KB-5492 free base

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KB-5492 free base

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

113594-64-2

KB-5492 free base 是一种有效的和选择性的sigma受体抑制剂，抑制 [³H]1,3-di(2-tolyl)guanidine (DTG) 与sigma受体结合，IC₅₀值为 3.15 μM。KB-5492 free base 是一种抗溃疡剂。

生物活性

KB-5492 free base is a potent and selective inhibitor ofsigma receptor, inhibits specific [³H]1,3-di(2-tolyl)guanidine (DTG) binding to thesigma receptorwith anIC₅₀of 3.15 μM. KB-5492 free base is an anti-ulcer agent^[1]^[2].

IC₅₀& Target

IC50: 3.15 μM (sigma receptor)^[1]

体外研究
(In Vitro)

KB-5492 (0.001-100 μM) free base inhibits specific [³H]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 in⁵¹Cr release from gastric epithelial cells^[2].

体内研究
(In Vivo)

KB-5492 (200 mg/kg; p.o.) free base prevents macroscopic lesions in the gastric mucosa^[2].

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.

分子量

430.49

性状

Solid

Formula

C₂₃H₃₀N₂O₆

CAS 号

113594-64-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL(232.29 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。