Home>>GPR81 agonist 1

GPR81 agonist 1

Catalog No.GC61625

GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC50s of 58 nM and 50 nM for human and mouse GPR81, respectively.

Products are for research use only. Not for human use. We do not sell to patients.

GPR81 agonist 1 Chemical Structure

Cas No.: 1620992-67-7

Size Price Stock Qty
5 mg
$371.00
In stock
10 mg
$630.00
In stock
50 mg
$1,808.00
In stock
100 mg
$2,688.00
In stock

Tel:(909) 407-4943 Email: sales@glpbio.com

Customer Reviews

Based on customer reviews.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

View current batch:

Background

GPR81 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[1].

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

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 Cmax (6.3 μM)[1]. Animal Model: Nine-week-old male C57/Bl6 mice (fed and fasted mice)[1]

[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.

Chemical Properties

Cas No. 1620992-67-7 SDF
Canonical SMILES O=C([C@H]1CC[C@H](C)CC1)NC2=NC(C3=CC=CS3)=C(CC(N4CCN(C)CC4)=O)S2
Formula C22H30N4O2S2 M.Wt 446.63
Solubility Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.239 mL 11.1949 mL 22.3899 mL
5 mM 0.4478 mL 2.239 mL 4.478 mL
10 mM 0.2239 mL 1.1195 mL 2.239 mL
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Reviews

Review for GPR81 agonist 1

Average Rating: 5 ★★★★★ (Based on Reviews and 18 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for GPR81 agonist 1

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.