MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM) and a partial agonist at human MC3 and MC5 receptors (EC50 values of 59 and 1300 nM, respectively). In addition, MSG606 TFA reversed the hyperalgesia induced in female mice but had no effect in male mice.
| Molecular Weight | 1461.53 |
| Formula | C63H83F3N20O15S |
| CAS Number | 1416983-77-1 (free base) |
| Form | Solid |
| 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.
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|---|
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Adrenocorticotropic Hormone (ACTH) (4-10), human is a melanocortin 4 (MC4R) receptor agonist. |
| γ1-MSH
γ1-MSH is a melanocortin MC3 receptor agonist, with a Ki of 34 nM for the rat MC3 receptor. |
| γ-1-Melanocyte Stimulating Hormone (MSH), amide
γ-1-Melanocyte Stimulating Hormone (MSH), amide is a 11-amino acid peptide. |
| JKC363
JKC363, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). |
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ACTH (11-24) is an adrenocorticotropic hormone (ACTH) receptor antagonist. |
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