| ln Vitro |
tandem peptide containing LNSMGQD (20 μM; 30 min) selectively enhanced isotype binding of Dsg2 under cell-free conditions and reversed the inhibitory effect of L-tryptophan without affecting E-cadherin binding [1]. A tandem peptide containing LNSMGQD (20 μM; 24 h) prevented TNF-α-induced loss of intercellular adhesion and increased cell permeability in CaCo2 and HCT116 intestinal epithelial cells [1]. A tandem peptide containing LNSMGQD (20 μM; 24 h) blocked the upregulation of pore-forming tight junction protein claudin-2 in CaCo2 intestinal epithelial cells induced by TNF-α and maintained the junctional localization of Dsg2 and claudin-1 [1]. LNSMGQD (200 μM; 24 h) disrupted intercellular adhesion of human keratinocytes HaCaT in a dissociation assay based on dispersants and induced keratin filament contraction [2]. LNSMGQD (200 μM; 30 min) induces phosphorylation of p38 MAPK in human keratinocytes HaCaT[2]. LNSMGQD (40 μM; 1 h) directly interferes with the binding sites involved in homo- and hetero-desmosome core protein 2 interactions, thereby reducing the binding probability without altering the unimolecular dissociation force[3].
|
|---|---|
| ln Vivo |
LNSMGQD (200 μmol/L; intradermal injection; single dose) increased phosphorylation of p38 MAPK in the dorsal skin of newborn Balb/c mice [2].
|
| Cell Assay |
Immunofluorescence [1]
Cell Types: CaCO2 Tested Concentrations: 20 μM Incubation Duration: 24 hours Experimental Results: It prevented the reduction and breakage of Dsg2 and claudin-1 staining at intercellular junctions induced by TNF-α. It maintained their linear and regular positioning along the cell boundary. Western Blot analysis [2] Cell Types: HaCaT human keratinocytes Tested Concentrations: 200 μM Incubation Duration: 30 minutes Experimental Results: p38 MAPK phosphorylation level increased to 1.9 ± 0.4 times that of untreated control cells. |
| Animal Protocol |
Animal/Disease Models:Balb/c mouse pemphigus vulgaris (newborn, 1.4–1.8 g) [2]
Doses: 200 μmol/L Route of Administration: Intradermal injection; single dose Experimental Results: Phosphorylated p38 MAPK levels in the dorsal skin of mice increased to 2.0 ± 0.3 times that of control IgG-injected mice. DSG3 immunostaining fragmentation was detected; no intradermal vesicle formation was observed. |
| References |
|
| CAS # |
1152066-26-6
|
|---|---|
| Sequence |
Leu-Asn-Ser-Met-Gly-Gln-AspLNSMGQD
|
| SequenceShortening |
LNSMGQD
|
| Appearance |
White to off-white solid
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: 请将本产品存放在密封保护的环境中，避免受潮。 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~130.92 mM; with sonication)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
