HPGDS inhibitor 1 (Synonyms: H-PGDS Inhibitor I) |
| Katalog-Nr.GC14633 |
HPGDS-Inhibitor 1 ist ein potenter, selektiver und oral aktiver Inhibitor der hÄmatopoetischen Prostaglandin-D-Synthase (HPGDS) mit einem IC50-Wert von 0,6 nM bzw. 32 nM in Enzym- bzw. Zellassays.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1033836-12-2
Sample solution is provided at 25 µL, 10mM.
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HPGDS inhibitor 1 is an oral potent and selective inhibitor of hematopoietic prostaglandin D synthase (HPGDS) with IC50 value of 0.7nM [1].
Prostaglandin D2 (PGD2) is a mediator of allergy and inflammation. It is isomerized from PGH2 by PGDS. This production is important in airway allergic and inflammatory processes. HPGDS inhibitor 1 has a 3-fluorine substituent, making it stable in the in vitro human microsome assay. It has potent effects in enzyme assay and cellular assay with IC50 values of 0.7nM and 32nM, respectively. In addition, the potency is equal against purified HPGDS from various species with IC50 values ranging from 0.5-2.3nM. Besides that, HPGDS inhibitor 1 is selective against HPGDS over other relevant human enzymes including L-PGDS, mPGES, COX-1, COX-2 and 5 LOX [1].
In a model of antigen-induced airway response in allergic sheep, treatment of HPGDS inhibitor 1 completely prevents the late asthma reaction and blocks the Airway hyper-responsiveness [1].
References:
[1] Carron C P, Trujillo J I, Olson K L, et al. Discovery of an oral potent selective inhibitor of hematopoietic prostaglandin D synthase (HPGDS). ACS Medicinal Chemistry Letters, 2010, 1(2): 59-63.
| Cas No. | 1033836-12-2 | SDF | |
| Überlieferungen | H-PGDS Inhibitor I | ||
| Chemical Name | 6-(3-fluorophenyl)-N-[1-(2,2,2-trifluoroethyl)piperidin-4-yl]pyridine-3-carboxamide | ||
| Canonical SMILES | C1CN(CCC1NC(=O)C2=CN=C(C=C2)C3=CC(=CC=C3)F)CC(F)(F)F | ||
| Formula | C19H19F4N3O | M.Wt | 381.37 |
| Löslichkeit | DMF: 5 mg/ml,DMSO: 5 mg/ml,Ethanol: 1 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6221 mL | 13.1106 mL | 26.2213 mL |
| 5 mM | 524.4 μL | 2.6221 mL | 5.2443 mL |
| 10 mM | 262.2 μL | 1.3111 mL | 2.6221 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.00%
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- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 2 reference(s) in Google Scholar.)
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