ACT-389949 is a first-in-class, potent, selective formyl peptide receptor 2/lipoprotein A4 receptor (FPR2)/(ALX) agonist with an EC50 value of 3 nM for FPR2/ALX entry into monocytes.Additionally, ACT-389949 is an excellent tool compound for in vitro and in vivo to further analyze FPR2-regulated activity, which could be used in the development of next-generation FPR signaling-regulated anti-inflammatory therapies.
| Molecular Weight | 428.39 |
| Formula | C20H18F2N6O3 |
| CAS Number | 1258417-54-7 |
| Solubility (25°C) | DMSO 5 mg/mL (May need ultrasonic and adjust pH with HCl) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related FPR Products |
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| Ac9-25
Ac9-25, a N-terminal peptide of Annexin I, acts as a formyl peptide receptor (FPR) agonist and activates the neutrophil NADPH oxidase through FPR. |
| N-Formyl-Nle-Leu-Phe-Nle-Tyr-Lys
N-Formyl-Nle-Leu-Phe-Nle-Tyr-Lys TFA (For-Nle-Leu-Phe-Nle-Tyr-Lys-OH TFA) is a formyl peptide receptor (FPR) agonist. |
| WKYMVM-NH2 TFA
WKYMVM-NH2 TFA is a potent N-formyl peptide receptor (FPR1) and FPRL1/2 agonist, also activates several leukocyte effector functions. |
| {Boc}-Phe-Leu-Phe-Leu-Phe
{Boc}-Phe-Leu-Phe-Leu-Phe ({Boc}-FLFLF) is a formyl peptide receptor (FPR) family antagonist that preferentially inhibits activity triggered through the formyl peptide receptor. |
| WKYMVM
WKYMVM is a potent N-formyl peptide receptor (FPR1) and FPRL1/2 agonist, also activates several leukocyte effector functions such as chemotaxis, mobilization of complement receptor-3, and activation of the NADPH oxidase. |
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