TRPV3 antagonist 74a

Name: TRPV3 antagonist 74a
Brand: MedChemExpress
SKU: HY-131868
Rating: 4.5 (1 reviews)

Cat. No.: HY-131868 Purity: 99.85%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

TRPV3 antagonist 74a is a potent and selective TRPV3 antagonist. TRPV3 antagonist 74a displays no significant activity against a panel of other ion channels. TRPV3 antagonist 74a can be used for the research of neuropathic pain.

For research use only. We do not sell to patients.

TRPV3 antagonist 74a Chemical Structure

CAS No. : 1432051-63-2

Size	Price	Stock	Quantity
1 mg	USD 175	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 430	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 690	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1380	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2200	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3500	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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TRPC TRPM TRPV TRPA TRPML

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]

TRPV3

In Vitro

TRPV3 antagonist 74a (100 μΜ; 2300 seconds; keratinocytes) largely attenuates SLIGRL or SLIGKV-induced Ca²⁺ responses^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TRPV3 antagonist 74a (150 μg; intradermal injection; 30 minutes) decreases the number of scratches significantly^[2].
. TRPV3 antagonist 74a (10~100 mg/kg; p.o.) dose-dependently attenuates mechanical allodynia induced by von Frey hair stimulation to the ipsilateral (injured) hind paw. TRPV3 antagonist 74a exhibits anti-nociceptive activity in the reserpine model of central pain by increasing muscle pressure threshold^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	WT mice
Dosage:	150 μg
Administration:	Intradermal injection; 30 minutes
Result:	The number of scratches decreased significantly.

Molecular Weight

338.32

Formula

C₁₇H₁₇F₃N₂O₂

CAS No.

1432051-63-2

Appearance

Solid

Color

White to off-white

SMILES

O[C@H](C1=CC=CC=N1)[C@@]2(C3=CC(C(F)(F)F)=CC=N3)C[C@@](O)(C2)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (295.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9558 mL	14.7789 mL	29.5578 mL
5 mM	0.5912 mL	2.9558 mL	5.9116 mL
10 mM	0.2956 mL	1.4779 mL	2.9558 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.85%

Select Batch:

Data Sheet (278 KB) SDS (251 KB)

COA (255 KB) HNMR (211 KB) CNMR (216 KB) LCMS (117 KB) Elemental Analysis Report (113 KB)

Handling Instructions (2659 KB)

References

[1]. Gomtsyan A, et al. Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists. J Med Chem. 2016;59(10):4926-4947. [Content Brief]

[2]. Zhao J, et al. PAR2 Mediates Itch via TRPV3 Signaling in Keratinocytes. J Invest Dermatol. 2020;140(8):1524-1532. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9558 mL	14.7789 mL	29.5578 mL	73.8945 mL
	5 mM	0.5912 mL	2.9558 mL	5.9116 mL	14.7789 mL
	10 mM	0.2956 mL	1.4779 mL	2.9558 mL	7.3895 mL
	15 mM	0.1971 mL	0.9853 mL	1.9705 mL	4.9263 mL
	20 mM	0.1478 mL	0.7389 mL	1.4779 mL	3.6947 mL
	25 mM	0.1182 mL	0.5912 mL	1.1823 mL	2.9558 mL
	30 mM	0.0985 mL	0.4926 mL	0.9853 mL	2.4632 mL
	40 mM	0.0739 mL	0.3695 mL	0.7389 mL	1.8474 mL
	50 mM	0.0591 mL	0.2956 mL	0.5912 mL	1.4779 mL
	60 mM	0.0493 mL	0.2463 mL	0.4926 mL	1.2316 mL
	80 mM	0.0369 mL	0.1847 mL	0.3695 mL	0.9237 mL
	100 mM	0.0296 mL	0.1478 mL	0.2956 mL	0.7389 mL