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AT-56 Exclusive

Cayman Chemical Item Number 13160

(CAS 162640-98-4)

AT-56 (CAS 162640-98-4)

See more	Inhibitors (493) Allergy/Asthma (97) Inflammation (383) Neuroscience (654)

Description

Prostaglandin D synthase (PGDS) catalyzes the isomerization of PGH₂ to produce PGD₂. PGD₂ induces sleep, regulates nociception, inhibits platelet aggregation, and acts as an allergic mediator. Two distinct types of PGDS have been identified, namely the lipocalin-type enzyme (β-trace, L-PGDS) and the hematopoietic-type enzyme (H-PGDS).^1,2,3 L-PGDS is localized in the central nervous system, male genital organs of various mammals, and the human heart and is a major protein in human cerebrospinal fluid (CSF).¹ AT-56 is a selective, competitive, and highly bioavailable inhibitor of L-PGDS with a K_i value of 75 µM.⁴ It inhibits the production of PGD₂ by L-PGDS purified from human CSF and recombinant mouse cells with an IC₅₀ value of 95 µM.⁴ At concentrations as high as 100 µM in vitro or 30 mg/kg in vivo, AT-56 does not affect the production of PGE₂, PGF_2α, or H-PGDS-catalyzed PGD₂.⁴ At 10 mg/kg AT-56, the numbers of total cells, infiltrating eosinophils, and monocytes in bronchoalveolar lavage fluid of L-PGDS transgenic mice were decreased to 23, 6, and 41% of controls, respectively.⁴

1 Urade, Y., Watanabe, K., and Hayaishi, O. Prostaglandin D, E, and F synthases. J Lipid Mediat Cell Signal 12 257-273 (1995).

2 Urade, Y., and Hayaishi, O. Prostaglandin D synthase: Structure and function. Vitam Horm 58 89-120 (2000).

3 Urade, Y., and Eguchi, N. Lipocalin-type and hematopoietic prostaglandin D synthases as a novel example of functional convergence. Prostaglandins Other Lipid Mediat 68-69 375-382 (2002).

4 Irikura, D., Aritake, K., Nagata, N., et al. Biochemical, functional, and pharmacological characterization of AT-56, an orally active and selective inhibitor of lipocalin-type prostaglandin D synthase. J Biol Chem 284(12) 7623-7630 (2009).

Formal Name	4-(5H-dibenzo[a,d]cyclohepten-5-ylidene)-1-[4-(2H-tetrazol-5-yl)butyl]-piperidine
CAS Number	162640-98-4
Molecular Formula	C₂₅H₂₇N₅
Formula Weight	397.5
Formulation	A crystalline solid
Purity	≥95%
Stability	2 years
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard C12=C(C=CC=C2)C=CC3=C(C=CC=C3)/C1=C4CCN(CCCCC5=NN=NN5)CC\4

Background Reading

Urade, Y., and Eguchi, N. Lipocalin-type and hematopoietic prostaglandin D synthases as a novel example of functional convergence. Prostaglandins Other Lipid Mediat 68-69 375-382 (2002).

Urade, Y., and Hayaishi, O. Prostaglandin D synthase: Structure and function. Vitam Horm 58 89-120 (2000).

Urade, Y., Watanabe, K., and Hayaishi, O. Prostaglandin D, E, and F synthases. J Lipid Mediat Cell Signal 12 257-273 (1995).

Irikura, D., Aritake, K., Nagata, N., et al. Biochemical, functional, and pharmacological characterization of AT-56, an orally active and selective inhibitor of lipocalin-type prostaglandin D synthase. J Biol Chem 284(12) 7623-7630 (2009).

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Size	Price	Quantity	Subtotal
1 mg	$33.00		$0.00
5 mg	$149.00		$0.00
10 mg	$264.00		$0.00
50 mg	$1,155.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-02-11. Prices are subject to change without notice.

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