Timapiprant(OC000459) - 半岛电竞官方网址

Molecular Weight (MW)	348.37
Formula	C21H17FN2O2
CAS No.	851723-84-7, 950688-14-9 (sodium salt)
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility(In vitro)	DMSO: 4 mg/mL (11.5 mM)
Water: <1 mg/mL
Ethanol:<1 mg/mL
Other info	Chemical Name: 2-(5-fluoro-2-methyl-3-(quinolin-2-ylmethyl)-1H-indol-1-yl)acetic acid SMILES Code: O=C(O)CN1C(C)=C(CC2=NC3=CC=CC=C3C=C2)C4=C1C=CC(F)=C4 Exact Mass: 348.1274
Synonyms	OC000459; OC-000459; OC 000459

Molecular Weight (MW)

348.37

Formula

C21H17FN2O2

CAS No.

851723-84-7, 950688-14-9 (sodium salt)

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility(In vitro)

DMSO: 4 mg/mL (11.5 mM)

Water: <1 mg/mL

Ethanol:<1 mg/mL

Other info

Chemical Name: 2-(5-fluoro-2-methyl-3-(quinolin-2-ylmethyl)-1H-indol-1-yl)acetic acid

SMILES Code: O=C(O)CN1C(C)=C(CC2=NC3=CC=CC=C3C=C2)C4=C1C=CC(F)=C4

Exact Mass: 348.1274

Synonyms

OC000459; OC-000459; OC 000459

In Vitro	In vitroactivity: OC000459 inhibits the binding of [3H]PGD2 to membranes from CHO cells transfected with human DP2 with Ki of 13 nM. OC000459 also displaces [3H]PGD2 from membranes from human Th2 lymphocytes with Ki of 4 nM. OC000459 antagonizes PGD2-mediated calcium mobilization in a concentration-dependent manner with IC50 of 28 nM in intact CHO cells expressing DP2. OC000459 inhibits chemotaxis of human Th2 cells in response to PGD2 (10 nM) with IC50 of 28 nM. OC000459 (< 3 μM) antagonizes the effect of PGD2 competitively in both the isolated leukocyte preparation and heparinized human whole blood. OC000459 inhibits eosinophil shape change responses to DK-PGD2 with IC50 of 11 nM. OC000459 (1 μM) inhibits the activation of Th2 cells and eosinophils in response to mast cell supernatants. Cell Assay: Timapiprant (OC000459) (0.0001 μM-10 μM; 5 hours) inhibits chemotaxis (IC50=0.028 μM) of human Th2 lymphocytes and cytokine production (IC50=0.019 μM) by human Th2 lymphocytes. Timapiprant (OC000459) (1 μM) inhibits the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells.
In Vivo	OC000459 administrated at doses of 2 mg/kg p.o. in the Sprague-Dawley rats shows plasma half-life of 2.9 hours, time that maximal plasma concentration is achieved of 1.3 hours, maximal plasma concentration achieved is 1.54 μg/mL. OC000459 orally administrated 0.5 hour before injection of DK-PGD2 leads to a dose-dependent reduction in blood eosinophilia with ED50 of 0.04 mg/kg in rats. OC000459 orally administrated 0.5 hour before injection of DK-PGD2 also leads to a dose-dependent inhibition eosinophil accumulation ED50 of 0.01 mg/kg in rats. OC000459 (200 mg twice daily for 28 days) administrated in patients with moderate persistent asthma shows improvement in quality of life as analysed for both the Full Analysis (FA) population and the Per Protocol (PP) population. In those patients, OC000459 improves the night-time symptom scores, reduces the geometric mean sputum eosinophil count and respiratory infections. OC000459 (200 mg twice daily) treatment inhibits the later asthmatic responses and the post allergen increase in sputum eosinophils in steroid naive asthmatic patients.
Animal model	Sprague-Dawley rats
Formulation & Dosage	Dissolved in 10% DMSO/saline solution; 10 mg/kg; Oral administration
References	J Pharmacol Exp Ther. 2012 Feb;340(2):473-82.

In Vitro

In vitroactivity: OC000459 inhibits the binding of [3H]PGD2 to membranes from CHO cells transfected with human DP2 with Ki of 13 nM. OC000459 also displaces [3H]PGD2 from membranes from human Th2 lymphocytes with Ki of 4 nM. OC000459 antagonizes PGD2-mediated calcium mobilization in a concentration-dependent manner with IC50 of 28 nM in intact CHO cells expressing DP2. OC000459 inhibits chemotaxis of human Th2 cells in response to PGD2 (10 nM) with IC50 of 28 nM. OC000459 (< 3 μM) antagonizes the effect of PGD2 competitively in both the isolated leukocyte preparation and heparinized human whole blood. OC000459 inhibits eosinophil shape change responses to DK-PGD2 with IC50 of 11 nM. OC000459 (1 μM) inhibits the activation of Th2 cells and eosinophils in response to mast cell supernatants.

Cell Assay: Timapiprant (OC000459) (0.0001 μM-10 μM; 5 hours) inhibits chemotaxis (IC50=0.028 μM) of human Th2 lymphocytes and cytokine production (IC50=0.019 μM) by human Th2 lymphocytes. Timapiprant (OC000459) (1 μM) inhibits the activation of Th2 cells and eosinophils in response to supernatants from IgE/anti-IgE-activated human mast cells.

In Vivo

OC000459 administrated at doses of 2 mg/kg p.o. in the Sprague-Dawley rats shows plasma half-life of 2.9 hours, time that maximal plasma concentration is achieved of 1.3 hours, maximal plasma concentration achieved is 1.54 μg/mL. OC000459 orally administrated 0.5 hour before injection of DK-PGD2 leads to a dose-dependent reduction in blood eosinophilia with ED50 of 0.04 mg/kg in rats. OC000459 orally administrated 0.5 hour before injection of DK-PGD2 also leads to a dose-dependent inhibition eosinophil accumulation ED50 of 0.01 mg/kg in rats. OC000459 (200 mg twice daily for 28 days) administrated in patients with moderate persistent asthma shows improvement in quality of life as analysed for both the Full Analysis (FA) population and the Per Protocol (PP) population. In those patients, OC000459 improves the night-time symptom scores, reduces the geometric mean sputum eosinophil count and respiratory infections. OC000459 (200 mg twice daily) treatment inhibits the later asthmatic responses and the post allergen increase in sputum eosinophils in steroid naive asthmatic patients.

Animal model

Sprague-Dawley rats

Formulation & Dosage

Dissolved in 10% DMSO/saline solution; 10 mg/kg; Oral administration

References

J Pharmacol Exp Ther. 2012 Feb;340(2):473-82.

CAS NO:	851723-84-7
规格:	≥98%

包装	价格(元)
1mg	电议
2mg	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议
1g	电议