[CAS NO. 113594-64-2] KB-5492freebase
PRODUCTS SPECIFICATIONS [113594-64-2]
DESCRIPTION [113594-64-2]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 430.49 |
| Molecular Formula | C23H30N2O6 |
| SMILES | O=C(OC1=CC=C(OC)C=C1)CN2CCN(CC3=CC(OC)=C(OC)C(OC)=C3)CC2 |
Summary
KB-5492 free base is a potent and selective inhibitor of sigma receptor , inhibits specific [ 3 H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC 50 of 3.15 μM. KB-5492 free base is an anti-ulcer agent [1] [2] .
IC50 & Target
IC50: 3.15 μM (sigma receptor) [1]
In Vitro
KB-5492 (0.001-100 μM) free base inhibits specific [
3
H]DTG binding in a concentration-dependent manner
[1]
.
KB-5492 (0.1-1 mM) free base significantly and concentration-dependently prevents the ethanol- and acidified aspirin-induced increases in
51
Cr release from gastric epithelial cells
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
KB-5492 (200 mg/kg; p.o.) free base prevents macroscopic lesions in the gastric mucosa [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Sprague-Dawley rats weighing 210-240 g are induced gastric mucosal damage [2] |
| Dosage: | 200 mg/kg |
| Administration: | Oral gavage |
| Result: |
Reduced the lesion length as compared with the control.
Prevented the deep mucosal lesions and exfoliation of surface epithelial cells. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 232.29 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
References
- [1] Harada Y, et, al. Receptor binding profiles of KB-5492, a novel anti-ulcer agent, at sigma receptors in guinea-pig brain. Eur J Pharmacol. 1994 May 2; 256(3): 321-8.
- [2] Morimoto Y, et, al. Effects of KB-5492, a new anti-ulcer agent, on ethanol- and acidified aspirin-induced gastric mucosal damage in vivo and in vitro. Jpn J Pharmacol. 1994 Jan; 64(1): 41-7.