2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. Trpvicin

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.

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Trpvicin

Trpvicin Chemical Structure

CAS No. : 2019994-90-0

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Description

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[1].

IC50 & Target[1]

TRPV3

 

In Vitro

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.

Trpvicin Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: HEK293T cells
Concentration: 10 μM
Incubation Time: 24 h
Result: Rescued the cell viability of HEK293T cells expressing the cytotoxic hTRPV3-G573S mutant.
In Vivo

Trpvicin (10 and 100 µM, i.d., 30 min pre-SLIGRL) significantly reduces acute scratching in mice induced by SLIGRL (HY-P1308)[1].
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.

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]
Dosage: 30 and 100 mg/kg
Administration: p.o., daily starting from 5 days before MC903 for 12 days
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.
Animal Model: Adult wild-type male C57BL/6J mice (8-12 weeks old) intradermally injected with SLIGRL (50 µg)[1]
Dosage: 10 and 100 µM
Administration: i.d., 30 min pre-SLIGRL
Result: Exhibited fewer scratching bouts elicited by SLIGRL at both 10 and 100 µM.
Animal Model: Trpv3+/G568V knock-in mice[1]
Dosage: 1 wt%
Administration: topically, daily from postnatal day 50 (P50) for 16 days
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.
Molecular Weight

478.45

Formula

C20H17F3N6O3S
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Trpvicin2019994-90-0TRP ChannelTransient receptor potential channelsTRPV3TRP familyVSLD-PDG573S mutantpharmacologicalitchhair lossInhibitorinhibitorinhibit

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