hMCH-1R antagonist 1 is an effective and selective antagonist of human melanin-concentrating hormone receptor 1 (hMCHR1) with an KB value of 3.6 nM.
| Molecular Weight | 1167.47 |
| Formula | C49H82N16O11S3 |
| CAS Number | 353487-64-6 |
| 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 GPR/FFAR Products |
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| CID1231538
CID1231538 is a potent GPR35 antagonist, with IC50 of 0.55 μM. CID1231538 is a benzothiazole analogue. |
| [Ala17]-MCH
[Ala17]-MCH, a MCH analogue, is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). |
| BigLEN(rat)
BigLEN(rat) is a potent GPR171 agonist with an EC50 of 1.6 nM. |
| BigLEN(mouse)
BigLEN(mouse) is a potent and selective agonist of orphan G protein-coupled receptor 171 (GPR171), with a Kd of ∼0.5 nM. |
| Neuropeptide EI, rat
Neuropeptide EI, rat displays functional melanin concentrating hormone (MCH)-antagonist and melanocyte-stimulating hormone (MSH) agonist activity in different behavioral paradigms. |
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