YHV98-4
Based on 1 Customer Validation
YHV98-4 is a selective, blood-brain barrier-permeable Hv1 inhibitor with an IC50 of 0.7 μM. YHV98-4 reduces ROS production and restores the SHP-1-pAKT signaling pathway. YHV98-4 decreases the spread of hyperphosphorylated Tau protein. YHV98-4 alleviates inflammation and produces analgesic effects. YHV98-4 improves cognitive function in mouse models of Alzheimer's disease. YHV98-4 can be used in research related to inflammatory pain, neuropathic pain and Alzheimer's disease.
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- Pureté : 98.26%
- CAS No.: 132858-26-5
- Formule: C16H13ClN2O2S
- Masse moléculaire:332.80
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Stockage: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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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
Activité biologique
Description
IC50 & Target
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
0.7 μM
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Inhibition of human Hv1-mediated outward proton currents in human embryonic kidney (HEK)-293T cells transiently expressing human Hv1 channel, measured via whole-cell patch-clamp electrophysiology at 20 mV under acidic intracellular solution (pH 6.0).
Inhibition of human Hv1-mediated outward proton currents in human embryonic kidney (HEK)-293T cells transiently expressing human Hv1 channel, measured via whole-cell patch-clamp electrophysiology at 20 mV under acidic intracellular solution (pH 6.0).
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35115667 |
In Vitro
YHV98-4 (0.1-10 μM) potently inhibits the Hv1 channel expressed in HEK-293T cells, with an IC50 of 0.7 μM[3].
YHV98-4 (20 μM) exhibits no inhibitory activity against hERG, KCNQ2, BK, Nav1.7, TRPV1, TRPA1 or VRAC channels, demonstrating high selectivity for Hv1[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | Cmax | T1/2 |
|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 4 | 1.75 h |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:3×Tg (male and female, 7 months old at study initiation, genetic model with both Aβ and tau pathology)[2]
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Dosage:10 mg/kg
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Administration:i.p.; daily; 30 days
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Result:Restored microglial morphological homeostasis, including increased segment branch number, segment terminal number, microglial area, and microglial volume compared to untreated 3×Tg mice.
Reduced hippocampal Hv1 intensity in Iba1-positive microglia.
Decreased hippocampal AT8 coverage and AT8 intensity (hyperphosphorylated tau marker), with no significant effect on 4G8-positive Aβ area.
Reduced hippocampal reactive oxygen species (ROS) levels measured by DHE fluorescence intensity.
Restored neuronal health with increased hippocampal NeuN intensity and MAP2 coverage.
Improved cognitive function as measured by reduced escape latency in MWM training trials, increased platform crossings and time spent in the target quadrant during MWM probe trials, higher discrimination index in the NOR test, and higher percentage of spontaneous alternation in the Y-maze test.
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Animal Model:C57BL/6 (male and female, 8-10 weeks old, disrupted inflammatory signaling in sensory neurons induced by CFA-induced chronic inflammatory pain)[3]
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Dosage:10 mg/kg
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Administration:i.p.
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Result:Reversed the CFA-induced decrease in total SHP-1 and pSHP-1 levels in DRG.
Reversed the CFA-induced increase in pAKT levels in DRG.
Chemical Information
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CAS No. 132858-26-5
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Appearance Solid
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Masse moléculaire 332.80
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Formule C16H13ClN2O2S
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Color White to off-white
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SMILES
O=C(NC1=CC=C(Cl)C=C1)CC2C(NC3=CC=CC=C3S2)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (300.48 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: ≥ 5 mg/mL (15.02 mM); Suspended solution
This protocol yields a suspended solution of ≥ 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 (50.0 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.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Furutani K, et al. Targeting Hv1 proton channel for pain control. Cell Res. 2022 May;32(5):419-420. [Content Brief]
[2]. Lin J, et al. Hv1 inhibition rescues AD pathology by restoring microglial mitochondrial function and enhancing mitochondrial transfer. Experimental & molecular medicine. 2025 Dec;57(12):2833-2851. [Content Brief]
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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 | 3.0048 mL | 15.0240 mL | 30.0481 mL | 75.1202 mL |
| 5 mM | 0.6010 mL | 3.0048 mL | 6.0096 mL | 15.0240 mL | |
| 10 mM | 0.3005 mL | 1.5024 mL | 3.0048 mL | 7.5120 mL | |
| 15 mM | 0.2003 mL | 1.0016 mL | 2.0032 mL | 5.0080 mL | |
| 20 mM | 0.1502 mL | 0.7512 mL | 1.5024 mL | 3.7560 mL | |
| 25 mM | 0.1202 mL | 0.6010 mL | 1.2019 mL | 3.0048 mL | |
| 30 mM | 0.1002 mL | 0.5008 mL | 1.0016 mL | 2.5040 mL | |
| 40 mM | 0.0751 mL | 0.3756 mL | 0.7512 mL | 1.8780 mL | |
| 50 mM | 0.0601 mL | 0.3005 mL | 0.6010 mL | 1.5024 mL | |
| 60 mM | 0.0501 mL | 0.2504 mL | 0.5008 mL | 1.2520 mL | |
| 80 mM | 0.0376 mL | 0.1878 mL | 0.3756 mL | 0.9390 mL | |
| 100 mM | 0.0300 mL | 0.1502 mL | 0.3005 mL | 0.7512 mL |
YHV98-4 Related Classifications
HY-W283930 Related Classifications
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Keywords
- YHV98-4
- 132858-26-5
- Tau Protein
- Reactive Oxygen Species (ROS)
- Proton Pump
- Akt
- SHP1
- PKB
- Protein kinase B
- Shp1
- PTPN6
- Src homology region 2 (SH-2) domain-containing phosphatase 1
- HEK-293T cells
- reactive oxygen species
- SHP-1-pAKT
- Hv1
- 3×Tg Alzheimer's disease mice
- μ-opioid receptor agonist
- Hydrogen voltage-gated channel 1
- BV2 microglial cells
- SHP-1-PI3K/AKT-CXCL1
- AD mouse models
- Inhibitor
- inhibitor
- inhibit