| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
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| Other Sizes |
|
| Targets |
ALDH1
|
|---|---|
| ln Vitro |
Stra8 expression in entire testis cultures containing germ cells and somatic cells is inhibited by WIN 18446 (1 μM, 24 hours) [2].
|
| ln Vivo |
Win 18446 (200 mg/kg, taken orally for 4, 8, and 16 weeks) causes severe impairments to spermatogenesis, a major decrease in intratesticular retinoic acid concentration, and ultimately sterility[1].
|
| Cell Assay |
RT-PCR[2]
Cell Types: Testes were collected from 2-dpp mice. Tested Concentrations: 1 μM. Incubation Duration: 24 h. Experimental Results: Results in a VAD-like phenotype in the testis. Alone or in combination with ROL Dramatically diminished Stra8 expression. |
| Animal Protocol |
Animal/Disease Models: Six-month-old male New Zealand white rabbits[1].
Doses: 200 mg/kg. Route of Administration: Orally for 4, 8, and 16 weeks. Experimental Results: Resulted in marked suppression of testicular weight over time. Dramatically suppressed spermatogenesis. Dramatically reduces intratesticular concentrations of retinoic acid and Stra8 expression and very severely suppresses spermatogenesis and fertility. |
| References | |
| Additional Infomation |
WIN 18446 is a carboxamide that is 1,8-diaminooctane in which a hydrogen attached to each of the amino groups has been replaced by a dichloroacetyl group. Inhibitor of aldehyde dehydrogenase 1a2 (ALDH1a2). Inhibits the biosynthesis of retinoic acid from retinol in neonatal and adult murine testis. It down-regulates sex related genes in zebrafish. It has a role as an EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor. It is an organochlorine compound and a secondary carboxamide. It is functionally related to a dichloroacetic acid and a 1,8-diaminooctane.
|
| Molecular Formula |
C12H20CL4N2O2
|
|---|---|
| Molecular Weight |
366.11
|
| Exact Mass |
364.027
|
| CAS # |
1477-57-2
|
| PubChem CID |
15134
|
| Appearance |
Solid powder
|
| Density |
1.3±0.1 g/cm3
|
| Boiling Point |
530.2±50.0 °C at 760 mmHg
|
| Melting Point |
118-120ºC
|
| Flash Point |
274.5±30.1 °C
|
| Vapour Pressure |
0.0±1.4 mmHg at 25°C
|
| Index of Refraction |
1.503
|
| LogP |
1.96
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
11
|
| Heavy Atom Count |
20
|
| Complexity |
261
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
FAOMZVDZARKPFJ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H20Cl4N2O2/c13-9(14)11(19)17-7-5-3-1-2-4-6-8-18-12(20)10(15)16/h9-10H,1-8H2,(H,17,19)(H,18,20)
|
| Chemical Name |
2,2-dichloro-N-[8-[(2,2-dichloroacetyl)amino]octyl]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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 (273.14 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7314 mL | 13.6571 mL | 27.3142 mL | |
| 5 mM | 0.5463 mL | 2.7314 mL | 5.4628 mL | |
| 10 mM | 0.2731 mL | 1.3657 mL | 2.7314 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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