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Novokinin acetate exhibited an affinity for the AT2 receptor with Ki of 7 nM, and its antihypertensive and vasorelaxing activities were blocked by PD123319, an AT2 receptor antagonist.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $142 | - | In Stock | |
| 2 mg | $196 | - | In Stock | |
| 5 mg | $320 | - | In Stock | |
| 10 mg | $461 | - | In Stock | |
| 25 mg | $713 | - | In Stock | |
| 50 mg | $948 | - | In Stock | |
| 100 mg | $1,290 | - | In Stock | |
| 200 mg | $1,730 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $513 | - | In Stock |
| Description | Novokinin acetate exhibited an affinity for the AT2 receptor with Ki of 7 nM, and its antihypertensive and vasorelaxing activities were blocked by PD123319, an AT2 receptor antagonist. |
| Targets&IC50 | AT2:7 nM(Ki) |
| In vitro | Novokinin relaxed a mesenteric artery isolated from the spontaneously hypertensive rat (SHR) at 10(-5) M, and reduced SHR blood pressure at a dose of 0.1 mg/kg (po.) emulsified in 30% egg yolk[1]. |
| In vivo | The hypotensive effect of novokinin in normotensive mice was not observed in the AT2 receptor-knockout mice. Its antihypertensive and vasorelaxing activities in SHR were also blocked by CAY-10441, an antagonist of the IP receptor for prostaglandin I2 PGI2 suggesting that these activities are mediated by the AT2 receptor, followed by the prostaglandin I2-IP receptor pathway. Novokinin suppressed food intake after icv. or po. administration in mice. The anorexigenic activity was not observed in the AT2 receptor- knockout mice, but was observed in the AT 1 receptor-knockout mice. The anorexigenic activities of novokinin and angiotensin II were blocked by PD123319, and ONO-AE3-208, an antagonist of the EP4 receptor suggesting that the anorexigenic activities of the AT2 agonists are mediated by the PGE 2-EP4 receptor pathway downstream of the AT2 receptor. Novokinin given icv. in mice antagonized the antinociceptive effect of morphine[1]. |
| Synonyms | Novokinin acetate (358738-77-9 free base) |
| Molecular Weight | 856.02 |
| Formula | C41H65N11O9 |
| Smiles | CC(C)C[C@@H](C(N[C@@H](CCCCN)C(N(CCC1)[C@@H]1C(N[C@@H](Cc1c[nH]c2c1cccc2)C(O)=O)=O)=O)=O)NC([C@H](CCC1)N1C([C@H](CCCNC(N)=N)N)=O)=O.CC(O)=O |
| Relative Density. | no data available |
| Sequence | Arg-Pro-Leu-Lys-Pro-Trp |
| Sequence Short | RPLKPW |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||
| Solubility Information | DMSO: 13 mg/mL (15.19 mM), Sonication is recommended. | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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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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