| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Targets |
WT-TTR inhibitor 1 targets wild-type Transthyretin (WT-TTR), a protein that transports thyroxine and retinol-binding protein in the blood and cerebrospinal fluid. TTR can misfold and form amyloid fibrils, leading to familial amyloid polyneuropathy and other amyloid diseases. By occupying the thyroxine binding site, the compound stabilizes the tetrameric structure of TTR, preventing its dissociation into monomers that can aggregate into amyloid fibrils. The compound shows 29.05% inhibition at 100 μM. It can be used for research of familial amyloid polyneuropathy.
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| ln Vitro |
In vitro studies demonstrate that WT-TTR inhibitor 1 (Compound 21) is a wild-type Transthyretin (WT-TTR) inhibitor with 29.05% inhibition at 100 μM. It stabilizes the tetrameric structure of TTR by occupying its thyroxine binding site, preventing its dissociation and amyloidosis. The compound's ability to inhibit TTR aggregation makes it a valuable tool for studying amyloid diseases. It can be used for research of familial amyloid polyneuropathy. Detailed in vitro characterization data, including binding affinity and aggregation inhibition assays, are available in the primary literature.
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| ln Vivo |
In vivo studies of WT-TTR inhibitor 1 are limited in publicly available literature. As a TTR tetramer stabilizer, the compound has potential for in vivo investigations of familial amyloid polyneuropathy and other TTR amyloid diseases. TTR stabilizers have been shown to reduce amyloid deposition and disease progression in animal models. However, specific in vivo efficacy data and detailed animal model studies for this particular compound are not extensively reported. Further research is needed to establish its in vivo activity profile, pharmacokinetic properties, and therapeutic potential.
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| Enzyme Assay |
For TTR binding and stabilization assays, recombinant wild-type TTR protein is incubated with varying concentrations of WT-TTR inhibitor 1. Binding affinity is assessed by fluorescence quenching or surface plasmon resonance (SPR). TTR tetramer stabilization is assessed by acid-mediated dissociation assays, where TTR is exposed to acidic conditions and tetramer stability is measured by native gel electrophoresis or size-exclusion chromatography. Inhibition of amyloid formation is assessed by Thioflavin T (ThT) fluorescence assays under amyloidogenic conditions. IC50 values or percent inhibition (e.g., 29.05% at 100 μM) are calculated. Assays are performed in triplicate with appropriate vehicle controls.
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| Cell Assay |
For in vitro cellular assays, cell lines expressing TTR (e.g., HepG2 cells) or neuronal cells are cultured in appropriate media under standard conditions (37°C, 5% CO2). WT-TTR inhibitor 1 is dissolved in DMSO and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. TTR secretion and aggregation can be assessed by ELISA or Western blot. Cell viability and cytotoxicity are assessed using MTT or similar assays. For amyloidosis models, cells may be exposed to amyloidogenic conditions. Each concentration is tested in replicate wells with vehicle controls.
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| Animal Protocol |
For in vivo animal studies of WT-TTR inhibitor 1, no specific published protocols are available. For general in vivo administration of TTR stabilizers, compounds are typically formulated in suitable vehicles and administered via oral gavage, intraperitoneal (i.p.) injection, or intravenous (i.v.) injection. Dosing regimens vary by study objective. In TTR amyloidosis models (e.g., transgenic mice expressing mutant TTR), animals may be treated with compound and TTR aggregation and tissue deposition are assessed. Blood and tissue samples may be collected for pharmacokinetic analysis. All procedures must follow institutional animal care and use committee guidelines.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of WT-TTR inhibitor 1 are characteristic of a small-molecule TTR stabilizer. The compound has a molecular weight of 312.77, formula C16H9ClN2OS, and CAS number 23983-05-3. Purity: typically high. Storage: typically at -20°C for powder; in solvent at -80°C. Solubility: soluble in DMSO and other organic solvents. Stability and solubility advice: information concerning product stability, particularly in solution, has rarely been reported. Specific pharmacokinetic parameters are not extensively reported in publicly available sources.
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| Toxicity/Toxicokinetics |
According to available safety information, WT-TTR inhibitor 1 is intended for research purposes only. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. No clinical toxicity data are available.
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| References | |
| Additional Infomation |
WT-TTR inhibitor 1 (Compound 21) is a wild-type Transthyretin (WT-TTR) inhibitor with 29.05% inhibition at 100 μM. It stabilizes TTR tetramers by occupying the thyroxine binding site, preventing dissociation and amyloidosis. It can be used for research of familial amyloid polyneuropathy. It has a molecular weight of 312.77 and formula C16H9ClN2OS. It is for research use only with no clinical development or regulatory approvals reported.
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| Molecular Formula |
C16H9CLN2OS
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| Molecular Weight |
312.77
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| Exact Mass |
312.012
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| CAS # |
23983-05-3
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| PubChem CID |
689165
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.11
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
469
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C(=C1)/C=C\2/C(=O)N3C4=CC=CC=C4N=C3S2)Cl
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| InChi Key |
LSMPFFSYANAQSU-ZROIWOOFSA-N
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| InChi Code |
InChI=1S/C16H9ClN2OS/c17-11-6-2-1-5-10(11)9-14-15(20)19-13-8-4-3-7-12(13)18-16(19)21-14/h1-9H/b14-9-
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| Chemical Name |
(2Z)-2-[(2-chlorophenyl)methylidene]-[1,3]thiazolo[3,2-a]benzimidazol-1-one
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| 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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1972 mL | 15.9862 mL | 31.9724 mL | |
| 5 mM | 0.6394 mL | 3.1972 mL | 6.3945 mL | |
| 10 mM | 0.3197 mL | 1.5986 mL | 3.1972 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.
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