PDE4-IN-12

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PDE4-IN-12

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

PDE4-IN-12 是一种强效的PDE4泛型抑制剂，其对PDE4和PDE7的IC₅₀值分别为 3.5 和 15 nM (SI分别为 2.71 和 4.27)。PDE4-IN-12 具有较好的安全性，可用于炎症性肠病 (IBDs) 的研究。

生物活性

PDE4-IN-12 is a potent pan-PDE4 inhibitor, withIC₅₀s of 3.5 and 15 nM forPDE4andPDE7, respectively (SI=2.71 and 4.27, respectively). PDE4-IN-12 shows well tolerated, can be used in study of inflammatory bowel diseases (IBDs)^[1].

IC₅₀& Target

PDE4D2

3.51 nM (IC₅₀)

PDE4B2

9.51 nM (IC₅₀)

PDE7A

15 nM (IC₅₀)

PDE5A1

1.24 μM (IC₅₀)

PDE10A

1.02 μM (IC₅₀)

PDE8A1

194 nM (IC₅₀)

体外研究
(In Vitro)

PDE4-IN-12 (compound 22d) (10, 20 μM; 24 h) reduces the release of NO in LPS induced inflammation cell model (indicates anti-inflammatory effect)^[1].

Cell Viability Assay^[1]

Cell Line:	Raw264.6 cells
Concentration:	10, 20 μM
Incubation Time:	24 h
Result:	Reduced the NO release by dose-dependent manner in the LPS induced inflammatory cell model.

体内研究
(In Vivo)

PDE4-IN-12 (5 mg/kg; i.p.; twice daily for 8 days) ameliorates mouse acute colitis induced by DSS (dextran sulfate sodium)^[1].
PDE4-IN-12 (10 mg/kg; p.o.; single) shows well tolerated in dogs^[1].
PDE4-IN-1 (2.5 mg/kg; i.v.; single) shows great plasma exposure, with T_1/2and AUC_{0-24 h}values of 4.18 h and 6522 h?ng/mL^[1].

Animal Model:	Male C57BL/6 mice (5 to 6-week old; 15-17 g; DSS-induced mouse model)^[1].
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; twice daily for 8 days.
Result:	Ameliorated the acute colitis by decreasing disease activity index, increasing the colon length, and also ameliorating the pathological damages.

Animal Model:	Beagle dogs^[1].
Dosage:	10 mg/kg (solved in 0.5% CMC-Na solution).
Administration:	Oral administration; single.
Result:	Exhibited good safety, which caused no emesis on beagle dogs at 10 mg/kg.

Animal Model:

Male C57BL/6 mice (5 to 6-week old; 15-17 g)^[1].

Dosage:

2.5 mg/kg

Administration:

Intravenous injection; single.

Result:

1.19Pharmacokinetic Parameters of PDE4-IN-12 in Male C57BL/6 mice^[1].

	T_1/2(h)	AUC_{0-24 h}(h·ng/mL)	MRT_{0-24 h}(h)	CL (mL/min/kg)	Vss (mL/kg)
IV (2.5 mg/kg)	4.18	6522	1.76	6.40	673

分子量

553.64

Formula

C₃₄H₃₅NO₆

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.