1. GPCR/G Protein Anti-infection
  2. Endothelin Receptor Bacterial Antibiotic
  3. Sulfisoxazole

スルフィソキサゾール  (Synonyms: Sulfisoxazole; Sulfafurazole)

製品番号: HY-B0323 純度: 99.90%
COA 取扱説明書 Technical Support

Sulfisoxazole (Sulfafurazole) is an orally active endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole is a sulfonamide antibacterial agent with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A.

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Sulfisoxazole

スルフィソキサゾール 構造式

CAS 番号 : 127-69-5

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 33 在庫あり
Solution
10 mM * 1 mL in DMSO USD 33 在庫あり
Solid
100 mg $30 在庫あり
500 mg $60 在庫あり
1 g   お問い合わせ  
5 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Other Forms of Sulfisoxazole:

Top Publications Citing Use of Products

Endothelin Receptor アイソフォーム固有の製品をすべて表示:

Antibiotic アイソフォーム固有の製品をすべて表示:

  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

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製品説明

Sulfisoxazole (Sulfafurazole) is an orally active endothelin receptor antagonist with IC50 values of 0.60 μM and 22 μM against endothelin receptor A and endothelin receptor B, respectively. Sulfisoxazole is a sulfonamide antibacterial agent with an oxazole substituent. Sulfisoxazole inhibits breast cancer exosome release by targeting endothelin receptor A[1][2].

IC50 & Target

ETA

0.60 μM (IC50)

ETB

22 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
A10 IC50
0.78 3
Compound: 2
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
[PMID: 8308857]
A10 IC50
0.78 3
Compound: 2
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
[PMID: 8308857]
A7R5 IC50
9 3
Compound: 5g
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
[PMID: 10969989]
A7R5 IC50
9 3
Compound: 5g
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
Displacement of [125 I] ET-1 from rat aortic smooth muscle A7r5 cells transfected with Endothelin A receptor
[PMID: 10969989]
体外実験

Sulfisoxazole (0-100 μM) inhibits the secretion of sEV in three representative human breast cell lines: MCF10A (normal), MCF7 (weakly invasive), and MDA-MB231 (highly invasive)[2].
Sulfisoxazole (200 μM, 48 h) together with αPD‐L1 recovers the activity of CD8+ cytotoxic T cells by inhibiting secretion of cancer cell (MDA-MB-231) exosomal PD‐L1[3].
Sulfisoxazole (100 μM, 72 h) inhibits the LPS induced elevation of nitric oxide and the reduction in GABA-containing neurones in a primary rat retinal culture[4].

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

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cell
Concentration: 100 μM
Incubation Time: 24 h
Result: Reduced the expression of Rab27a.
体内実験

Sulfisoxazole (p.o., 200 mg/kg, 14 days) inhibits tumor growth in mouse 4T1 breast cancer xenografts and female nude mice orthotopically implanted with MDA-MB231 cells[2].
Sulfisoxazole (p.o., 200 mg/kg) together with αPD‐L1 (5 mg/kg, i.p.) reduces the tumor growth rate in CT26 tumor‐bearing mice, and boosts the antitumor effect of αPD‐1[3].
Sulfisoxazole (5 μL of 400 μM, injected into the vitreous humour of the ischemic eye) shows neuroprotection effect to the retina of rats with ischemia/reperfusion[4].

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

分子量

267.30

分子式

C11H13N3O3S

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(N)C=C1)(NC2=C(C)C(C)=NO2)=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 : ≥ 150 mg/mL (561.17 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 3.7411 mL 18.7056 mL 37.4112 mL
5 mM 0.7482 mL 3.7411 mL 7.4822 mL
10 mM 0.3741 mL 1.8706 mL 3.7411 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (9.35 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 (9.35 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.
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

純度: 99.90%

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 3.7411 mL 18.7056 mL 37.4112 mL 93.5279 mL
5 mM 0.7482 mL 3.7411 mL 7.4822 mL 18.7056 mL
10 mM 0.3741 mL 1.8706 mL 3.7411 mL 9.3528 mL
15 mM 0.2494 mL 1.2470 mL 2.4941 mL 6.2352 mL
20 mM 0.1871 mL 0.9353 mL 1.8706 mL 4.6764 mL
25 mM 0.1496 mL 0.7482 mL 1.4964 mL 3.7411 mL
30 mM 0.1247 mL 0.6235 mL 1.2470 mL 3.1176 mL
40 mM 0.0935 mL 0.4676 mL 0.9353 mL 2.3382 mL
50 mM 0.0748 mL 0.3741 mL 0.7482 mL 1.8706 mL
60 mM 0.0624 mL 0.3118 mL 0.6235 mL 1.5588 mL
80 mM 0.0468 mL 0.2338 mL 0.4676 mL 1.1691 mL
100 mM 0.0374 mL 0.1871 mL 0.3741 mL 0.9353 mL
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  • 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.

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製品名:
Sulfisoxazole
製品番号:
HY-B0323
数量:
MCE 日本正規代理店: