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MedChemExpressModel 4-DAMP -1952-15-4

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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].
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4-DAMP

MCE China:4-DAMP

Brand:MedChemExpress (MCE)

Cat. No.HY-100958

CAS:1952-15-4

Synonyms:4-DAMP methiodide

Purity:99.99%

Storage: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)

Shipping:Room temperature in continental US; may vary elsewhere.

Description: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.

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].

In Vivo: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].

IC50 & Target:mAChR3 mAChR5

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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]

Brand introduction:
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