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KB-5492 anhydrous

Catalog No.GC60216

KB-5492 무수물은 시그마 수용체의 강력하고 선택적인 억제제이며 3.15μM의 IC50으로 시그마 수용체에 대한 특이적인 [3H]1,3-디(2-톨릴)구아니딘(DTG) 결합을 억제합니다.

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KB-5492 anhydrous Chemical Structure

Cas No.: 129200-10-8

Size 가격 재고 수량
1mg
US$162.00
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5mg
US$387.00
재고 있음

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Sample solution is provided at 25 µL, 10mM.

Description of KB-5492 anhydrous

KB-5492 anhydrous is a potent and selective inhibitor of sigma receptor, inhibits specific [3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 anhydrous is an anti-ulcer agent[1][2].

KB-5492 (0.001-100 μM) inhibits specific [3H]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 51Cr release from gastric epithelial cells[2].

KB-5492 (200 mg/kg; p.o.) prevents macroscopic lesions in the gastric mucosa[2]. Animal Model: Male Sprague-Dawley rats weighing 210-240 g are induced gastric mucosal damage[2]

[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.

Chemical Properties of KB-5492 anhydrous

Cas No. 129200-10-8 SDF
Canonical 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
Formula C27H34N2O10 M.Wt 546.57
Solubility DMSO: 250 mg/mL (457.40 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of KB-5492 anhydrous

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1 mg 5 mg 10 mg
1 mM 1.8296 mL 9.148 mL 18.2959 mL
5 mM 0.3659 mL 1.8296 mL 3.6592 mL
10 mM 0.183 mL 0.9148 mL 1.8296 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Average Rating: 5 ★★★★★ (Based on Reviews and 20 reference(s) in Google Scholar.)

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