HPGDS inhibitor 1

SKU: orb1227100

Description

A potent, selective, oral hematopoietic prostaglandin D synthase (HPGDS) inhibitor with enzyme IC50 of 0.6 nM; does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5 LOX (IC50>10 uM); reduces the antigen-induced response in vivo.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1033836-12-2
• MW: 381.3673
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₉F₄N₃O
• SMILES: O=C(C1=CC=C(C2=CC=CC(F)=C2)N=C1)NC3CCN(CC(F)(F)F)CC3
• Target: PGE synthase
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  HPGDS inhibitor 1 (compound 8; 1 mg/kg) has excellent PK characteristics with 76% bioavailability, and the T1/2 is 4.1 hours in rats. Rats dosed orally with 1 mg/kg and 10 mg/kg HPGDS inhibitor 1 (compound 8) are sacrificed at various times. Oral administration of HPGDS inhibitor 1 blocks PGD2 production in the rat spleen; inhibition of PGD2 is inversely correlated with the plasma concentration of HPGDS inhibitor 1 in a time-and dose-dependent manner. HPGDS inhibitor 1 (compound 8; 1 mg/mL) illustrates efficacy in an In vivo sheep model of asthma.
• In Vitro:
  HPGDS inhibitor 1 has equal potency against purified HPGDS from human, rat, dog, and sheep (IC50, 0.5-2.3 nM).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

H-PGDS Inhibitor I

Quick Database Links

Gene Symbol

PGE synthase