Libvatrep
Based on 1 Customer Validation
Libvatrep (SAF312) is a non-competitive TRPV1 antagonist with an IC50 of 0.35-0.69 µM in HEK293T cells. It binds to the vanilloid pocket and an allosteric site, preventing S4/S5 conformational changes and channel opening. Libvatrep can be used for research on ocular surface pain and eye pain after photorefractive keratectomy.
For research use only. We do not sell to patients.
- Purity : 99.54%
- CAS No.: 871814-52-7
- Formula: C18H15N3O2
- Molecular Weight:305.33
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
TRPV1 0.35-0.69 μM (IC50) |
In Vitro
SAF312 (3 μM; 30 s) inhibits pH 5-stimulated hTRPV1 currents in HEK293T cells with an IC50 of 0.69 µM[1].
SAF312 (10 μL; 10 min) is a potent antagonist of hTRPV1 in CHO-hTRPV1 cells, inhibiting calcium influx induced by multiple stimuli (low pH 5.5 MES, AEA, capsaicin, NADA, PKC, and noxious heat) with IC50 values ranging from 5 nM to 57 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 871814-52-7
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Appearance Solid
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Molecular Weight 305.33
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Formula C18H15N3O2
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Color White to light yellow
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SMILES
N#CC1=CC=C(N2C(C(C)C)=NC3=C(C=CC(O)=C3)C2=O)C=C1
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Synonyms
SAF312; Vanilloid receptor antagonist 1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (327.51 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)
In Vivo:
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 (8.19 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 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.
In Vivo Dissolution Calculator
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.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
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 | 3.2751 mL | 16.3757 mL | 32.7515 mL | 81.8786 mL |
| 5 mM | 0.6550 mL | 3.2751 mL | 6.5503 mL | 16.3757 mL | |
| 10 mM | 0.3275 mL | 1.6376 mL | 3.2751 mL | 8.1879 mL | |
| 15 mM | 0.2183 mL | 1.0917 mL | 2.1834 mL | 5.4586 mL | |
| 20 mM | 0.1638 mL | 0.8188 mL | 1.6376 mL | 4.0939 mL | |
| 25 mM | 0.1310 mL | 0.6550 mL | 1.3101 mL | 3.2751 mL | |
| 30 mM | 0.1092 mL | 0.5459 mL | 1.0917 mL | 2.7293 mL | |
| 40 mM | 0.0819 mL | 0.4094 mL | 0.8188 mL | 2.0470 mL | |
| 50 mM | 0.0655 mL | 0.3275 mL | 0.6550 mL | 1.6376 mL | |
| 60 mM | 0.0546 mL | 0.2729 mL | 0.5459 mL | 1.3646 mL | |
| 80 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0235 mL | |
| 100 mM | 0.0328 mL | 0.1638 mL | 0.3275 mL | 0.8188 mL |
Libvatrep Related Classifications
HY-114017 Related Classifications
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Keywords
- Libvatrep
- 871814-52-7
- SAF312
- Vanilloid receptor antagonist 1
- SAF 312
- SAF-312
- Vanilloid receptor antagonist1
- Vanilloid receptor antagonist 1
- Vanilloid receptor antagonist-1
- TRP Channel
- HEK293T cells
- CHO-hTRPV1 cells
- TRPV1
- NADA
- noxious heat
- calcium influx
- TRPM8
- capsaicin
- vanilloid pocket
- allosteric site
- Inhibitor
- inhibitor
- inhibit