[CAS NO. 129200-10-8] KB-5492anhydrous
PRODUCTS SPECIFICATIONS [129200-10-8]
DESCRIPTION [129200-10-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 546.57 |
| Molecular Formula | C27H34N2O10 |
| SMILES | O=C(OC1=CC=C(OC)C=C1)CN2CCN(CC3=CC(OC)=C(OC)C(OC)=C3)CC2.O=C(O)/C=C/C(O)=O |
Summary
KB-5492 anhydrous 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 anhydrous is an anti-ulcer agent [1] [2] .
IC50 & Target
IC50: 3.15 μM (sigma receptor) [1]
In Vitro
KB-5492 (0.001-100 μM) inhibits specific [
3
H]DTG binding in a concentration-dependent manner
[1]
.
KB-5492 (0.1-1 mM) 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.) 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
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 250 mg/mL ( 457.40 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.8296 mL | 9.1480 mL | 18.2959 mL |
| 5 mM | 0.3659 mL | 1.8296 mL | 3.6592 mL |
| 10 mM | 0.1830 mL | 0.9148 mL | 1.8296 mL |
-
1.
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.81 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.81 mM); Clear solution
-
5.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.81 mM); Clear solution
-
6.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.81 mM); Clear solution
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.