| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
KB-5492 free base targets the sigma receptor, a class of proteins that have been implicated in various physiological processes, including modulation of neurotransmitter release, lipid metabolism, and cell survival. The compound acts as a selective inhibitor, as demonstrated by its ability to displace the sigma receptor ligand DTG. The specific sigma receptor subtype (e.g., sigma-1 or sigma-2) targeted by KB-5492 is not specified in the available sources. Its anti-ulcer activity is thought to be related to its sigma receptor inhibition.
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| ln Vitro |
In a concentration-dependent manner, KB-5492 (0.001-100 μM) free base inhibits selective [3H]DTG binding [1]. The release of 51Cr from gastric epithelial cells is considerably and concentration-dependently inhibited by KB-5492 (0.1-1 mM) free base [2]. This effect is observed both in response to acidified aspirin and ethanol.
In vitro, KB-5492 free base inhibits specific [³H]DTG binding to sigma receptors in a concentration-dependent manner at concentrations ranging from 0.001 to 100 μM. Additionally, at concentrations of 0.1-1 mM, it significantly and concentration-dependently prevents the ethanol- and acidified aspirin-induced increases in ⁵¹Cr release from gastric epithelial cells. This indicates a protective effect on gastric epithelial cells in vitro, which is consistent with its reported anti-ulcer activity. |
| ln Vivo |
KB-5492 (200 mg/kg; oral) free base inhibits macroscopic lesions of the gastric mucosa [2].
In vivo, KB-5492 free base has been shown to prevent macroscopic lesions in the gastric mucosa. In a study using male Sprague-Dawley rats (weighing 210-240 g) with induced gastric mucosal damage, oral administration of KB-5492 at a dose of 200 mg/kg reduced lesion length compared to control. It prevented deep mucosal lesions and exfoliation of surface epithelial cells. These findings support its potential as an anti-ulcer agent. |
| Enzyme Assay |
A cell-free assay for KB-5492 free base involves measuring its ability to inhibit the binding of [³H]1,3-di(2-tolyl)guanidine (DTG) to sigma receptors. In this assay, sigma receptor preparations (typically from guinea-pig brain) are incubated with [³H]DTG and varying concentrations of KB-5492. The amount of [³H]DTG bound to the receptors is measured, and the concentration of KB-5492 required to inhibit 50% of specific binding (IC₅₀) is determined. For KB-5492, this IC₅₀ is 3.15 μM. This assay confirms the compound's affinity for the sigma receptor.
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| Cell Assay |
In vitro cellular experiments with KB-5492 free base have evaluated its protective effects on gastric epithelial cells. In one study, gastric epithelial cells were exposed to ethanol or acidified aspirin to induce damage, measured by ⁵¹Cr release. Cells were treated with KB-5492 at concentrations of 0.1-1 mM, and the compound significantly and concentration-dependently prevented the increase in ⁵¹Cr release, indicating protection against cell damage. This cell-based assay demonstrates the compound's cytoprotective effects in vitro.
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| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats, body weight 210-240 g, induced gastric mucosal damage [2]
Doses: 200 mg/kg Route of Administration: po (oral gavage) Experimental Results: Compared with the control, the lesion length was shortened. Prevent deep mucosal lesions and surface epithelial cell shedding. In vivo experiments with KB-5492 free base were conducted in male Sprague-Dawley rats (210-240 g) with induced gastric mucosal damage. Gastric mucosal damage was induced using agents such as ethanol or acidified aspirin. KB-5492 was administered orally at a dose of 200 mg/kg. The animals were then evaluated for macroscopic lesions in the gastric mucosa. The compound reduced lesion length and prevented deep mucosal lesions and surface epithelial cell exfoliation compared to the control group. |
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties of KB-5492 free base are not detailed in the available sources. The compound is described as orally available, suggesting it has sufficient oral bioavailability for in vivo studies. In animal experiments, it was administered at a dose of 200 mg/kg via oral gavage. General storage recommendations include keeping the powder at -20°C for up to 3 years or at 4°C for up to 2 years. Solutions should be stored at -80°C for up to 6 months or at -20°C for up to 1 month.
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| Toxicity/Toxicokinetics |
Specific toxicity data for KB-5492 free base are not provided in the available sources. The compound is described as an anti-ulcer agent and has been tested in animal models at a dose of 200 mg/kg without reported adverse effects in the described studies. However, detailed toxicological profiles, including acute or chronic toxicity studies, are not available from the provided references. As with all research compounds, it is intended for research use only and not for human consumption.
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| References |
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| Additional Infomation |
See also: KB 5492 (Notes moved to).
KB-5492 free base (CAS: 113594-64-2) is a research compound with anti-ulcer activity that functions as a selective sigma receptor inhibitor. Its molecular formula is C₂₃H₃₀N₂O₆ with a molecular weight of 430.49. The compound is also known as KB-5492 and is available in its free base form. It has been studied for its potential in treating gastric lesions and regulating gastric secretion. Its mechanism of action is believed to be related to sigma receptor inhibition. The compound is not an approved drug and has not undergone clinical trials; it is strictly for research purposes. |
| Molecular Formula |
C23H30N2O6
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|---|---|
| Molecular Weight |
430.494
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| Exact Mass |
430.21
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| CAS # |
113594-64-2
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| Related CAS # |
KB-5492 anhydrous;129200-10-8
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| PubChem CID |
131083
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| Appearance |
White to off-white solid powder
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
31
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| Complexity |
520
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1C(OC)=C(OC)C=C(CN2CCN(CC(OC3=CC=C(OC)C=C3)=O)CC2)C=1
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| InChi Key |
RVYZAZTXLLAVGZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H30N2O6/c1-27-18-5-7-19(8-6-18)31-22(26)16-25-11-9-24(10-12-25)15-17-13-20(28-2)23(30-4)21(14-17)29-3/h5-8,13-14H,9-12,15-16H2,1-4H3
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| Chemical Name |
(4-methoxyphenyl) 2-[4-[(3,4,5-trimethoxyphenyl)methyl]piperazin-1-yl]acetate
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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 : ~100 mg/mL (~232.29 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 | 2.3229 mL | 11.6147 mL | 23.2293 mL | |
| 5 mM | 0.4646 mL | 2.3229 mL | 4.6459 mL | |
| 10 mM | 0.2323 mL | 1.1615 mL | 2.3229 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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