PPARα/γ agonist 4

Cat. No.: HY-162578: Data Sheet Handling Instructions
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PPARα/γ agonist 4 (Compound (S)-7) is an orally active dual potent agonist of PPARα and PPARγ, with EC₅₀ values of 0.061 μM and 1.42 μM respectively. PPARα/γ agonist 4 acts through an insulin-independent mechanism and exhibits mitochondrial pyruvate carrier inhibition and anti-diabetic properties. PPARα/γ agonist 4 is expected to be used in research for dyslipidemic type 2 diabetes.

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PPARα/γ agonist 4 화학구조

사이즈		재고
MOQ		Minimum order quantity
50 mg		견적 받기
100 mg		견적 받기
250 mg		견적 받기
Other size		견적 받기

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This product is a controlled substance and not for sale in your territory.

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PPARα PPARβ/δ PPARγ PPAR PPARδ

Biological Activity
순도&문서
References
고객리뷰

제품 설명

IC₅₀ & Target^[1]

PPARα

PPAR-γ

In Vitro

PPARα/γ agonist 4 (100 nM, 24 h) is able to increase the uptake and metabolism of glucose in C2C12 cell line and enhance mitochondrial activity by boosting fatty acid degradation, thus avoiding lipid accumulation in liver or muscle cells ^[1].

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

In Vivo

PPARα/γ agonist 4 (25 mg/kg, 50 mg/kg, p.o., a period of 15 days) exhibits dose-dependent antihyperglycemic effects in diabetic mouse models, along with lipid-lowering efficacy^[1].

Pharmacokinetic Analysis in MC38 Syngeneic Model^[1]

PPARα/γ agonist 4	Does Volume (mL/kg)	C₀/C_max(ng/mL)	T_max (h)	AUC_last(h·ng/mL)	AUC_infinity(h⋅ng/mL)	T_1/2(h)	V_d(L/kg)	CL (mL/min/kg)	MRT_last(h)	F (%)
i.v. (1 mg/kg)	10	2300	0.083	11400	11800	4.74	0.581	1.42	6.04	-
p.o. (5 mg/kg)	10	4280	2	43600	49000	7.61	1.16	1.74	7.74	76.4

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

Animal Model:	Streptozotocin (HY-13753) -induced diabetic mouse model^[1]
Dosage:	25 mg/kg, 50 mg/kg
Administration:	Oral gavage (p.o.), 15 days
Result:	At a dose of 50 mg/kg exhibited greater hypoglycemic effects compared to the 25 mg/kg dose. Oral treatment with PPARα/γ agonist 4 at 25 mg/kg significantly reduced levels of total cholesterol, high-density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C), and triglycerides. The 50 mg/kg dose reduced total cholesterol and HDL-C levels, but showed a smaller improvement in triglyceride levels.

분자량

368.42

화학식

C₂₅H₂₀O₃

SMILES

O=C(O)[C@H](CC1=CC=CC=C1)OC2=CC=C(C=C2)C3=C4C(C=CC=C4)=CC=C3

선적

Room temperature in continental US; may vary elsewhere.

보관

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

순도&문서

Handling Instructions (2659 KB)

References

[1]. Laghezza A. A chemical modification of a peroxisome proliferator-activated receptor pan agonist produced a shift to a new dual alpha/gamma partial agonist endowed with mitochondrial pyruvate carrier inhibition and antidiabetic properties. Eur J Med Chem. 2024; 275:116567. [Content Brief]