15-PGDH-IN-1

立即咨询

15-PGDH-IN-1

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:

2241676-74-2

15-PGDH-IN-1 是一种有效的 15-PGDH 抑制剂，具有口服活性。15-PGDH-IN-1 对重组人 15-PGDH 具有抑制活性，IC₅₀值为 3 nM。15-PGDH-IN-1 可用于组织修复和再生的研究。

生物活性

15-PGDH-IN-1 is a potent and orally active15-PGDHinhibitior. 15-PGDH-IN-1 has inhibition activity against recombinant human15-PGDHwith anIC₅₀value of 3 nM. 15-PGDH-IN-1 can be used for the research of tissue repair and regeneration^[1].

IC₅₀& Target

IC50: 3 nM (15-PGDH)^[1]

体外研究
(In Vitro)

15-PGDH-IN-1 (compound 49) has inhibition activity against recombinant human 15-PGDH with an IC₅₀value of 3 nM^[1].
15-PGDH-IN-1 (4, 20, 100, 500, 2500 nM) induces PGE2 in A549 cells at 20 nM^[1].

体内研究
(In Vivo)

15-PGDH-IN-1 (compound 49) (5, 10, 20, 40 mg/kg; IV, IP, PO) shows potent inhibition of 15-PGDH, good oral bioavailability, and protective activity in mouse models of ulcerative colitis and recovery from bone marrow transplantation^[1].

Animal Model:	CD1 Mice (female)^[1]
Dosage:	5, 10 mg/kg
Administration:	IV, IP, PO
Result:	Showed a low C_maxvalue when dosed orally versus IP, but the AUC was only reduced by half and had good oral bioavailability (63%).

Animal Model:	C57Bl/6 mice^[1]
Dosage:	5, 20, 40 mg/kg
Administration:	IP, Oral
Result:	Showed elevation of PGE2 levels in colon and lung inhibited 15-PGDH enzymatic activity in the colon.

Animal Model:	DSS model^[1]
Dosage:	10, 40 mg/kg
Administration:	IP (10 mg/kg BID) or PO (40 mg/kg BID)
Result:	Showed protection in the mouse DSS model of ulcerative colitis.

分子量

398.46

Formula

C₂₄H₂₂N₄O₂

CAS 号

2241676-74-2

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.