| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Sulazepam acts on the central nervous system by enhancing the effect of gamma-aminobutyric acid (GABA) at GABA-A receptors. Additionally, it functions as a selective agonist for the ovarian cancer G protein-coupled receptor (OGR1). The compound is also described as a Gs-biased OGR1 agonist, selectively activating this receptor.
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| ln Vitro |
Sulazepam is a selective OGR1 agonist. In vitro studies have characterized its biased signaling at the proton-sensing receptor OGR1. As a benzodiazepine, it potentiates GABA-induced chloride currents at GABA-A receptors, although specific potency values (EC50/IC50) are not extensively detailed in standard reference sources.
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| ln Vivo |
In male and female wild-type C57BL/6 mice (AHR) development (8–10 weeks of age), sulazepam (3.2 mg/kg, 25 µL, administered by the intranasal route approximately 30 minutes before HDM challenge; five days per week for three weeks) inhibits airway hyperresponsiveness, but not in age-matched OGR1KO mice (C57BL/6 background) with house dust mite (HDM) allergen (25 μg; intranasally) [1].
Sulazepam (3.2 mg/kg in 25 µL via intranasal route, ~30 min before house dust mite challenge, 5 days a week for three consecutive weeks) inhibits the development of airway hyperresponsiveness (AHR) in male and female wild-type C57BL/6 mice (8-10 wk old), but not in age-matched OGR1 knockout mice. This demonstrates that its in vivo effect on AHR is OGR1-dependent. |
| Enzyme Assay |
Sulazepam's receptor binding affinity can be assessed using standard radioligand binding assays with membrane preparations from cells expressing recombinant human OGR1 or GABA-A receptors. Competition binding experiments are performed with increasing concentrations of sulazepam against a fixed concentration of a high-affinity radioligand specific for the target receptor. Non-specific binding is determined in the presence of an excess of a reference compound. Samples are incubated at room temperature for a defined period, followed by rapid filtration through glass fiber filters, and bound radioactivity is measured by scintillation counting to calculate Ki or IC50 values.
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| Cell Assay |
The functional activity of sulazepam at GABA-A receptors can be evaluated in vitro using cell lines (such as HEK293 or CHO cells) stably or transiently expressing recombinant GABA-A receptor subunits. Cells are loaded with a calcium-sensitive fluorescent dye (e.g., Fluo-4 AM) and intracellular calcium changes upon GABA stimulation in the presence or absence of sulazepam are measured using a fluorescence microplate reader. Potentiation of GABA-induced responses indicates positive allosteric modulator activity. For OGR1 activity, cells expressing OGR1 are stimulated with sulazepam and downstream signaling (e.g., cAMP accumulation) is quantified.
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| Animal Protocol |
In a mouse model of airway hyperresponsiveness, sulazepam is administered intranasally at 3.2 mg/kg in 25 µL volume, 30 minutes prior to allergen challenge with house dust mite (25 μg, intranasally). This treatment is given 5 days a week for three consecutive weeks. Airway hyperresponsiveness is then assessed by measuring airway resistance in response to increasing doses of methacholine in wild-type and OGR1 knockout mice to determine the OGR1-dependent effects of the compound.
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| ADME/Pharmacokinetics |
Sulazepam is a benzodiazepine derivative that is metabolized into active compounds, including diazepam. The compound is soluble in DMSO. Specific pharmacokinetic parameters such as half-life, volume of distribution, clearance, and oral bioavailability are not extensively detailed in standard reference sources, though as a benzodiazepine, it is expected to be well-absorbed and extensively metabolized in the liver.
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| Toxicity/Toxicokinetics |
The acute toxicity profile of sulazepam is not extensively detailed in standard reference sources. As a benzodiazepine derivative, it is expected to exhibit central nervous system depressant effects at high doses, including sedation, ataxia, and respiratory depression. Long-term use is associated with risks of dependence and withdrawal symptoms. Specific LD50 values and organ-specific toxicity data are not readily available in the public domain.
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| References | |
| Additional Infomation |
Sulazepam (CAS# 2898-13-7) has a molecular weight of 300.80 and a purity of ≥98%. It has been investigated for potential in treating anxiety disorders and insomnia, though its clinical use is limited compared to other benzodiazepines due to metabolic considerations. Research has also explored its role in OGR1-dependent regulation of allergen-induced asthma phenotype. Synonyms include W 3676.
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| Molecular Formula |
C16H13CLN2S
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|---|---|
| Molecular Weight |
300.804
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| Exact Mass |
300.049
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| CAS # |
2898-13-7
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| Related CAS # |
Sulazepam-d5
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| PubChem CID |
17931
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.26g/cm3
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| Boiling Point |
429.4ºC at 760mmHg
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| Flash Point |
213.5ºC
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| Vapour Pressure |
1.4E-07mmHg at 25°C
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| Index of Refraction |
1.657
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| LogP |
3.455
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
403
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1C=CC(C2=NCC(=S)N(C)C3C=CC(=CC2=3)Cl)=CC=1
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| InChi Key |
MWGWTOPCKLQYEU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H13ClN2S/c1-19-14-8-7-12(17)9-13(14)16(18-10-15(19)20)11-5-3-2-4-6-11/h2-9H,10H2,1H3
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| Chemical Name |
7-chloro-1-methyl-5-phenyl-3H-1,4-benzodiazepine-2-thione
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| Synonyms |
W-3676; W 3676; Sulazepam
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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 |
| 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) |
DMSO : ~50 mg/mL (~166.22 mM)
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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 | 3.3245 mL | 16.6223 mL | 33.2447 mL | |
| 5 mM | 0.6649 mL | 3.3245 mL | 6.6489 mL | |
| 10 mM | 0.3324 mL | 1.6622 mL | 3.3245 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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