1. GPCR/G Protein Neuronal Signaling Apoptosis Metabolic Enzyme/Protease Protein Tyrosine Kinase/RTK JAK/STAT Signaling Immunology/Inflammation
  2. mAChR Apoptosis MMP EGFR Interleukin Related
  3. 4-DAMP

4-DAMP  (Synonyms: 4-DAMP methiodide)

製品番号: HY-100958 純度: 99.96%
COA 取扱説明書 Technical Support

4-DAMP (4-DAMP methiodide) is a potent and selective antagonist of M3 receptors and also has a high affinity for the closely-related M5 receptors. 4-DAMP combined with 5-Fluorouracil (5-Fu) (HY-90006) could significantly reduce the cell viability and enhance apoptosis in MKN45 and BGC823 gastric cancer cells. 4-DAMP inhibits lipopolysaccharide (LPS)- and tobacco-induced pulmonary inflammation and reduces mucin 5AC (MUC5AC), oligomeric mucus/gel-forming secretion.

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4-DAMP

4-DAMP 構造式

CAS 番号 : 1952-15-4

容量 価格(税別) 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 44 在庫あり
Solution
10 mM * 1 mL in DMSO USD 44 在庫あり
Solid
5 mg $40 在庫あり
10 mg $60 在庫あり
25 mg $110 在庫あり
50 mg $170 在庫あり
100 mg $255 在庫あり
200 mg   お問い合わせ  
500 mg   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

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • 生物活性

  • 純度とドキュメンテーション

  • 参考文献

  • カスタマーレビュー

製品説明

4-DAMP (4-DAMP methiodide) is a potent and selective antagonist of M3 receptors and also has a high affinity for the closely-related M5 receptors. 4-DAMP combined with 5-Fluorouracil (5-Fu) (HY-90006) could significantly reduce the cell viability and enhance apoptosis in MKN45 and BGC823 gastric cancer cells. 4-DAMP inhibits lipopolysaccharide (LPS)- and tobacco-induced pulmonary inflammation and reduces mucin 5AC (MUC5AC), oligomeric mucus/gel-forming secretion[1][2][3].

IC50 & Target

mAChR3

 

mAChR5

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
4.1 × 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
CHO IC50
3.2 x 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
CHO IC50
3.2 x 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant muscarinic M5 receptor expressed in CHO cells
Displacement of [3H]4-DAMP from human recombinant muscarinic M5 receptor expressed in CHO cells
[PMID: 26988801]
CHO IC50
4.1 x 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
CHO IC50
3.2 x 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
CHO IC50
4.9 × 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
CHO IC50
4.9 x 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
CHO IC50
3.2 × 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [3H]4-DAMP from human recombinant M5 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
CHO IC50
4.1 x 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cells
Displacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cells
[PMID: 26988801]
CHO-K1 IC50
0.055 3
Compound: 4-DAMP
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M2 receptor expressed in CHOK1 cells after 2 hrs
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M2 receptor expressed in CHOK1 cells after 2 hrs
[PMID: 23403082]
CHO IC50
4.1 × 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cells
Displacement of [3H]4-DAMP from human recombinant muscarinic M3 receptor expressed in CHO cells
[PMID: 26988801]
CHO IC50
4.1 x 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [3H]4-DAMP from human recombinant M3 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
CHO-K1 IC50
4.5 1
Compound: 4-DAMP
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M1 receptor expressed in CHOK1 cells after 2 hrs
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M1 receptor expressed in CHOK1 cells after 2 hrs
[PMID: 23403082]
CHO IC50
4.9 × 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant muscarinic M4 receptor expressed in CHO cells
Displacement of [3H]4-DAMP from human recombinant muscarinic M4 receptor expressed in CHO cells
[PMID: 26988801]
CHO IC50
4.9 x 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant muscarinic M4 receptor expressed in CHO cells
Displacement of [3H]4-DAMP from human recombinant muscarinic M4 receptor expressed in CHO cells
[PMID: 26988801]
CHO-K1 IC50
5.1 1
Compound: 4-DAMP
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
[PMID: 23403082]
CHO IC50
3.2 × 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant muscarinic M5 receptor expressed in CHO cells
Displacement of [3H]4-DAMP from human recombinant muscarinic M5 receptor expressed in CHO cells
[PMID: 26988801]
CHO IC50
4.9 x 10-10 41
Compound: 4-DAMP
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
Displacement of [3H]4-DAMP from human recombinant M4 receptor expressed in CHO cells measured after 60 mins by scintillation counting method
[PMID: 27876250]
CHO-K1 IC50
0.055 3
Compound: 4-DAMP
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M2 receptor expressed in CHOK1 cells after 2 hrs
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M2 receptor expressed in CHOK1 cells after 2 hrs
[PMID: 23403082]
CHO-K1 IC50
4.5 1
Compound: 4-DAMP
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M1 receptor expressed in CHOK1 cells after 2 hrs
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M1 receptor expressed in CHOK1 cells after 2 hrs
[PMID: 23403082]
CHO-K1 IC50
5.1 1
Compound: 4-DAMP
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
[PMID: 23403082]
CHO-K1 IC50
0.055 3
Compound: 4-DAMP
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M2 receptor expressed in CHOK1 cells after 2 hrs
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M2 receptor expressed in CHOK1 cells after 2 hrs
[PMID: 23403082]
CHO-K1 IC50
4.5 1
Compound: 4-DAMP
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M1 receptor expressed in CHOK1 cells after 2 hrs
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M1 receptor expressed in CHOK1 cells after 2 hrs
[PMID: 23403082]
CHO-K1 IC50
5.1 1
Compound: 4-DAMP
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
Displacement of [3H]N-methylscopolamine from human recombinant muscarinic M3 receptor expressed in CHOK1 cells after 2 hrs
[PMID: 23403082]
体外実験

4-DAMP (10 μM, 5 days) combined with 5-Fu (5 μM, 5 days) can inhibit cell growth and promote apoptosis in MKN45 and BGC823 cells[2].

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

Cell Viability Assay[2]

Cell Line: MKN45 and BGC823 cells
Concentration: 10 μM
Incubation Time: 5 days
Result: Reduced the cell viability to (30±4.0)% and (35±6.0)% combined with 5-Fu in MKN45 and BGC823 cells, respectively.
体内実験

4-DAMP (1mg/kg, i.p., daily for 12 days) inhibits gastric tumor formation in nude mouse MKN45 and BGC823 tumor xenografts[2].
4-DAMP (0.6 or 0.12 mg/kg, intranasal instillation, daily for 35 days) reduces the allergic rhinitis (AR) symptom scores and nasal secretion weights, reverses goblet cell metaplasia, alleviates eosinophil infiltration, inhibits the levels of MUC5AC, histamine and cytokines, MMP9, EGFR in AR guinea pigs[3].

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

Animal Model: Mouse MKN45 and BGC823 tumor xenografts[2]
Dosage: 1mg/kg
Administration: i.p., daily for 12 days
Result: Reduced the tumor sizes and the tumor weights in both MKN45 and BGC823 xenografts.
Animal Model: AR guinea pigs[3]
Dosage: 0.6 or 0.12 mg/kg
Administration: intranasal instillation, daily for 35 days
Result: Reduced the weights of nasal secretions, reversed goblet cell metaplasia of the animal nasal mucosal epithelium, inhibited the levels of MUC5AC mRNA, IL-4, IL-13, and TNF-α in AR guinea pigs.
分子量

451.34

分子式

C21H26INO2

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

C[N+]1(C)CCC(OC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)CC1.[I-]

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (221.56 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 2.2156 mL 11.0781 mL 22.1562 mL
5 mM 0.4431 mL 2.2156 mL 4.4312 mL
10 mM 0.2216 mL 1.1078 mL 2.2156 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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一般には略語で表示されます:C1V1 = C2V2

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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: ≥ 5 mg/mL (11.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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% Corn Oil

    Solubility: ≥ 5 mg/mL (11.08 mM); Clear solution

    This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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Please enter your animal formula composition:
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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

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, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2156 mL 11.0781 mL 22.1562 mL 55.3906 mL
5 mM 0.4431 mL 2.2156 mL 4.4312 mL 11.0781 mL
10 mM 0.2216 mL 1.1078 mL 2.2156 mL 5.5391 mL
15 mM 0.1477 mL 0.7385 mL 1.4771 mL 3.6927 mL
20 mM 0.1108 mL 0.5539 mL 1.1078 mL 2.7695 mL
25 mM 0.0886 mL 0.4431 mL 0.8862 mL 2.2156 mL
30 mM 0.0739 mL 0.3693 mL 0.7385 mL 1.8464 mL
40 mM 0.0554 mL 0.2770 mL 0.5539 mL 1.3848 mL
50 mM 0.0443 mL 0.2216 mL 0.4431 mL 1.1078 mL
60 mM 0.0369 mL 0.1846 mL 0.3693 mL 0.9232 mL
80 mM 0.0277 mL 0.1385 mL 0.2770 mL 0.6924 mL
100 mM 0.0222 mL 0.1108 mL 0.2216 mL 0.5539 mL
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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)
× = ×
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Inquiry Information

製品名:
4-DAMP
製品番号:
HY-100958
数量:
MCE 日本正規代理店: