Trpvicin
Based on 1 Customer Validation
Trpvicin is a potent and subtype-selective TRPV3 inhibitor with IC50s of 0.41 and 0.22 μM for hTRPV3-WT and hTRPV3-G573S mutant, respectively. Trpvicin exhibits minimal effects on other TRP family members (such as TRPV1/2/4/5/6, TRPA1 and TRPM8). Trpvicin inhibits the TRPV3 channel by stabilizing it in a closed state via VSLD-PD binding. Trpvicin accesses additional binding sites inside the central cavity of the G573S mutant to remodel symmetry and block the channel. Trpvicin inhibits itch and hair loss in mouse models. Trpvicin can be used for study of inflammation and immunology.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.45%
- CAS. Nr.: 2019994-90-0
- Formel: C20H17F3N6O3S
- Molecular Weight:478.45
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Speicherung: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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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
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Help & FAQs
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Immunology/Inflammation Compound Library
HY-L007
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Highly Selective Inhibitors Library
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High-Throughput Bioactive Compound Library
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Biologische Aktivität
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TRPV3 |
Trpvicin (0-100 μM) dose-dependently inhibits the currents of TRPV3-WT and hTRPV3-G573S expressed in HEK293T cells, achieving nearly complete inhibition at 10 μM, with potency comparable to Ruthenium Red (HY-103311)[1].
Trpvicin (10 μM, 24 h) rescues the cell viability of HEK293T cells expressing the cytotoxic hTRPV3-G573S mutant, demonstrating its functional blockade of the constitutively active channel[1].
Trpvicin (0-100 μM) dose-dependently inhibits the currents of hTRPV3-G568V and mTRPV3-G568V heterologously expressed in HEK293T cells[1].
Trpvicin potently inhibits both wild-type mouse TRPV3 (mTRPV3-WT) and the gain-of-function mutant mTRPV3-G568V heterologously expressed in HEK293T cells, with IC50 values of 0.38 μM and 0.42 μM, respectively[1].
Trpvicin exhibits a dramatic loss in potency (158-, 162-, and 208-fold) against the hTRPV3 A556V, A560T, and F601A mutants compared to the wild-type channel, suggesting that these residues are the key determinants for Trpvicin binding[1].
Trpvicin exhibits a 17-fold, 12-fold, and 16-fold decrease in potency against hTRPV3-G573S-F666A, hTRPV3-G573S-F666Y and hTRPV3-G573S-T665A double mutants, respectively, suggesting that these residues are functionally important for drug binding in the central cavity, beyond its primary VSLD-PD binding site[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Rescued the cell viability of HEK293T cells expressing the cytotoxic hTRPV3-G573S mutant.
| Species | Dose | Route | Note | T1/2 | Tmax | Cmax | AUC0-t | AUC0-inf | MRT0-inf | F | CL | Vz |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 8-week-old male CD-1 mice | 10.96 h | 0.139 h | 1553 ng/mL | 11633 ng·h/mL | 12146 ng·h/mL | 13.61 h | 50.15 % | / | / |
| Mice[1] | 2.5 mg/kg | i.v. | 8-week-old male CD-1 mice | 0.80 h | / | 1523 ng/mL | 5970 ng·h/mL | 6083 ng·h/mL | 9.28 h | / | 0.00042 L/h/kg | 0.00547 L/kg |
Trpvicin (30 and 100 mg/kg, p.o., daily starting from 5 days before MC903 for 12 days) alleviates chronic scratching and ear swelling in an MC903 (HY-10001)-induced dermatitis mice model[1].
Trpvicin (1 wt%, topically, daily from postnatal day 50 for 16 days) effectively rescues hair loss in both male and female Trpv3+/G568V knock-in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult wild-type male C57BL/6J mice (8-12 weeks old) topically treated with 20 μL of 100 μM MC903 on both ears, daily for 7 days[1]
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Dosage:30 and 100 mg/kg
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Administration:p.o., daily starting from 5 days before MC903 for 12 days
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Result:Reduced the scratching behavior at a dose of 100 mg/kg, compared to the vehicle-treated control mice in the MC903-induced chronic itch model.
Reduced the percentage of ear thickness increase induced by MC903.
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Animal Model:Adult wild-type male C57BL/6J mice (8-12 weeks old) intradermally injected with SLIGRL (50 µg)[1]
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Dosage:10 and 100 µM
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Administration:i.d., 30 min pre-SLIGRL
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Result:Exhibited fewer scratching bouts elicited by SLIGRL at both 10 and 100 µM.
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Animal Model:Trpv3+/G568V knock-in mice[1]
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Dosage:1 wt%
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Administration:topically, daily from postnatal day 50 (P50) for 16 days
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Result:Showed substantially longer hair shafts and less hair shedding throughout the period.
Demonstrated efficacy in rescuing hair loss in both male and female mouse models.
Chemical Information
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CAS. Nr. 2019994-90-0
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Appearance Solid
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Molecular Weight 478.45
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Formel C20H17F3N6O3S
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Color White to off-white
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SMILES
N#CC(C)(C)C1=NC=CC(C2=C(C(F)(F)F)N=C(NC(C3=C(OC)N=CN=C3OC)=O)S2)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 25 mg/mL (52.25 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 2.0901 mL | 10.4504 mL | 20.9008 mL | 52.2521 mL |
| 5 mM | 0.4180 mL | 2.0901 mL | 4.1802 mL | 10.4504 mL | |
| 10 mM | 0.2090 mL | 1.0450 mL | 2.0901 mL | 5.2252 mL | |
| 15 mM | 0.1393 mL | 0.6967 mL | 1.3934 mL | 3.4835 mL | |
| 20 mM | 0.1045 mL | 0.5225 mL | 1.0450 mL | 2.6126 mL | |
| 25 mM | 0.0836 mL | 0.4180 mL | 0.8360 mL | 2.0901 mL | |
| 30 mM | 0.0697 mL | 0.3483 mL | 0.6967 mL | 1.7417 mL | |
| 40 mM | 0.0523 mL | 0.2613 mL | 0.5225 mL | 1.3063 mL | |
| 50 mM | 0.0418 mL | 0.2090 mL | 0.4180 mL | 1.0450 mL |
Trpvicin Related Classifications
HY-165559 Related Classifications
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