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| 5mg |
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| Other Sizes |
| ln Vitro |
Trpvicin (0-100 μM) dose-dependently inhibited the currents of TRPV3-WT and hTRPV3-G573S channels expressed in HEK293T cells, achieving almost complete inhibition at a concentration of 10 μM, with efficacy comparable to Ruthenium Red [1]. Trpvicin (10 μM, 24 hours) rescued the viability of HEK293T cells expressing the cytotoxic hTRPV3-G573S mutant, indicating that it has a functional blocking effect on constitutive active channels [1]. Trpvicin (0-100 μM) dose-dependently inhibited the currents of heterologously expressed hTRPV3-G568V and mTRPV3-G568V channels in HEK293T cells [1]. Trpvicin effectively inhibited heterologous expression of wild-type mouse TRPV3 (mTRPV3-WT) and gain-of-function mutant mTRPV3-G568V in HEK293T cells, with IC50 values of 0.38 μM and 0.42 μM, respectively [1]. The potency of Trpvicin against hTRPV3 A556V, A560T and F601A mutants was significantly reduced compared to the wild-type channel (reduced by 158-fold, 162-fold and 208-fold, respectively), indicating that these residues are key determinants of Trpvicin binding [1]. The efficacy of Trpvicin against the double mutants hTRPV3-G573S-F666A, hTRPV3-G573S-F666Y and hTRPV3-G573S-T665A was reduced by 17-fold, 12-fold and 16-fold, respectively, indicating that these residues have important drug-binding functions in the central cavity region, and their role exceeds their primary VSLD-PD binding site [1].
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| ln Vivo |
Trpvicin (10 and 100 µM, intradermal injection, sprayed 30 minutes before SLIGRL injection) significantly reduced acute scratching behavior in mice induced by SLIGRL [1]. Trpvicin (30 and 100 mg/kg, oral gavage, laboratory daily for 12 days starting 5 days before MC903 modeling) achieved chronic scratching and ear swelling in a MC903-induced mouse dermatitis model [1]. Trpvicin (1 wt%, topical, daily formulation for 16 days starting 50 days after birth) effectively improved hair loss in female and Trpv3+/G568V knock-in mice [1].
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| Cell Assay |
Cell Cytotoxicity Assay[1]
Cell Types: HEK293T cells Tested Concentrations: 10 μM Incubation Duration: 24 h Experimental Results: Rescued the cell viability of HEK293T cells expressing the cytotoxic hTRPV3-G573S mutant. |
| Animal Protocol |
Animal/Disease Models: 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]
Doses: 30 and 100 mg/kg Route of Administration: p.o., daily starting from 5 days before MC903 for 12 days Experimental Results: 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. Animal/Disease Models: Adult wild-type male C57BL/6J mice (8-12 weeks old) intradermally injected with SLIGRL (50 µg)[1] Doses: 10 and 100 µM Route of Administration: i.d., 30 min pre-SLIGRL Experimental Results: Exhibited fewer scratching bouts elicited by SLIGRL at both 10 and 100 µM. Animal/Disease Models: Trpv3+/G568V knock-in mice[1] Doses: 1 wt% Route of Administration: topically, daily from postnatal day 50 (P50) for 16 days Experimental Results: 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. |
| References |
| Molecular Formula |
C20H17F3N6O3S
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|---|---|
| Molecular Weight |
478.45
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| CAS # |
2019994-90-0
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~52.25 mM; with sonication)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0901 mL | 10.4504 mL | 20.9008 mL | |
| 5 mM | 0.4180 mL | 2.0901 mL | 4.1802 mL | |
| 10 mM | 0.2090 mL | 1.0450 mL | 2.0901 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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