LY3526318
Based on 1 Customer Validation
LY3526318 is an orally active, selective TRPA1 antagonist (IC50=5-6μM). LY3526318 blocks TRPA1 channels, inhibits pain signal transduction mediated by the channel, and exerts analgesic activity. LY3526318 is mainly used in the research of chronic pain-related fields, such as diabetic peripheral neuropathy, chronic low back pain, and pain caused by osteoarthritis.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.92%
- CAS No.: 1889218-34-1
- 화학식: C23H19F3N10O4
- 분자량:556.46
-
보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
-
Biological Activity
-
Chemical Information
-
용액&용해도
- 순도&문서
- References
-
Help & FAQs
Biological Activity
|
TRPA1 |
LY3526318 blocks transient TRPA1 inward currents activated by Allyl Isothiocyanate (HY-B1515) with IC50 values of 13.5 nM, 55.7 nM, 7.6 nM, and 8.2 nM for TRPA1 channels in humans, rats, dogs, and cynomolgus monkeys, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1889218-34-1
-
Appearance Solid
-
분자량 556.46
-
화학식 C23H19F3N10O4
-
Color White to light yellow
-
SMILES
FC(F)(F)C1=NC=C(C=N1)C2=NC(NC([C@@H](N3C4=C(N=C3)N(C(N(C4=O)CC5=NC(C)=NO5)=O)C)C)=O)=CC=C2
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 80 mg/mL (143.77 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
순도&문서
-
Data Sheet (272 KB)
-
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)
-
Handling Instructions (2659 KB)
References
[1]. Bamps D, et al. TRPA1 Antagonist LY3526318 Inhibits the Cinnamaldehyde-Evoked Dermal Blood Flow Increase: Translational Proof of Pharmacology. Clin Pharmacol Ther. 2023 Nov;114(5):1093-1103. [Content Brief]
[2]. Broad LM, et al. Preclinical and clinical evaluation of a novel TRPA1 antagonist LY3526318. Pain. 2025 Apr 18. [Content Brief]
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 | 1.7971 mL | 8.9854 mL | 17.9707 mL | 44.9269 mL |
| 5 mM | 0.3594 mL | 1.7971 mL | 3.5941 mL | 8.9854 mL | |
| 10 mM | 0.1797 mL | 0.8985 mL | 1.7971 mL | 4.4927 mL | |
| 15 mM | 0.1198 mL | 0.5990 mL | 1.1980 mL | 2.9951 mL | |
| 20 mM | 0.0899 mL | 0.4493 mL | 0.8985 mL | 2.2463 mL | |
| 25 mM | 0.0719 mL | 0.3594 mL | 0.7188 mL | 1.7971 mL | |
| 30 mM | 0.0599 mL | 0.2995 mL | 0.5990 mL | 1.4976 mL | |
| 40 mM | 0.0449 mL | 0.2246 mL | 0.4493 mL | 1.1232 mL | |
| 50 mM | 0.0359 mL | 0.1797 mL | 0.3594 mL | 0.8985 mL | |
| 60 mM | 0.0300 mL | 0.1498 mL | 0.2995 mL | 0.7488 mL | |
| 80 mM | 0.0225 mL | 0.1123 mL | 0.2246 mL | 0.5616 mL | |
| 100 mM | 0.0180 mL | 0.0899 mL | 0.1797 mL | 0.4493 mL |
Powered by Bioz