 ± 7% of control.
After 18 days, AldDH was 72 ± 8% and ADH was 108 ± 19% of control.
After 41 days, AldDH was 67 ± 4% and ADH was 151 ± 8% of control.
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Animal Model:NMRI/BOM (male, 25-35 g)[7]
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Dosage:50, 100, 200 mg/kg (chronic); 50, 100, 200, 400 mg/kg (acute)
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Administration:i.p.; once daily for 4 days (chronic); single dose (acute)
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Result:Did not alter brain noradrenaline levels (0.552-0.591 μg/g vs control 0.588 μg/g) after chronic dosing.
Did not alter brain dopamine levels (1.205-1.307 μg/g) or 5-hydroxytryptamine levels (1.598-1.793 μg/g) after chronic dosing.
Did not alter brain noradrenaline levels (0.547-0.587 μg/g vs control 0.578 μg/g) after acute dosing.
Increased brain dopamine levels at 400 mg/kg (1.274 μg/g vs control 1.109 μg/g).
Induced hypothermia at 90 min post-injection (38.2°C at 50 mg/kg; 36.7°C at 100 mg/kg; 35.3°C at 200 mg/kg; 32.5°C at 400 mg/kg).
Induced hypothermia at 6 hrs post-injection (37.6°C at 50 mg/kg; 37.4°C at 100 mg/kg; 36.4°C at 200 mg/kg; 33.7°C at 400 mg/kg).
Reduced exploratory activity at 30 min (478 counts at 50 mg/kg; 652 counts at 100 mg/kg; 293 counts at 200 mg/kg; 0 counts at 400 mg/kg).
Reduced exploratory activity at 6 hrs (611 counts at 50 mg/kg; 631 counts at 100 mg/kg; 483 counts at 200 mg/kg; 51 counts at 400 mg/kg).
Caused loss of righting reflex at 400 mg/kg (onset 1.3 min; duration 141 min).
Chemical Information
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No. CAS 2075-45-8
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Appearance Solid
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Peso molecular 146.97
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Fòrmula C3H3BrN2
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Color Off-white to light yellow
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SMILES
BrC1=CNN=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 200 mg/mL (1360.82 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)
Pureza y Documentación
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Ficha de datos (355 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 6.8041 mL | 34.0205 mL | 68.0411 mL | 170.1027 mL |
| 5 mM | 1.3608 mL | 6.8041 mL | 13.6082 mL | 34.0205 mL | |
| 10 mM | 0.6804 mL | 3.4021 mL | 6.8041 mL | 17.0103 mL | |
| 15 mM | 0.4536 mL | 2.2680 mL | 4.5361 mL | 11.3402 mL | |
| 20 mM | 0.3402 mL | 1.7010 mL | 3.4021 mL | 8.5051 mL | |
| 25 mM | 0.2722 mL | 1.3608 mL | 2.7216 mL | 6.8041 mL | |
| 30 mM | 0.2268 mL | 1.1340 mL | 2.2680 mL | 5.6701 mL | |
| 40 mM | 0.1701 mL | 0.8505 mL | 1.7010 mL | 4.2526 mL | |
| 50 mM | 0.1361 mL | 0.6804 mL | 1.3608 mL | 3.4021 mL | |
| 60 mM | 0.1134 mL | 0.5670 mL | 1.1340 mL | 2.8350 mL | |
| 80 mM | 0.0851 mL | 0.4253 mL | 0.8505 mL | 2.1263 mL | |
| 100 mM | 0.0680 mL | 0.3402 mL | 0.6804 mL | 1.7010 mL |
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