TRPV1 antagonist 10
TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist (IC50 = 33.06 nM), moderate to weak URAT1 (IC50 = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain.
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- Pureté: 98.54%
- CAS No.: 896584-55-7
- Formule: C16H14N2O5
- Masse moléculaire:314.29
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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TRPV1 36.47 nM (IC50) |
TRPV3 >100 μM (IC50) |
TRPV4 >100 μM (IC50) |
TRPA1 >100 μM (IC50) |
TRPM8 6.47 μM (IC50) |
CYP1A2 28.31 μM (IC50) |
CYP2C9 42.85 μM (IC50) |
CYP2C19 9.23 μM (IC50) |
CYP2D6 >100 μM (IC50) |
CYP3A4M 8.73 μM (IC50) |
TRPV1 antagonist 10 (Compound 39) (50 μM, 24 h) shows 60.25% inhibition rate against GLUT9 in UA (1 mM)-treated HEK293T cells[1].
TRPV1 antagonist 10 (0-400 μM, 24-72 h) exhibits higher levels of cytotoxicity on HepG2 and HK2 cells with increasing dose and time of incubation[1].
TRPV1 antagonist 10 (0-100 μM, 3-20 min) shows high metabolic stability in human and rat liver microsomes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 and HK2 cell lines
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Concentration:0-400 μM
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Incubation Time:24 or 72 h incubation
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Result:Exhibited little cytotoxicity in HepG2 cells after 24 h incubation.
Caused significant cytotoxicity at the concentration of 50 μM after 72 h incubation in HepG2 cells.
Led to significant inhibition of cell viability in HK2 cell line at 200 μM and 24 h incubation.
Had slightly less toxicity in both cell lines in comparison to Benzbromaron (HY-B1135).
| Species | Dose | Route | T1/2 | Plasma Concentration | AUC | MRT | Bioavailability | Tmax | Clearance (CL) |
|---|---|---|---|---|---|---|---|---|---|
| Rat | 1 mg/kg | i.v. | 14.38 h | 106.16 ng/mL | 121.54 ng·h/mL | 13.39 h | 100 % | / | / |
| Rat | 3 mg/kg | p.o. | 8.27 h | 37.94 ng/mL | 141.01 ng·h/mL | 8.78 h | 34.4 % | 0.5 h | 0.018993 mg·h/L |
TRPV1 antagonist 10 (10-20 mg/kg, p.o., 21 consecutive days) reduces the uric acid level and improves the renal function at 20 mg/kg in hyperuricemia mice model[1].
TRPV1 antagonist 10 (500 mg/kg, p.o., one single dose) leads to no obvious abnormal behaviors and difference in weight and food intake in healthy Kunming mice[1].
TRPV1 antagonist 10 (100 mg/kg, p.o., every other day for 14 consecutive days) leads to no obvious abnormal behaviors and difference in weight and food intake in healthy Kunming mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Kunming mice, 5% Formalin (injected subcutaneously into the right rear toe)-induced persistent pain model (8 weeks, 22-25 g)[1]
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Dosage:3 mg/kg, 10 mg/kg, 20 mg/kg
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Administration:Oral gavage (p.o.), one single dose
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Result:Showed no obvious anti-nociceptive activity at dose of 3 mg/kg and 10 mg/kg.
Exhibited significantly better analgesic effect with 20 mg/kg dosage in phase I (0-5 min) and phase II (6-45 min) pain.
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Animal Model:Male Kunming hyperuricemia mice model (8 weeks, 22-25 g)[1]
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Dosage:10 mg/kg, 20 mg/kg
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Administration:Oral gavage (p.o.), 21 consecutive days
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Result:Reduced inflammatory cytokines (IL-1β, TNF-α, and IL-6) with both dosages.
Reduced the level of renal interstitial fibrosis after 21 continuous days.
Chemical Information
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CAS No. 896584-55-7
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Appearance Solid
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Masse moléculaire 314.29
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Formule C16H14N2O5
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Color White to off-white
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SMILES
O=C(NC1=CC(OCCO2)=C2C=C1)NC3=CC=C(OCO4)C4=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 70 mg/mL (222.72 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
Pureté et documentation
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Fiche technique (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
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 (sealed storage, away from moisture). 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 | 3.1818 mL | 15.9089 mL | 31.8177 mL | 79.5444 mL |
| 5 mM | 0.6364 mL | 3.1818 mL | 6.3635 mL | 15.9089 mL | |
| 10 mM | 0.3182 mL | 1.5909 mL | 3.1818 mL | 7.9544 mL | |
| 15 mM | 0.2121 mL | 1.0606 mL | 2.1212 mL | 5.3030 mL | |
| 20 mM | 0.1591 mL | 0.7954 mL | 1.5909 mL | 3.9772 mL | |
| 25 mM | 0.1273 mL | 0.6364 mL | 1.2727 mL | 3.1818 mL | |
| 30 mM | 0.1061 mL | 0.5303 mL | 1.0606 mL | 2.6515 mL | |
| 40 mM | 0.0795 mL | 0.3977 mL | 0.7954 mL | 1.9886 mL | |
| 50 mM | 0.0636 mL | 0.3182 mL | 0.6364 mL | 1.5909 mL | |
| 60 mM | 0.0530 mL | 0.2651 mL | 0.5303 mL | 1.3257 mL | |
| 80 mM | 0.0398 mL | 0.1989 mL | 0.3977 mL | 0.9943 mL | |
| 100 mM | 0.0318 mL | 0.1591 mL | 0.3182 mL | 0.7954 mL |
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