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GPR81 agonist 1
CAS No. 1620992-67-7
GPR81 agonist 1( —— )
Catalog No. M35660 CAS No. 1620992-67-7
GPR81 agonist 1 is a potent and selective GPR81 agonist with high affinity for human and mouse GPR81, inhibiting lipolysis of differentiated 3T3-L1 adipocytes, improving insulin sensitivity and glycaemic control in mouse models of insulin resistance and diabetes, and can be used in the study of diabetes and obesity.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 277 | In Stock |
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| 5MG | 312 | In Stock |
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| 10MG | 534 | In Stock |
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| 25MG | 998 | In Stock |
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| 50MG | 1479 | In Stock |
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| 100MG | Get Quote | In Stock |
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| 200MG | Get Quote | In Stock |
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| 500MG | Get Quote | In Stock |
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| 1G | Get Quote | In Stock |
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Biological Information
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Product NameGPR81 agonist 1
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NoteResearch use only, not for human use.
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Brief DescriptionGPR81 agonist 1 is a potent and selective GPR81 agonist with high affinity for human and mouse GPR81, inhibiting lipolysis of differentiated 3T3-L1 adipocytes, improving insulin sensitivity and glycaemic control in mouse models of insulin resistance and diabetes, and can be used in the study of diabetes and obesity.
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DescriptionGPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC50s 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.
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In Vitro——
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In VivoAnimal Model:Nine-week-old male C57/Bl6 mice (fed and fasted mice)Dosage:100 mg/kg Administration:I.p.Result:Reduced plasma FFA content of fed and fasted mice by approximately 50% and 35%, respectively, at 15 min postdose when intraperitoneally administered at a dose of 100 mg/kg.Animal Model:Male C57/Bl6 mice Dosage:10 mg/kg (Pharmacokinetic Analysis) Administration:I.p.(Pharmacokinetic Analysis)Result:Showed good bioavailability (71%) and Cmax (6.3 μM).
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Synonyms——
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PathwayCell Cycle/DNA Damage
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TargetGPR
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RecptorGPR
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Research Area——
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Indication——
Chemical Information
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CAS Number1620992-67-7
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Formula Weight446.63
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Molecular FormulaC22H30N4O2S2
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 50 mg/mL (111.95 mM; Ultrasonic )
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SMILESC[C@H]1CC[C@@H](CC1)C(=O)Nc1nc(c(CC(=O)N2CCN(C)CC2)s1)-c1cccs1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Sakurai T, et al. Identification of a novel GPR81-selective agonist that suppresses lipolysis in mice without cutaneous flushing. Eur J Pharmacol. 2014;727:1-7.?
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