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Cat. No.: HY-156073

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LY3325656

LY3325656 is a selective GPR142 receptor agonist. LY3325656 selectively activates GPR142 in humans and mice. LY3325656 enhances glucose-dependent insulin secretion, glucagon secretion, as well as the secretion of incretin hormones GLP-1 and GIP. LY3325656 can be used in research related to type 2 diabetes.

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

CAS No.: 1998714-25-2
Formula: C₂₁H₂₃F₃N₆O₂
Molecular Weight:448.45

Storage:

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

Data Sheet (268 KB)

LY3325656 Chemical Structure

CAS No.: 1998714-25-2

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

Description

IC₅₀ & Target^[1]^[2]

GPR142

GLP-1

GIP

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	43 nM Compound: 21; LY3325656	Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assay Agonist activity at human GPR142 receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate incubated for 1 hr followed by IP1-d2 addition by HTRF assay	[PMID: 31982234]

In Vitro

LY3325656 (compound 21) (30 min) exhibits low metabolic turnover with mouse, rat, dog, and human liver microsomes, with turnover rates of 22%, 14%, 13%, and 14% respectively^[1].
LY3325656 (10 μM) inhibits CYP 3A4, CYP 2C9, and CYP 2D6 enzymes by 22%, 11%, and 16% respectively at a concentration of 10 μM^[1].

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

Parmacokinetics

Species	Dose	Route	CL	V_ss	F
Rat^[1]	1 mg/kg	i.v.	22.1 mL/min/kg	1.1 L/kg	/
Rat^[1]	10 mg/kg	p.o.	/	/	63 %
Dog^[1]	1 mg/kg	i.v.	8.4 mL/min/kg	1.3 L/kg	/
Dog^[1]	5 mg/kg	p.o.	/	/	78 %

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1998714-25-2
Molecular Weight 448.45
Formula C₂₁H₂₃F₃N₆O₂
SMILES

CC1=C(N(C)C=N1)C=2NC(=NN2)[C@@H]3C[C@H](N(C(=O)C4=CC(C(F)(F)F)=CC=C4)C)CCO3
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 (268 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]. Liu LZ, et al. Discovery of LY3325656: A GPR142 agonist suitable for clinical testing in human. Bioorganic & medicinal chemistry letters. 2020 Mar 01;30(5):126857. [Content Brief]

[2]. Pratt EJ, et al. 20‑OR: GPR142 Agonists Increase Glucose‑Dependent Insulin Secretion and Differentially Regulate Hormone Secretion in Preclinical and Phase 1 Studies. Diabetes. 2019;68(Suppl 1):20‑OR.

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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.

MOQ

Minimum order quantity

100 mg

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