UKH-1114
Based on 1 Customer Validation
UKH-1114 is a selective TMEM97 (a sigma-2 receptor) agonist with a Ki values of 1279 and 46 nM for σ1R and σ2R/TMEM97, respectively. UKH-1114 exhibits exceptional selectivity with negligible affinity for over 50 other receptors and channels. UKH-1114 effectively relieves spared nerve injury (SNI)-induced mechanical hypersensitivity with a long-lasting duration and without motor impairment. UKH-1114 can be used for neuropathic pain research.
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- Purity : 99.88%
- CAS No.: 2113664-14-3
- 화학식: C22H24F3NO
- 분자량:375.43
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보관: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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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
[1]|
σ1R 1279 nM (Ki) |
σ2 46 nM (Ki) |
In Vivo
UKH-1114 (10 mg/kg, i.v., once, lasting for 0-164 h) alleviates neuropathic pain without motor impairment in the SNI mice model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57Bl6/J mice (underwent SNI surgery)[1]
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Dosage:10 µg
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Administration:i.t. once, lasting for 1, 3, 24, 48 and 72 h
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Result:Resulted a significant anti-mechanical hypersensitivity effect at 24-72 h.
Exerted anti-mechanical hypersensitivity effect abolished by SAS-0132 (HY-119386) (a σ2R/Tmem97 antagonist).
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Animal Model:Male C57Bl6/J mice (underwent SNI surgery)[1]
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Dosage:10 mg/kg
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Administration:i.v., once, lasting for1, 3, 24, 48, 72, 96 and 164 h
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Result:Resulted a significant anti-mechanical hypersensitivity effect at 24 and 48 h.
Had no effect on motor performance.
Chemical Information
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CAS No. 2113664-14-3
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Appearance Solid
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분자량 375.43
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화학식 C22H24F3NO
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Color Off-white to light yellow
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SMILES
OCCCN1CCCC2C3=CC=C(C4=CC=C(C(F)(F)F)C=C4)C=C3C1C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (266.36 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 (6.66 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.
순도&문서
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Data Sheet (272 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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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 |
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| DMSO | 1 mM | 2.6636 mL | 13.3181 mL | 26.6361 mL | 66.5903 mL |
| 5 mM | 0.5327 mL | 2.6636 mL | 5.3272 mL | 13.3181 mL | |
| 10 mM | 0.2664 mL | 1.3318 mL | 2.6636 mL | 6.6590 mL | |
| 15 mM | 0.1776 mL | 0.8879 mL | 1.7757 mL | 4.4394 mL | |
| 20 mM | 0.1332 mL | 0.6659 mL | 1.3318 mL | 3.3295 mL | |
| 25 mM | 0.1065 mL | 0.5327 mL | 1.0654 mL | 2.6636 mL | |
| 30 mM | 0.0888 mL | 0.4439 mL | 0.8879 mL | 2.2197 mL | |
| 40 mM | 0.0666 mL | 0.3330 mL | 0.6659 mL | 1.6648 mL | |
| 50 mM | 0.0533 mL | 0.2664 mL | 0.5327 mL | 1.3318 mL | |
| 60 mM | 0.0444 mL | 0.2220 mL | 0.4439 mL | 1.1098 mL | |
| 80 mM | 0.0333 mL | 0.1665 mL | 0.3330 mL | 0.8324 mL | |
| 100 mM | 0.0266 mL | 0.1332 mL | 0.2664 mL | 0.6659 mL |
UKH-1114 Related Classifications
HY-117731 Related Classifications
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