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FR167344 free base is an orally active, nonpeptide antagonist of the bradykinin receptor B2, exhibiting high-affinity binding (IC50: 65 nM) and showing no binding affinity for the B1 receptor.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | $2,570 | 3-6 months | 3-6 months | |
| 50 mg | $3,380 | 3-6 months | 3-6 months | |
| 100 mg | $4,600 | 3-6 months | 3-6 months |
| Description | FR167344 free base is an orally active, nonpeptide antagonist of the bradykinin receptor B2, exhibiting high-affinity binding (IC50: 65 nM) and showing no binding affinity for the B1 receptor. |
| Targets&IC50 | Bradykinin receptor B2:65 nM |
| In vitro | FR167344 shows no stimulatory effects on PI hydrolysis. FR167344 inhibits the B2 receptor-mediated phosphatidylinositol (PI) hydrolysis and produces a concentration-dependent rightward shift in the dose-response curve to bradykinin, in competitive experiments using membranes prepared from Chinese hamster ovary cells expressing the bradykinin receptor subtypes. This shift is accompanied by a progressive reduction of maximal response. Estimated pA2 values for the antagonism of bradykinin-induced PI hydrolysis by FR167344 is 8.0 [1]. |
| In vivo | FR167344 (p.o.; 2h; carrageenin injection) inhibits carrageenin-induced paw oedema in rats (ID50: 2.7 mg/kg). FR167344 (p.o.) inhibits kaolin-induced writhing in mice (ID50: 2.8 mg/kg in 10 min writhing and 4.2 mg/kg in 15 min writhing). FR167344(p.o.) inhibits caerulein-induced pancreatic oedema (ID50: 13.8 mg/kg) and it also increases in amylase and lipase of blood samples (ID50: 10.3 and 7.4 mg/kg, respectively, in rats) [2]. |
| Molecular Weight | 673.38 |
| Formula | C30H28BrCl2N5O4 |
| Cas No. | 215258-13-2 |
| Smiles | O(CC1=C(Cl)C(N(C(CNC(/C=C/C2=CC=C(C(N(C)C)=O)C=C2)=O)=O)C)=CC=C1Cl)C=3C=4N(C(Br)=C(C)N4)C=CC3 |
| Relative Density. | 1.43 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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