JYL 1421
Based on 1 Customer Validation
JYL 1421 is a TRPV1 receptor antagonist, with an IC50 of 8 nM.
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- Pureté: 99.54%
- CAS No.: 401907-26-4
- Formule: C20H26FN3O2S2
- Masse moléculaire:423.57
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
IC50: 8 nM (TRPV1 receptor)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
8 nM
Compound: 4
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Concentration required to antagonized capsaicin-induced calcium uptake at the transient receptor potential cation channel (subfamily V member 1) expressed in chinese hamster ovary cells
Concentration required to antagonized capsaicin-induced calcium uptake at the transient receptor potential cation channel (subfamily V member 1) expressed in chinese hamster ovary cells
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[PMID: 16134949] |
| CHO | IC50 |
54 nM
Compound: 4
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Concentration required to inhibit [3H]RTX radioligand binding towards transient receptor potential cation channel (subfamily V, member 1) expressed in chinese hamster ovary cells
Concentration required to inhibit [3H]RTX radioligand binding towards transient receptor potential cation channel (subfamily V, member 1) expressed in chinese hamster ovary cells
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[PMID: 16134949] |
Incubation with JYL 1421 for 5 min concentration-dependently inhibits the capsaicin (330 nM)-evoked Ca2+ accumulation. The inhibitory effect of the lowest concentration (5 nM) of JYL 1421 reaches the level of significance and 1 μM almost abolishes the response, only 3.1±0.65% of the first capsaicin-induced Ca2+ influx could be observed. The IC50 value is 8 nM for JYL 1421. Meanwhile, the effect of capsazepine is markedly smaller, it induces 41.7% inhibition in 1 μM concentration, but this inhibitory effect does not increase further in 10 μM and does not reach 50%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 401907-26-4
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Appearance Solid
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Masse moléculaire 423.57
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Formule C20H26FN3O2S2
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Color White to off-white
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SMILES
CS(=O)(NC1=CC=C(CNC(NCC2=CC=C(C(C)(C)C)C=C2)=S)C=C1F)=O
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Synonyms
SC 0030
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (236.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.90 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
Rats[1] Pretreatment with JYL 1421 (0.4, 1, 2, or 5 mg/kg) is performed i.p. 20 min before capsaicin administration. In control rats the solvent is injected in the same volume, in the reference group capsazepine (2 or 5 mg/kg) is administered i.p. The number of wiping movements in response to 50 μL capsaicin solution (10 μg/mL) drops into the left eye of male Wistar rats (180-220 g) is determined during 60 s after instillation. The body temperature is maintained at 37°C by a heating lamp. Drugs are administered through a cannula inserted into the right jugular vein. The pulmonary chemoreflex is evoked by rapid injections of capsaicin (1 and 2 μg/kg i.v.) separated by a 5 min interval. Thereafter JYL 1421 (0.4 and 1.6 mg/kg i.v.) is administered and 5 min later capsaicin injections are repeated at increasing doses until the magnitude of the control responses could be achieved. For quantitative analysis the area under the curve (AUC) of the capsaicin-induced hypotension is determined[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3609 mL | 11.8044 mL | 23.6088 mL | 59.0221 mL |
| 5 mM | 0.4722 mL | 2.3609 mL | 4.7218 mL | 11.8044 mL | |
| 10 mM | 0.2361 mL | 1.1804 mL | 2.3609 mL | 5.9022 mL | |
| 15 mM | 0.1574 mL | 0.7870 mL | 1.5739 mL | 3.9348 mL | |
| 20 mM | 0.1180 mL | 0.5902 mL | 1.1804 mL | 2.9511 mL | |
| 25 mM | 0.0944 mL | 0.4722 mL | 0.9444 mL | 2.3609 mL | |
| 30 mM | 0.0787 mL | 0.3935 mL | 0.7870 mL | 1.9674 mL | |
| 40 mM | 0.0590 mL | 0.2951 mL | 0.5902 mL | 1.4756 mL | |
| 50 mM | 0.0472 mL | 0.2361 mL | 0.4722 mL | 1.1804 mL | |
| 60 mM | 0.0393 mL | 0.1967 mL | 0.3935 mL | 0.9837 mL | |
| 80 mM | 0.0295 mL | 0.1476 mL | 0.2951 mL | 0.7378 mL | |
| 100 mM | 0.0236 mL | 0.1180 mL | 0.2361 mL | 0.5902 mL |
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