| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
Target: Lamin isoform A-delta10. Lamin A-delta10 is a splice variant of lamin A/C, a type V intermediate filament protein that forms the nuclear lamina, a meshwork underlying the inner nuclear membrane. The lamin proteins provide structural support to the nucleus and regulate nuclear processes including transcription, DNA replication, and chromatin organization.
|
|---|---|
| ln Vitro |
In vitro, the specific biological activity of MLS-001006105 is not fully detailed in public literature. It is used as a chemical probe in biological assays to study the function of lamin isoform A-delta10. No specific IC50 or EC50 values have been disclosed. Further published data is required to characterize its in vitro potency and selectivity.
|
| ln Vivo |
No in vivo efficacy data have been published specifically for MLS-001006105 in animal models. As a chemical tool targeting lamin isoforms, it is expected to be used in preclinical studies to investigate the role of nuclear lamina alterations in disease models (e.g., mouse models of Emery-Dreifuss muscular dystrophy or Hutchinson-Gilford progeria syndrome), but no such data is currently available in the public domain.
|
| Enzyme Assay |
For cell-free assays: not applicable. The compound is likely used in pull-down assays or biophysical binding studies with recombinant lamin A-delta10 protein to determine binding affinity (e.g., by surface plasmon resonance (SPR) or microscale thermophoresis (MST)). Binding constants (KD) have not been publicly disclosed.
|
| Cell Assay |
For cell assays: cell lines expressing lamin isoform A-delta10 (e.g., transfected HeLa cells, fibroblasts from laminopathy patients) are treated with MLS-001006105 (likely 1-50 uM range, 24-72 h). Nuclear morphology is assessed by immunofluorescence staining of lamin proteins. Cell viability, proliferation, and nuclear blebbing are measured to evaluate the compound's effect on nuclear integrity and cellular function. Detailed protocols are not publicly available for this specific compound.
|
| Animal Protocol |
No in vivo animal studies have been specifically reported for MLS-001006105 in peer-reviewed literature. Potential future studies would involve its use in transgenic mouse models of laminopathies (e.g., Lmna knockout mice or progeria mice). The compound would likely be administered via intraperitoneal injection (IP) or oral gavage to assess its effects on muscle function, lifespan, and nuclear morphology in tissues. However, no such data is available.
|
| ADME/Pharmacokinetics |
No PK data are available for MLS-001006105. For small molecule inhibitors targeting nuclear proteins (MW 377.44, LogP 2.7), predicted PK in rodents: moderate oral bioavailability, Tmax 1-2 h, half-life 4-6 h. The compound is soluble in DMSO (125 mg/mL) for in vitro and in vivo formulation. In vivo formulation is proposed as 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (2.08 mg/mL, 5.51 mM).
|
| Toxicity/Toxicokinetics |
No toxicity data have been reported for MLS-001006105. As the compound targets nuclear lamins, potential toxicities may include disruption of nuclear integrity in non-diseased cells, leading to cell cycle defects and genomic instability. Off-target effects on other lamin isoforms or nuclear proteins are not documented. No acute toxicity or LD50 studies have been published.
|
| Additional Infomation |
MLS-001006105 is a research compound not yet approved for clinical use. It is a valuable chemical probe for studying the molecular mechanisms of nuclear envelope disorders (laminopathies) and for validating lamin isoform A-delta10 as a therapeutic target. The compound is for research use only and is not intended for human therapeutic administration. No clinical trials have been registered for this compound.
|
| Molecular Formula |
C15H15N5O3S2
|
|---|---|
| Molecular Weight |
377.441299676895
|
| Exact Mass |
377.061
|
| CAS # |
455310-36-8
|
| PubChem CID |
2341387
|
| Appearance |
Off-white to pink solid powder
|
| LogP |
2.7
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
25
|
| Complexity |
447
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
MOJJOJXUACHANH-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C15H15N5O3S2/c1-22-11-4-3-9(5-12(11)23-2)10-6-24-15(18-10)19-13(21)7-25-14-16-8-17-20-14/h3-6,8H,7H2,1-2H3,(H,16,17,20)(H,18,19,21)
|
| Chemical Name |
N-[4-(3,4-dimethoxyphenyl)-1,3-thiazol-2-yl]-2-(1H-1,2,4-triazol-5-ylsulfanyl)acetamide
|
| 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 |
| 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 : ~125 mg/mL (~331.18 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.51 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6494 mL | 13.2471 mL | 26.4943 mL | |
| 5 mM | 0.5299 mL | 2.6494 mL | 5.2989 mL | |
| 10 mM | 0.2649 mL | 1.3247 mL | 2.6494 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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
