Bombesin is a tetradecapeptide, which plays an important role in the release of gastrin and the activation of G-protein receptors. Bombesin is found to have stimulatory effects upon gastric and pancreatic secretions, release of gastrointestinal hormones, gallbladder contraction and bronchoconstriction. It is present in amphibian gastric endocrine cells, avian proventriculus endocrine cells and avian brain. In mammals it is present mainly in nerve cells and fibers. The only mammalian endocrine cell shown to date to have bombesin is the P-cell in fetal lung. Bombesin is shown to be a potent mitogen for Swiss 3T3 cells. In the presence of a low concentration (3.5%) of serum, bombesin stimulates 3T3 cell proliferation. In serum-free medium, bombesin induces DNA synthesis in the absence of any other added growth factor with IC50 of 1 nM.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||0.05M acetic acid 20 mg/mL
Water 1 mg/mL
|Storage||-20°C, protect from light, sealed|
Garcinone E is the most active xanthone from mangosteen, which has potent cytotoxic effect against hepatocellular carcinoma cell lines. Garcinone E might inhibit metastasis of an oral cancer cell line by blocking invasion, migration and MMP production.
GRP-60367 hydrochloride is a first-in-class potent and selective inhibitor of rabies virus (RABV) entry that specifically targets the RABV G protein.
ML382 is a potent and selective MrgX1 (Mas-related G protein-coupled receptor X1, MRGPRX1) positive allosteric modulator with EC50 of 190 nM.
Enpp-1-IN-1, also known as MV 658, is a Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) inhibitor.
GW280264X is an ADAM17 inhibitor.
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