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Cat. No.: HY-148563

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GPR81 agonist 2

GPR81 agonist 2 is a GPR81 agonist with an EC₅₀ of 0.023 μM for the human receptor. GPR81 agonist 2 activates the lactate-sensing receptor GPR81, inhibits forskolin-stimulated cAMP production and GTP binding of G_i protein. GPR81 agonist 2 can be used for research on type 2 diabetes.

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

CAS No.: 1143024-28-5
Formula: C₂₆H₂₇ClN₆O₅S₂
Molecular Weight:603.11

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

GPR81 agonist 2 Chemical Structure

CAS No.: 1143024-28-5

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

GPR81

0.023 μM (EC₅₀)

All Hydroxycarboxylic Acid Receptor (HCAR) Isoforms :

HCAR1
HCAR2

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC50	0.023 μM	Agonist activity against human GPR81 overexpressing CHO cells assessed by functional cell-based cAMP assay. Agonist activity against human GPR81 overexpressing CHO cells assessed by functional cell-based cAMP assay.	31932225

In Vitro

GPR81 agonist 2 (compound 1) (10 μM) acts as a potent GPR81 agonist in CHO cells overexpressing hGPR81^[1].
GPR81 agonist 2 has hGPR81 EC₅₀ = 0.023 µM, hGPR109A EC₅₀ = 0.123 µM, and hGHS-R1a IC₅₀ = 0.008 µM; it shows poor selectivity for hGPR109A and hGHS-R1a^[1].

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

Chemical Information

CAS No. 1143024-28-5
Molecular Weight 603.11
Formula C₂₆H₂₇ClN₆O₅S₂
SMILES

O=C(NC1=NC2=C(S1)C=C(S(=O)(C3CCN(CC3)C)=O)C=C2)NC(C4=C(Cl)C=C(OCC)C(N5N=CC=C5)=C4)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Davidsson Ö, et al. Identification of novel GPR81 agonist lead series for target biology evaluation. Bioorganic & medicinal chemistry letters. 2020 Feb 15;30(4):126953. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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