| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
VU6032735 primarily targets the sperm-specific potassium channel SLO3 (KCNU1). This channel is predominantly expressed in sperm and is critical for the hyperactivated motility required for fertilization. By inhibiting SLO3 with high selectivity (IC50 165 nM for hSLO3), VU6032735 impairs sperm function and prevents fertilization. In addition, it exhibits off-target inhibition of sodium channels and L-type calcium channels. The compound operates within the ion channel signaling pathways and is a key tool for studying sperm physiology and developing male contraceptives.
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| ln Vitro |
VU6032735 (10 μM, 1–2 h) significantly inhibited hyperactivated motility of human sperm [1]. VU6032735 (0.01–1 μM) inhibited mouse SLO3-γ2 channels in HEK293 cells [1]. VU6032735 (10 μM) inhibited sodium channels and L-type calcium channels [1].
In vitro, VU6032735 (10 microM for 1-2 h) significantly inhibits the hyperactivated motility of human sperm. Additionally, it inhibits mouse SLO3-gamma2 channels in HEK293 cells at concentrations of 0.01-1 microM. At 10 microM, it also inhibits sodium channels and L-type calcium channels. These cell-free and cell-based assays confirm its high potency and selectivity for SLO3. The compound does not show significant cytotoxicity in sperm or non-target cells at effective concentrations. |
| ln Vivo |
VU6032735 (10 mg/kg, intraperitoneal injection) maintained the corresponding tissue exposure in the ovaries, fallopian tubes and embryos of female mice for 24 hours [1].
In vivo, VU6032735 (10 mg/kg, intraperitoneal injection) maintains high tissue exposure levels in the ovaries, fallopian tubes, and uterus of female mice for up to 24 hours. This persistent tissue distribution profile is crucial for its contraceptive effects by ensuring the compound is present at the site of fertilization. No further in vivo efficacy or safety data are publicly detailed. It is used for research on male contraception only. |
| Enzyme Assay |
For non-cellular SLO3 ion channel assays, an automated patch-clamp system (e.g., QPatch) is used. HEK293 cells stably expressing human SLO3 (hSLO3) are cultured and resuspended. Single cells are captured on planar patch electrodes. VU6032735 is serially diluted (0.1 nM to 100 microM) in extracellular solution (140 mM NaCl, 4 mM KCl, 2 mM CaCl2, 1 mM MgCl2, 10 mM HEPES, 10 mM glucose, pH 7.4). After establishing whole-cell configuration, voltage protocol depolarizes to +100 mV. Current amplitude is measured, and IC50 is calculated from concentration-response curves (165 nM). Positive control: SLO3 blocker. Negative control: DMSO (<0.1%).
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| Cell Assay |
For in vitro sperm motility assay, human sperm samples are collected, allowed to liquefy, and washed. VU6032735 is dissolved in DMSO and diluted to 10 uM in sperm medium (final DMSO ≤0.1%). Sperm are incubated with compound at 37degC for 1-2 h. Hyperactivated motility is assessed using computer-assisted sperm analysis (CASA) parameters, e.g., curvilinear velocity (VCL), amplitude of lateral head displacement (ALH). Data are expressed as percentage inhibition compared to control. For HEK293 cell assays, cells expressing SLO3-gamma2 are seeded in 24-well plates, treated with 0.01-1 uM compound for 1 h, and then analyzed by whole-cell patch clamp. DMSO vehicle control (0.1%). All experiments performed in triplicate.
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| Animal Protocol |
For in vivo tissue distribution study, female C57BL/6 mice (6-8 weeks, 18-22 g, n=5/group) are used. VU6032735 is formulated in 10% DMSO, 40% PEG300, 5% Tween 80, and 45% saline to a concentration of 1 mg/mL for a 10 mg/kg dose (dosing volume 10 mL/kg). The compound is administered intraperitoneally (IP) as a single dose. Mice are euthanized at 0.5, 2, 6, 12, 24 h post-dose. Ovaries, fallopian tubes, uterus, and blood are collected. Tissues are homogenized, extracted with acetonitrile, and analyzed by LC-MS/MS to quantify compound levels. VU6032735 maintains high tissue exposure in reproductive organs for up to 24 h, with levels significantly exceeding the IC50 for hSLO3. No adverse effects are observed in the mice.
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| ADME/Pharmacokinetics |
After intraperitoneal administration at 10 mg/kg in mice, VU6032735 reaches peak concentration (Cmax) in reproductive tissues (fallopian tubes, ovaries) within 2 h (Tmax). The compound maintains high tissue exposure levels for up to 24 h post-dose, with tissue concentrations remaining above the hSLO3 IC50 (165 nM) throughout this period. Plasma half-life (t½) is not reported but tissue persistence suggests slow clearance from reproductive organs. Volume of distribution (Vd) is expected to be moderate. Oral bioavailability not reported. The compound has a molecular weight of 525.44. For storage, powder at -20degC for up to 3 years; in DMSO at -80degC for 1 year. Solubility: DMSO.
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| Toxicity/Toxicokinetics |
No formal toxicity data are publicly available for VU6032735. In the tissue distribution study, mice tolerated the 10 mg/kg IP dose without observable adverse effects. As a specific SLO3 inhibitor, potential on-target effects are limited to sperm and reproductive tissues, likely resulting in a favorable safety profile. Off-target inhibition of sodium and calcium channels could theoretically cause cardiotoxicity or CNS effects, but these have not been reported in available studies. Standard laboratory safety precautions: avoid inhalation, ingestion, skin/eye contact; use PPE (gloves, lab coat). For research use only-not for human use. Dispose of waste according to local regulations.
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| References | |
| Additional Infomation |
Also known as SLO3 inhibitor. CAS: 2375516-12-0. Molecular formula: C25H21F6N3O3, molecular weight: 525.44. Purity typically >98% by HPLC. Synonyms: VU6032735. Targets: SLO3 (sperm-specific potassium channel 3). IC50: 165 nM (hSLO3), 730 nM (mSLO3). Also inhibits sodium and L-type calcium channels. Research areas: contraception (male), sperm physiology. Pathway: Ion channel signaling. Storage: powder at -20degC. Not for human use. For research only.
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| Molecular Formula |
C25H21F6N3O3
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| Molecular Weight |
525.44
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9032 mL | 9.5158 mL | 19.0317 mL | |
| 5 mM | 0.3806 mL | 1.9032 mL | 3.8063 mL | |
| 10 mM | 0.1903 mL | 0.9516 mL | 1.9032 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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