Chembridge-5861528 (Synonyms: TCS 5861528)

Cat. No.: HY-15065 Purity: 99.76%: FAQs
Data Sheet SDS COA Handling Instructions

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Chembridge-5861528 (TCS 5861528) is a potent TRPA1 channel antagonist that antagonizes similarly allyl isothiocyanate- and 4-HNE-evoked TRPA1 responses, with IC₅₀ values of 14.3 μM and 18.7 μM, respectively. Chembridge-5861528 shows antihypersensitivity activities.

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

Chembridge-5861528 Chemical Structure

CAS No. : 332117-28-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 87	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 87	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 79	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 528	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 924	In-stock	Estimated Time of Arrival: December 31
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TRPC TRPM TRPV TRPA TRPML

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

TRPA1

14.3 μM (IC₅₀, allyl isothiocyanate-evoked TRPA1 response)

TRPA1

18.7 μM (IC₅₀, 4-HNE-evoked TRPA1 response)

In Vitro

Chembridge-5861528 (TCS 5861528) shows no TRPA1 or TRPV1 channel agonism and no TRPV1 channel antagonism up to a dose of 100 μM^[1].

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

In Vivo

Chembridge-5861528 (TCS 5861528) (30 mg/kg; i.p.; twice daily for a week) significantly attenuates development of mechanical hypersensitivity in Streptozocin (HY-13753)-induced diabetes mellitus rat model^[1].
Chembridge-5861528 (3 and 10 μg/rat; i.t.; once) attenuates Capsaicin (HY-10448)-induced blood flow increase in a dose-related fashion^[2].

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

Animal Model:	Male Hannover-Wistar rats, Streptozocin-induced diabetes mellitus model^[1]
Dosage:	30 mg/kg
Administration:	Intraperitoneal injection, twice daily for a week
Result:	Significantly attenuated development of mechanical hypersensitivity as revealed by the paw pressure test (F^1,80= 31.4, P < 0.0001).

Animal Model:	Male Hannover–Wistar rats (220-260 g), Capsaicin-induced neurogenic inflammation model^[2]
Dosage:	0, 3, and 10 μg/rat
Administration:	Intrathecal injection, 20 min before Capsaicin injection
Result:	Significantly decreased the blood flow at 10 μg.

Molecular Weight

369.42

Formula

C₁₉H₂₃N₅O₃

CAS No.

332117-28-9

Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(N=CN2CC(NC3=CC=C(C(C)CC)C=C3)=O)N(C)C(N1C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 120 mg/mL (324.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.7069 mL	13.5347 mL	27.0695 mL
5 mM	0.5414 mL	2.7069 mL	5.4139 mL
10 mM	0.2707 mL	1.3535 mL	2.7069 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (8.12 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (8.12 mM); Clear solution

This protocol yields a clear solution of ≥ 3 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 (30.0 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: 99.76%

Select Batch:

Data Sheet (275 KB) SDS (0 KB)

COA (249 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[1]. Wei H, et al. Attenuation of mechanical hypersensitivity by an antagonist of the TRPA1 ion channel in diabetic animals. Anesthesiology. 2009 Jul;111(1):147-54. [Content Brief]

[2]. Wei H, et al. Spinal TRPA1 ion channels contribute to cutaneous neurogenic inflammation in the rat. Neurosci Lett. 2010 Aug 2;479(3):253-6. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.7069 mL	13.5347 mL	27.0695 mL	67.6736 mL
	5 mM	0.5414 mL	2.7069 mL	5.4139 mL	13.5347 mL
	10 mM	0.2707 mL	1.3535 mL	2.7069 mL	6.7674 mL
	15 mM	0.1805 mL	0.9023 mL	1.8046 mL	4.5116 mL
	20 mM	0.1353 mL	0.6767 mL	1.3535 mL	3.3837 mL
	25 mM	0.1083 mL	0.5414 mL	1.0828 mL	2.7069 mL
	30 mM	0.0902 mL	0.4512 mL	0.9023 mL	2.2558 mL
	40 mM	0.0677 mL	0.3384 mL	0.6767 mL	1.6918 mL
	50 mM	0.0541 mL	0.2707 mL	0.5414 mL	1.3535 mL
	60 mM	0.0451 mL	0.2256 mL	0.4512 mL	1.1279 mL
	80 mM	0.0338 mL	0.1692 mL	0.3384 mL	0.8459 mL
	100 mM	0.0271 mL	0.1353 mL	0.2707 mL	0.6767 mL

Chembridge-5861528 Related Classifications

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:

Chembridge-5861528332117-28-9TCS 5861528Chembridge5861528Chembridge 5861528TCS5861528TCS-5861528TRP ChannelTransient receptor potential channelsdiabetes mellitusantihypersensitivityneurogenic inflammationInhibitorinhibitorinhibit

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