| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Capsaicin (330 nM)-induced Ca2+ buildup was concentration-dependently reduced by JYL 1421 incubation for 5 minutes. At the lowest dose (5 nM), JYL 1421's inhibitory action became significant, and at 1 μM, the response was nearly completely abolished, with just 3.1 ± 0.65% of the initial Ca2+ influx caused by capsaicin being seen. The IC50 value of JYL 1421 is 8 nM. Meanwhile, capsaicin had a much lower effect, only producing 41.7% inhibition at 1 μM; nevertheless, this inhibition did not rise to 50% at 10 μM or higher [1].
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| ln Vivo |
After dripping 50 μL of capsaicin solution (10 μg/mL) into the rat's left eye, the animal wiped 12.9 ± 1.3 times in just three minutes. Rats' wiping behavior was not substantially affected by pretreatment with 0.4 or 1 mg/kg ip JYL 1421; however, the number of wiping movements was dose-dependently decreased with 2–5 mg/kg. A value of 4.6 mg/kg is the ID50. Rats without treatment had a mean arterial pressure of 109.9±4.2 Hgmm (n=6). When 1 and 2 μg/kg capsaicin were injected intravenously, the subjects' blood pressure temporarily dropped to 47.4±4.7 and 59.6±4.2 Hgmm, respectively (n=6). In both cases, JYL 1421 did not result in hypotension (0.4 and 1.6 mg/kg). The requirement for greater capsaicin dosages to produce reflex hypotension after JYL 1421 administration than before to treatment indicates that JYL 1421 dose-dependently suppresses the drops in blood pressure that capsaicin causes. Even at dosages as high as 2 mg/kg, capsaicin is unable to substantially prevent capsaicin-induced hypotension [1].
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| References |
| Molecular Formula |
C20H26FN3O2S2
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|---|---|
| Molecular Weight |
423.57
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| Exact Mass |
423.145
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| CAS # |
401907-26-4
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| PubChem CID |
10295883
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
546.6±60.0 °C at 760 mmHg
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| Flash Point |
284.4±32.9 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.609
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| LogP |
3.27
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
28
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| Complexity |
608
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DUHBVFMCIJLUJX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H26FN3O2S2/c1-20(2,3)16-8-5-14(6-9-16)12-22-19(27)23-13-15-7-10-18(17(21)11-15)24-28(4,25)26/h5-11,24H,12-13H2,1-4H3,(H2,22,23,27)
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| Chemical Name |
1-[(4-tert-butylphenyl)methyl]-3-[[3-fluoro-4-(methanesulfonamido)phenyl]methyl]thiourea
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| Synonyms |
JYL-1421; JYL 1421; JYL1421
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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 (~236.09 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.90 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), suspension 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 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 (5.90 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 25.0 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: ≥ 2.5 mg/mL (5.90 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 | 2.3609 mL | 11.8044 mL | 23.6088 mL | |
| 5 mM | 0.4722 mL | 2.3609 mL | 4.7218 mL | |
| 10 mM | 0.2361 mL | 1.1804 mL | 2.3609 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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