| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
Kv7.4 and Kv7.5 are inhibited by flindokalner (BMS-204352) (10 μM), with Kis values of 230 and 605 μM, respectively [1]. Flindokalner (1-10 μM) has a dose-dependent inhibition of Ca2+ currents, with a Kd of 6 μM and a Hill coefficient of 1.33. In freshly isolated rat ventricular myocytes, flindokalner directly blocks cardiac L-type Ca2+ channels without influencing BKCa channels or intracellular signaling [2].
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| ln Vivo |
The dose-dependent anxiolytic effects of flindokalner (BMS-204352) (3-30 mg/kg; i.p.) are reported [1]. Male Wistar rats were given shocks as part of a conditioned anxiety model, and Flindokalner (3–60 mg/kg; i.p.) produced anxiolytic effects [1].
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| Animal Protocol |
Animal/Disease Models: Female NMRI or male C57 mouse (20-25 g) (anxiety model) [1]
Doses: intraperitoneal (ip) injection: 3, 10, 30 mg/kg Experimental Results: The time spent in the open area was significant and There was a dose-dependent increase in the latency to enter the open field and increased the number of entries into the open field in the zero maze. |
| References |
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| Molecular Formula |
C16H10CLF4NO2
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|---|---|
| Molecular Weight |
359.7
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| Exact Mass |
359.034
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| Elemental Analysis |
C, 53.43; H, 2.80; Cl, 9.86; F, 21.13; N, 3.89; O, 8.90
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| CAS # |
187523-35-9
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| PubChem CID |
214350
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| Appearance |
White to off-white solid powder
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| Density |
1.5g/cm3
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| Boiling Point |
436.9ºC at 760mmHg
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| Flash Point |
218ºC
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| Vapour Pressure |
7.82E-08mmHg at 25°C
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| Index of Refraction |
1.574
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| LogP |
4.67
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
24
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| Complexity |
503
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| Defined Atom Stereocenter Count |
1
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| SMILES |
ClC1C([H])=C([H])C(=C(C=1[H])[C@@]1(C(N([H])C2C([H])=C(C(F)(F)F)C([H])=C([H])C1=2)=O)F)OC([H])([H])[H]
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| InChi Key |
ULYONBAOIMCNEH-HNNXBMFYSA-N
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| InChi Code |
InChI=1S/C16H10ClF4NO2/c1-24-13-5-3-9(17)7-11(13)15(18)10-4-2-8(16(19,20)21)6-12(10)22-14(15)23/h2-7H,1H3,(H,22,23)/t15-/m0/s1
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| Chemical Name |
(3S)-3-(5-chloro-2-methoxyphenyl)-3-fluoro-6-(trifluoromethyl)-1H-indol-2-one
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| Synonyms |
BMS 204352; BMS-204352; Flindokalner
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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 : ~100 mg/mL (~278.01 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.95 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: ≥ 2.5 mg/mL (6.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 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 | 2.7801 mL | 13.9005 mL | 27.8009 mL | |
| 5 mM | 0.5560 mL | 2.7801 mL | 5.5602 mL | |
| 10 mM | 0.2780 mL | 1.3900 mL | 2.7801 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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