[CAS NO. 1620992-67-7] GPR81agonist1

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PRODUCTS SPECIFICATIONS [1620992-67-7]

Catalog

HY-135982

Brand

MCE

CAS

1620992-67-7

DESCRIPTION [1620992-67-7]

Overview

MDL	-
Molecular Weight	446.63
Molecular Formula	C22H30N4O2S2
SMILES	O=C([C@H]1CC[C@H](C)CC1)NC2=NC(C3=CC=CS3)=C(CC(N4CCN(C)CC4)=O)S2

For research use only. We do not sell to patients.

Summary

GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC ₅₀ s 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 ^[1] .

In Vitro

GPR81 agonist 1 (compound 2) (1-1000 nM) inhibits lipolysis in differentiated 3T3-L1 adipocytes ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

GPR81 agonist 1 (100 mg/kg; i.p.) suppresses lipolysis in mice without cutaneous flushing ^[1] .
GPR81 agonist 1 (10 mg/kg; i.p.) shows good bioavailability (71%) and C _max (6.3 μM) ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nine-week-old male C57/Bl6 mice (fed and fasted mice) ^[1]
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 ^[1]
Dosage:	10 mg/kg (Pharmacokinetic Analysis)
Administration:	I.p.(Pharmacokinetic Analysis)
Result:	Showed good bioavailability (71%) and C _max (6.3 μM).

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 111.95 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2390 mL	11.1949 mL	22.3899 mL
5 mM	0.4478 mL	2.2390 mL	4.4780 mL
10 mM	0.2239 mL	1.1195 mL	2.2390 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.60 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[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.