2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. Chembridge-5861528

Chembridge-5861528  (Synonyms: TCS 5861528)

製品番号: HY-15065 純度: 99.12%
COA 取扱説明書 Technical Support

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.

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Chembridge-5861528

Chembridge-5861528 構造式

CAS 番号 : 332117-28-9

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 79 在庫あり
Solution
10 mM * 1 mL in DMSO USD 79 在庫あり
Solid
5 mg $72 在庫あり
10 mg $116 在庫あり
25 mg $233 在庫あり
50 mg $373 在庫あり
100 mg $560 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 1 publication(s) in Google Scholar

Chembridge-5861528 関連抗体

Top Publications Citing Use of Products

TRP Channel アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

  • 生物活性

  • 純度とドキュメンテーション

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製品説明

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[1].

IC50 & Target[1]

TRPA1

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

TRPA1

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

体外実験

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.

Chembridge-5861528 関連抗体
体内実験

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.html" class="link-product" target="_blank">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 (F1,80= 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.
分子量

369.42

分子式

C19H23N5O3
CAS 番号
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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

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)

g

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.
純度とドキュメンテーション
参考文献

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.

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
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Chembridge-5861528 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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