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GPR81 agonist 1

Cat. No. M10562
GPR81 agonist 1 Structure
Synonym:

GPR81 agonist I

Size Price Availability Quantity
2mg USD 230  USD230 In stock
5mg USD 400  USD400 In stock
10mg USD 660  USD660 In stock
50mg USD 1900  USD1900 In stock
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Quality Control & Documentation
Biological Activity

GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC50 values of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a.

In vivo, GPR81 agonist 1 (100 mg/kg; i.p.) suppresses lipolysis in mice without cutaneous flushing.

Chemical Information
Molecular Weight 446.63
Formula C22H30N4O2S2
CAS Number 1620992-67-7
Solubility (25°C) DMSO 45 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Taku Sakurai, et al. Eur J Pharmacol. Identification of a novel GPR81-selective agonist that suppresses lipolysis in mice without cutaneous flushing

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Keywords: GPR81 agonist 1, GPR81 agonist I supplier, GPR, inhibitors, activators

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