2. Neuronal Signaling
  3. Sigma Receptor
  4. UKH-1114

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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UKH-1114

UKH-1114 Chemical Structure

CAS No. : 2113664-14-3

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Description

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[1].

IC50 & Target[1]

σ1R

1279 nM (Ki)

σ2

46 nM (Ki)

In Vivo

UKH-1114 (10 µg, i.t. once, lasting for 1-72 h) elicits pronounced and sustained antinociceptive effects, by acting as an agonist at σ2R/Tmem97 in the SNI mice model[1].
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.

Animal Model: Male C57Bl6/J mice (underwent SNI surgery)[1]
Dosage: 10 µg
Administration: i.t. once, lasting for 1, 3, 24, 48 and 72 h
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).
Animal Model: Male C57Bl6/J mice (underwent SNI surgery)[1]
Dosage: 10 mg/kg
Administration: i.v., once, lasting for1, 3, 24, 48, 72, 96 and 164 h
Result: Resulted a significant anti-mechanical hypersensitivity effect at 24 and 48 h.
Had no effect on motor performance.
Molecular Weight

375.43

Formula

C22H24F3NO
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

OCCCN1CCCC2C3=CC=C(C4=CC=C(C(F)(F)F)C=C4)C=C3C1C2
Shipping

Room temperature in continental US; may vary elsewhere.
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 (266.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6636 mL 13.3181 mL 26.6361 mL
5 mM 0.5327 mL 2.6636 mL 5.3272 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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% 
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%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.88%

SDS (251 KB)

COA (246 KB)

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 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
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UKH-1114 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

UKH-11142113664-14-3UKH1114UKH 1114Sigma Receptormechanical hypersensitivitylong-lasting durationmotor impairmentneuropathic painInhibitorinhibitorinhibit

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