GPR84 antagonist 3

立即咨询

GPR84 antagonist 3

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

GPR84 antagonist 3 (compound 42) 是一种有效的GPR84(G 蛋白偶联受体 84)拮抗剂。GPR84 antagonist 3 可抑制GTPγS，其pIC₅₀为 8.28。GPR84 antagonist 3 具有良好的药代动力学特征。

生物活性

GPR84antagonist 3 (compound 42) is a potentGPR84(G-protein-coupled receptor 84) antagonist.GPR84antagonist 3 inhibitsGTPγS, with apIC₅₀of 8.28.GPR84antagonist 3 has a favorable pharmacokinetic profile suitable^[1].

IC₅₀& Target

pIC50: 8.28 ± 0.11 (GTPγS)^[1]

体外研究
(In Vitro)

GPR84 antagonist 3 (compound 42) displays no ability to block the actions of the C3 fatty acid propionate at either FFAR2 or FFAR3 when tested at 10 μM^[1]

体内研究
(In Vivo)

GPR84 antagonist 3 (compound 42) (1 mg/kg (IV), 10 mg/kg (Orally); once) has a good elimination half-life (2.51 h), moderate rate of clearance, and bioavailability^[1].

Animal Model:

Male C57BL/6J mice (n = 3)^[1]

Dosage:

1 mg/kg (IV), 10 mg/kg (Orally)

Administration:

IV, Orally; once (Pharmacokinetic Analysis)

Result:

Pharmacokinetic Parameters of GPR84 antagonist 3 in Male C57BL/6J mice^[1].

	IV (1 mg/kg)	PO (10 mg/kg)
half-life (h)	2.51 ± 6.55
CL (mL/min/kg)	38.9 ± 13.9
Vss (L/kg)	7.24 ± 9.2
C₀(ng/mL)	394 ± 19.1
AUCall (ng/mL·h)	420 ± 12.5	1590 ± 18.7
T_max(h)		1
C_max(ng/mL)		402 ± 31.8
F (%)		36.8 ± 18.7

分子量

461.56

Formula

C₂₉H₂₇N₅O

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.