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.
For research use only. We do not sell to patients.
- Purity : 98.26%
- CAS No.: 132858-26-5
- Formula: C16H13ClN2O2S
- Molecular Weight:332.80
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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 specifically inhibits Hv1 with a half-maximal inhibitory concentration of 1 μM, without inhibiting other ion channels[1].
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].
YHV98-4 (20 μM) alleviates mitochondrial oxidative stress, restores energy metabolism, rescues defects in mitophagy and autophagy, reduces mtDNA leakage, and enhances the phagocytosis of BV2 microglia stimulated by PHF[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | Cmax | T1/2 |
|---|---|---|---|---|
| Mice[1] | 10 mg/kg | i.p. | 4 | 1.75 h |
In Vivo
YHV98-4 (10 mg/kg; i.p.) restores the impaired SHP-1-pAKT inflammatory signaling pathway in sensory neurons of CFA (HY-153808)-treated mice[3].
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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Molecular Weight 332.80
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Formula 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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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 (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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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ROS/oxidative-stress fluorescent staining
ROS/oxidative-stress fluorescent staining uses cell-permeant fluorogenic probes that become fluorescent after oxidation inside cells or tissues; commonly used examples include DCFH-DA/DCFDA for broad cellular oxidant detection, DHE for superoxide-related signal detection, MitoSOX for mitochondrial superoxide-related signal detection, and CellROX probes for oxidative-stress-associated fluorescence readouts. The assay detects probe oxidation rather than a single ROS species unless the probe and analysis method have been chemically validated for that species. DCFH-DA enters cells, is deacetylated by intracellular esterases to DCFH, and produces fluorescent DCF after oxidation, so the readout is used as an operational measure of total cellular oxidative stress rather than a species-specific ROS measurement. DHE and MitoSOX can report superoxide-related oxidation, but red fluorescence alone can include non-specific ethidium-like oxidation products; HPLC or optimized spectral approaches are
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Protocol for Water Maze
The Morris Water Maze is a rodent spatial learning and memory assay in which a mouse or rat swims in opaque water to find an escape platform; in the hidden-platform version, the animal cannot see the platform and must use distal extra-maze cues to learn its fixed spatial location. The assay primarily measures hippocampus-dependent spatial learning during acquisition trials and spatial reference memory during probe trials after platform removal; readouts include escape latency, swim path length, swim speed, quadrant occupancy, platform-site crossings, and proximity to the former platform location.
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Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
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Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
[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]
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 | 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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