4-DAMP
Based on 4 publication(s) in Google Scholar
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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.96%
- CAS No.: 1952-15-4
- 화학식: C21H26INO2
- 분자량:451.34
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보관:
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) 4-DAMP
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Biological Activity
제품 설명
IC50 & Target
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mAChR3 |
mAChR5 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
3.2 x 10-10 M
Compound: 4-DAMP
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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
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[PMID: 26988801] |
| CHO | IC50 |
4.1 x 10-10 M
Compound: 4-DAMP
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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
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[PMID: 26988801] |
| CHO | IC50 |
4.9 x 10-10 M
Compound: 4-DAMP
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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
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[PMID: 26988801] |
| CHO | IC50 |
3.2 x 10-10 M
Compound: 4-DAMP
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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
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[PMID: 27876250] |
| CHO | IC50 |
4.1 x 10-10 M
Compound: 4-DAMP
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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
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[PMID: 27876250] |
| CHO | IC50 |
4.9 x 10-10 M
Compound: 4-DAMP
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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
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[PMID: 27876250] |
| CHO-K1 | IC50 |
0.055 μM
Compound: 4-DAMP
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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
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[PMID: 23403082] |
| CHO-K1 | IC50 |
4.5 nM
Compound: 4-DAMP
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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
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[PMID: 23403082] |
| CHO-K1 | IC50 |
5.1 nM
Compound: 4-DAMP
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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
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[PMID: 23403082] |
In Vitro
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. Further protocols information, click here.
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Cell Line:MKN45 and BGC823 cells
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Concentration:10 μM
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Incubation Time:5 days
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Result:Reduced the cell viability to (30±4.0)% and (35±6.0)% combined with 5-Fu in MKN45 and BGC823 cells, respectively.
In Vivo
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.
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Animal Model:Mouse MKN45 and BGC823 tumor xenografts[2]
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Dosage:1mg/kg
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Administration:i.p., daily for 12 days
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Result:Reduced the tumor sizes and the tumor weights in both MKN45 and BGC823 xenografts.
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Animal Model:AR guinea pigs[3]
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Dosage:0.6 or 0.12 mg/kg
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Administration:intranasal instillation, daily for 35 days
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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.
Chemical Information
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CAS No. 1952-15-4
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Appearance Solid
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분자량 451.34
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화학식 C21H26INO2
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Color White to off-white
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SMILES
C[N+]1(C)CCC(OC(C(C2=CC=CC=C2)C3=CC=CC=C3)=O)CC1.[I-]
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Synonyms
4-DAMP methiodide
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선적
Room temperature in continental US; may vary elsewhere.
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보관
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)
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Rep
Septo-subicular cholinergic circuit promotes seizure development via astrocytic inflammation. [Abstract]2025 May 14;44(5):115712. PMID: 40372911 -
Cell Biosci
Gut microbial metabolite deoxycholic acid facilitates Th17 differentiation through modulating cholesterol biosynthesis and participates in high-fat diet-associated colonic inflammation. [Abstract]2023 Oct 3;13(1):186. PMID: 37789469 -
Pharmaceuticals (Basel)
Ethanolic Extracts of Cupressaceae Species Conifers Provide Rapid Protection against Barium Chloride-Induced Cardiac Arrhythmia. [Abstract]2024 Jul 29;17(8):1003. PMID: 39204108 -
Mol Cell Endocrinol
Vagotomy suppresses food intake by increasing GLP-1 secretion via the M3 AChR-AMPKα pathway in mice. [Abstract]2025 Apr 1:599:112464. PMID: 39848433
용액&용해도
In Vitro:
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)
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.
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.
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.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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CCK-8/WST-8 Cell Proliferation Assay
The CCK-8/WST-8 assay is based on the reduction of the water-soluble tetrazolium salt WST-8 to a water-soluble formazan product by cellular dehydrogenases in metabolically active cells, where the generated formazan amount is proportional to the number of living cells and is quantified by measuring absorbance in the visible range, providing a colorimetric readout for cell viability and proliferation assessment. This class of tetrazolium-based assays improves upon earlier MTT-based systems by producing a water-soluble formazan, eliminating the need for organic solubilization steps and enabling direct spectrophotometric measurement in culture medium.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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MTT Cell Proliferation Assay
The MTT assay is a colorimetric endpoint assay for estimating viable cell number, cell growth, cytotoxicity, or cell activation in cultured mammalian cells. Living cells reduce the yellow tetrazolium salt MTT into purple/blue formazan, while dead cells do not generate the same signal; the resulting color can be quantified with a multiwell spectrophotometer. MTT reduction is commonly interpreted as a readout of metabolic activity that often correlates with viable cell number, but it should not be treated as a direct cell-counting method unless the assay is optimized for the cell type and experimental condition. Studies show that MTT reduction can involve mitochondrial and non-mitochondrial reducing systems, and formazan may accumulate in intracellular lipid droplets rather than simply marking mitochondria.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
순도&문서
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Data Sheet (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
[1]. Watson N, et al. Comparative pharmacology of recombinant human M3 and M5 muscarinic receptors expressed in CHO-K1 cells. Br J Pharmacol. 1999 May;127(2):590-6. [Content Brief]
[2]. Yu H, et al. Acetylcholine acts through M3 muscarinic receptor to activate the EGFR signaling and promotes gastric cancer cell proliferation. Sci Rep. 2017 Jan 19;7:40802. [Content Brief]
[3]. Huang Y, et al. Effects of 4-DAMP on allergic rhinitis in guinea pigs and its potential mechanism. Ann Transl Med. 2022 Jul;10(14):774. [Content Brief]
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 |
4-DAMP Related Classifications
HY-100958 Related Classifications
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