AT 56

Name	AT-56
Synonyms	AT 56 AT-56 CS-1414 4-Dibenzo[a,d]cyclohepten-5-ylidene-1-[4-(2H-tetrazol-5-yl)-butyl]-piperidine 4-(5H-Dibenzo[a,d]cyclohepten-5-ylidene)-1-[4-(1H-tetrazol-5-yl)butyl]piperidine 4-(5H-Dibenzo[a,d]cyclohepten-5-ylidene)-1-[4-(2H-tetrazol-5-yl)butyl]-piperidine
CAS	162640-98-4
EINECS	200-256-5

Molecular Formula	C25H27N5
Molar Mass	397.52
Density	1.216±0.06 g/cm3(Predicted)
Boling Point	620.4±65.0 °C(Predicted)
Solubility	DMSO: soluble10mg/mL, clear
Appearance	powder
Color	white to beige
pKa	4.99±0.10(Predicted)
Storage Condition	Inert atmosphere,Store in freezer, under -20°C
In vitro study	AT-56 (1-30 μM; 10 minutes) dose-dependently inhibits the production of PGD 2 in L-PGDS-expressing human medulloblastoma TE-671 cells with an IC 50 of about 3 μM.

WGK Germany

Last Update：2024-01-02 23:10:35

biological activity	AT-56 is an orally active lipocalin-type protaglandin (PG) D synthase (L-PGDS) the corresponding Ki and IC50 values were 75 μm and 95 μm, respectively.
Target	Value
L-PGDS (Cell-free assay)	75 μM(Ki) 95 μM
Animal Model:	H-PGDS KO mice (14-16weeks, 25-30 g, C57BL/6 strain) with a stab wound brain injury Human L-PGDS-overexpressing TG mice (males, 14-16 weeks, 25-30 g) Male C57BL/6 mice (7 weeks, 22-26 g)
Dosage:	0, 1, 3, 10, 30 mg/kg 0, 1, 10 mg/kg 10 mg/kg for p.o. and 2 mg/kg for i.v. (Pharmacokinetic Analysis)
Administration:	P.o. 1 h before the stab wound injury P.o. 1 h before and 24 h after the antigen exposure P.o. and i.v. administration
Result:	Inhibited the L-PGDS reaction in the brain. Decreased the total amount of PGD 2 in the brain to 40% with 30 mg/kg AT-56. Prevented the eosinophil infiltration by inhibiting transgened human L-PGDS. Oral bioavailability (82%); C max (2.15 μg/ml); T 1/2 (1.71 h, p.o.); T 1/2 (2.35 h, i.v.).

Last Update：2024-04-09 02:00:14

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CAS: 162640-98-4
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Email: 3008007409@qq.com
Mobile: 18021002903
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