| Size | Price | Stock | Qty |
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| 2mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
HPGDS Inhibitor I (also known as H-PGDS inhibitor 1) is a novel, orally bioavailable, potent and selective inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS) with IC50 Value of 0.7 nM. HPGDS Inhibitor I demonstrated equal potency against purified HPGDS from human , rat, dog, and sheep with IC50 in the range of 0.5-2.3 nM. Hematopoietic prostaglandin D synthase (HPGDS) is primarly expressed in mast cells, antigen-presenting cells, and Th-2 cells. HPGDS converts PGH2 into PGD2, a mediator thought to play a pivotal role in airway allergy and inflammatory processes. HPGDS Inhibitor I reduces the antigen-induced response in allergic sheep.
| ln Vitro |
With an IC50 of 0.5-2.3 nM, HPGDS inhibitor 1 exhibits equivalent potency against purified HPGDS from humans, rats, dogs, and sheep[1].
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| ln Vivo |
Compound 8, or HPGDS inhibitor 1, has a 76% bioavailability, 4.1-hour half-life in rats, and good PK characteristics[1]. Rats given oral doses of HPGDS inhibitor 1 (compound 8) at doses of 1 mg/kg and 10 mg/kg are sacrificed at different intervals. PGD2 production in the rat spleen is inhibited by oral administration of HPGDS inhibitor 1, and this inhibition is inversely correlated with the plasma concentration of HPGDS inhibitor 1 in a time- and dose-dependent manner[1]. In an in vivo sheep model of asthma, HPGDS inhibitor 1 (compound 8; 1 mg/mL) demonstrates effectiveness[1].
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| Animal Protocol |
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| References |
| Molecular Formula |
C19H19F4N3O
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|---|---|---|
| Molecular Weight |
381.37
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| Exact Mass |
381.146
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| CAS # |
1033836-12-2
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| Related CAS # |
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| PubChem CID |
24991044
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
487.2±45.0 °C at 760 mmHg
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| Flash Point |
248.5±28.7 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
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| Index of Refraction |
1.559
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| LogP |
3.24
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
27
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| Complexity |
494
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LPUCBGGXXIUBAZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H19F4N3O/c20-15-3-1-2-13(10-15)17-5-4-14(11-24-17)18(27)25-16-6-8-26(9-7-16)12-19(21,22)23/h1-5,10-11,16H,6-9,12H2,(H,25,27)
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| Chemical Name |
6-(3-fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.56 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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