| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
When CLP257 was added to HEK293-cl cells, there was no change in [Cl−]i, suggesting that NKCC1, KCC1, KCC3, or KCC4 were not active. Oocytes treated with 200 nM CLP257 prior to incubation showed a 61% increase in KCC2 transport activity; other CCCs did not exhibit any changes. Additionally, there was observed to be functional, dose-dependent antagonistic relationship between CLP257 and the newly identified KCC2 antagonist VU024055119. CLP257 (50 μM) had an impact on CHO cells transduced with recombinant α1β2η2 GABAA receptors that was less than 0.2% of that caused by 5 μM muscimol, suggesting that CLP257 has very little agonist activity at GABAA receptors [1].
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| References |
[1]. Gagnon M, et al. Chloride extrusion enhancers as novel therapeutics for neurological diseases. Nat Med. 2013 Nov;19(11):1524-8.
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| Molecular Formula |
C14H14FN3O2S
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|---|---|
| Molecular Weight |
307.34326505661
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| Exact Mass |
307.08
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| Elemental Analysis |
C, 54.71; H, 4.59; F, 6.18; N, 13.67; O, 10.41; S, 10.43
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| CAS # |
1181081-71-9
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| Appearance |
Solid powder
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| SMILES |
C1CCN(NC1)C2=NC(=O)/C(=C/C3=C(C=C(C=C3)F)O)/S2
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| InChi Key |
SKCADXVKQRCWTR-GHXNOFRVSA-N
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| InChi Code |
InChI=1S/C14H14FN3O2S/c15-10-4-3-9(11(19)8-10)7-12-13(20)17-14(21-12)18-6-2-1-5-16-18/h3-4,7-8,16,19H,1-2,5-6H2/b12-7-
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| Chemical Name |
(5Z)-2-(diazinan-1-yl)-5-[(4-fluoro-2-hydroxyphenyl)methylidene]-1,3-thiazol-4-one
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| Synonyms |
CLP-257; CLP 257; CLP257
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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) |
DMSO : ~17.86 mg/mL (~58.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.79 mg/mL (5.82 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 17.9 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: 1.79 mg/mL (5.82 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 17.9 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2537 mL | 16.2686 mL | 32.5373 mL | |
| 5 mM | 0.6507 mL | 3.2537 mL | 6.5075 mL | |
| 10 mM | 0.3254 mL | 1.6269 mL | 3.2537 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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