sEH inhibitor-8

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sEH inhibitor-8

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。

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

sEH inhibitor-8 (compound 15) 是sEH的抑制剂，对人和鼠 sEH 的IC₅₀值为分别为 0.4 和 1.0 nM。sEH inhibitor-8 抑制机械超敏反应在小鼠模型中。sEH inhibitor-8 可用于炎症的研究。

生物活性

sEH inhibitor-8 (compound 15) is asEHinhibitor withIC₅₀values of 0.4 and 1.0 nM for human sEH and murine sEH, respectively. sEH inhibitor-8 inhibits mechanical hypersensitivity in mouse models. sEH inhibitor-8 can be used for the research of inflammation^[1].

IC₅₀& Target

CYP3A4

1 μM (IC₅₀)

CYP2C9

34 μM (IC₅₀)

CYP2C19

38 μM (IC₅₀)

体外研究
(In Vitro)

sEH inhibitor-8 (0-1 μM) inhibits human sEH and murine sEH with IC₅₀values of 0.4 and 1.0 nM, respectively^[1].
sEH inhibitor-8 (0-100 μM) shows inhibition to cytochrome with IC₅₀values of 34, 38 and 1 μM for CYP 2C9, CYP 2C19 and CYP 3A4, respectively^[1].

Western Blot Analysis^[1]

Cell Line:	HEK293T cell line
Concentration:	100 μM
Incubation Time:	30 min
Result:	Showed no significant effects on the level of EPHX1, EPHX2, MAPK38 and VEGFR.

体内研究
(In Vivo)

sEH inhibitor-8 (1.25-5 mg/kg; s.c. once) inhibits mechanical hypersensitivity in vivo^[1].
1.19Pharmacokinetic Properties of sEH inhibitor-8 in Mice^[1].

	Mice SC 5 mg/kg
HL (h)	3.42
T_max(h)	0.75
C_max(μg/mL)	1.2
AUClast (μg*h/mL)	2.4
AUCINF (μg*h/mL)	2.5

Animal Model:	Mice with capsaicin-induced secondary mechanical hypersensitivity^[1]
Dosage:	1.25, 2.5 and 5 mg/kg
Administration:	Subcutaneous injection; 0.312, 0.625 and 1.25 mg/kg once
Result:	Dose-dependently inhibited mechanical hypersensitivity with a much higher potency than AS2586114 and showed a full reversal of sensory gain with a dose of 5 mg/kg.

分子量

486.05

Formula

C₂₇H₃₆ClN₃O₃

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.