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HPGDS inhibitor 3

Catalog No. T61250   CAS 2255311-93-2

HPGDS inhibitor 3 is a powerful oral compound that selectively inhibits the hematopoietic prostaglandin D synthase (H-PGDS). With an IC50 value of 9.4 nM and EC50 of 42 nM, it demonstrates high potency in peripherally restricting H-PGDS. Moreover, HPGDS inhibitor 3 exhibits excellent selectivity with no associated central nervous system toxicity. This compound also possesses favorable pharmacokinetic properties in mouse, rat, and dog models. Additionally, HPGDS inhibitor 3 displays noteworthy anti-inflammatory activity [1].

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HPGDS inhibitor 3 Chemical Structure
HPGDS inhibitor 3, CAS 2255311-93-2
Pack Size Availability Price/USD Quantity
25 mg 6-8 weeks $ 2,140.00
50 mg 6-8 weeks $ 2,785.00
100 mg 6-8 weeks $ 3,520.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description HPGDS inhibitor 3 is a powerful oral compound that selectively inhibits the hematopoietic prostaglandin D synthase (H-PGDS). With an IC50 value of 9.4 nM and EC50 of 42 nM, it demonstrates high potency in peripherally restricting H-PGDS. Moreover, HPGDS inhibitor 3 exhibits excellent selectivity with no associated central nervous system toxicity. This compound also possesses favorable pharmacokinetic properties in mouse, rat, and dog models. Additionally, HPGDS inhibitor 3 displays noteworthy anti-inflammatory activity [1].
In vivo HPGDS inhibitor 3 (compound 1y), administered orally (PO) and intravenously (IV), demonstrates lower IV clearance, a similar steady-state volume of distribution, and an extended terminal half-life, along with high oral bioavailability and minimal brain exposure in mice, rats, and dogs. At dosages ranging from 0.003 to 1 mg/kg (PO; single administration), it dose-dependently reduces PGD2 levels to baseline and inhibits LPS-induced increases of PGD2 in plasma and skeletal muscle. Furthermore, dosages of 1, 3, and 10 mg/kg (PO; once daily for 16 days) significantly improve and expedite the functional recovery of injured limb muscles, with the greatest efficacy observed at ≥10 mg/kg daily. Tolerance levels vary by species and dosage, with rats tolerating up to 30 mg/kg/day over 7 days and dogs up to 30 mg/kg/day over 4 days without adverse effects, though higher doses are not tolerated. Pharmacokinetic analysis reveals that, across species, HPGDS inhibitor 3 maintains a low brain-to-blood ratio, reaffirming its safety and efficacy profile for potential therapeutic applications.
Molecular Weight 353.46
Formula C21H27N3O2
CAS No. 2255311-93-2

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

HPGDS inhibitor 3 2255311-93-2 inhibitor inhibit

 

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