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) |
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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. |
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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 T1/2and AUC0-24 hvalues 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].
| T1/2(h) | AUC0-24 h(h·ng/mL) | MRT0-24 h(h) | CL (mL/min/kg) | Vss (mL/kg) | | IV (2.5 mg/kg) | 4.18 | 6522 | 1.76 | 6.40 | 673 |
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| 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. |
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