1. Immunology/Inflammation
  2. PGE synthase
  3. HPGDS inhibitor 1

HPGDS inhibitor 1 

Cat. No.: HY-10439 Purity: 99.32%
Handling Instructions

HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.

For research use only. We do not sell to patients.

HPGDS inhibitor 1 Chemical Structure

HPGDS inhibitor 1 Chemical Structure

CAS No. : 1033836-12-2

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 264 In-stock
Estimated Time of Arrival: December 31
5 mg USD 240 In-stock
Estimated Time of Arrival: December 31
10 mg USD 420 In-stock
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50 mg USD 1080 In-stock
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100 mg USD 1680 In-stock
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Description

HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX[1].

IC50 & Target

IC50: 0.6 nM (HPGDS in enzyme assays) and 32 nM (HPGDS in cellular assays)[1]

In Vitro

HPGDS inhibitor 1 has equal potency against purified HPGDS from human, rat, dog, and sheep (IC50, 0.5-2.3 nM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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[1].
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[1].
HPGDS inhibitor 1 (compound 8; 1 mg/mL) illustrates efficacy in an in vivo sheep model of asthma[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

381.37

Formula

C₁₉H₁₉F₄N₃O

CAS No.

1033836-12-2

SMILES

O=C(NC1CCN(CC(F)(F)F)CC1)C2=CC=C(C3=CC=CC(F)=C3)N=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (131.11 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6221 mL 13.1106 mL 26.2213 mL
5 mM 0.5244 mL 2.6221 mL 5.2443 mL
10 mM 0.2622 mL 1.3111 mL 2.6221 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.56 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

HPGDS inhibitor 1HPGDS inhibitor1HPGDS inhibitor-1PGE synthaseProstaglandin E synthaseHPGDSorallyPGD2asthmaInhibitorinhibitorinhibit

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Product Name:
HPGDS inhibitor 1
Cat. No.:
HY-10439
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