An inhibitor of H-PGDS
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TAS 205

Item No. 33261

Technical Information
Formal Name
4-[(1-methyl-1H-pyrrol-2-yl)carbonyl]-N-[4-[4-(4-morpholinylcarbonyl)-1-piperidinyl]phenyl]-1-piperazinecarboxamide, monohydrate
CAS Number
1584160-52-0
Molecular Formula
C27H36N6O4 • H2O
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH 7.2) (1:4): 0.20 mg/ml
λmax
266 nm
SMILES
O=C(N1CCN(CC1)C(C2=CC=CN2C)=O)NC3=CC=C(N4CCC(CC4)C(N5CCOCC5)=O)C=C3.O
InChi Code
InChI=1S/C27H36N6O4.H2O/c1-29-10-2-3-24(29)26(35)31-13-15-33(16-14-31)27(36)28-22-4-6-23(7-5-22)30-11-8-21(9-12-30)25(34)32-17-19-37-20-18-32;/h2-7,10,21H,8-9,11-20H2,1H3,(H,28,36);1H2
InChi Key
NFXCKTKGAJDCBA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    Product Description

    TAS 205 is an inhibitor of hematopoietic prostaglandin D synthase (H-PGDS; IC50 = 55.8 nM).1 It is selective for H-PGDS over lipocalin-type PGDS (L-PGDS) at 100 µM, as well as over enzyme and receptor panels at 10 µM. TAS 205 inhibits production of prostaglandin D2 (PGD2; Item No. 12010) induced by A23187 (Item No. 11016) in KU812 human and RBL-2H3 rat basophils with IC50 values of 78.3 and 181.3 nM, respectively. It inhibits ovalbumin-induced nasal lavage fluid eosinophil infiltration and late-phase nasal obstruction in an ovalbumin-sensitized guinea pig model of allergic rhinitis when administered at a dose of 30 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Aoyagi, H., Kajiwara, D., Tsunekuni, K., et alPotential synergistic effects of novel hematopoietic prostaglandin D synthase inhibitor TAS-205 and different types of anti-allergic medicine on nasal obstruction in a Guinea pig model of experimental allergic rhinitis. Eur. J. Pharmacol. 875, 173030 (2020).