Cat. No.: HY-171889

BI-9774

Name: BI-9774
Brand: MedChemExpress
SKU: HY-171889
Availability: PreOrder

BI-9774 is a potent, selective, and orally active AMPK activator, with EC₅₀ values of 20.0 nM and 63.1 nM against human AMPK α1β1γ1 and AMPK α1β2γ1, respectively. BI-9774 binds to the allosteric drug and metabolite (ADaM) site and induces ACC Ser79 phosphorylation in HepG2 cells, with an EC₅₀ of 83.2 nM. BI-9774 can be used in studies related to AMPK signaling, multiple sclerosis, and non-alcoholic fatty liver disease.

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The BI-9774 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.

CAS No.: 1644498-53-2
화학식: C₂₆H₂₅ClN₄O₅S
분자량:541.02

보관:

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

Data Sheet (283 KB)

BI-9774 Chemical Structure

CAS No.: 1644498-53-2

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Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[4]

AMPK α1β1γ1

20 nM (EC₅₀)

AMPK α1β2γ1

63.1 nM (EC₅₀)

All AMPK Isoforms :

In Vitro

BI-9774 (following a 1-hour incubation) potently induces the phosphorylation of ACC in human HepG2 hepatocellular carcinoma cells, with an EC₅₀ of 83.2 nM^[4].
BI-9774 (10 μM; 72 h) reduces PCAF protein abundance in pathogenic TH17 (pTH17) cells^[3].
BI-9774 (1.25 or 10 μM; 2 h) increases the phosphorylation of ACC Ser79, ULK1 Ser555 and AMPKα Thr172 in undifferentiated primary mouse adipose-derived stem cells (mADSCs); no significant difference in the phosphorylation level of target proteins is observed between 1.25 μM and 10 μM^[2].
BI-9774 (1.25 or 10 μM; 3 days) increases ACC Ser79 phosphorylation in mature primary mouse adipocytes. At 10 μM, BI-9774 significantly reduces Lep mRNA, but does not significantly alter lipid droplet accumulation, nuclear number, adipogenic index, or the mRNA levels of Pparg, Lpl, Plin1 and Adipoq. BI-9774 also does not significantly change UCP1, CKB and SERCA2 under either unstimulated or Isoprenaline (HY-108353)-stimulated conditions^[2].
BI-9774 (1.25-10 μM; 8 days) reduces lipid accumulation, nuclear count and adipogenic index in a concentration-dependent manner during adipogenic differentiation of mADSC, and significantly decreases lipid droplet size at 10 μM; 1.25 μM BI-9774 simultaneously downregulates the mRNA levels of *Pparg*, *Lpl*, *Plin1*, *Adipoq* and *Lep*, as well as the protein levels of FAS, ACC and PLIN1^[2].
BI-9774 (1.25 μM; administered from day 2 or day 4 to day 8) consistently reduces Lep mRNA during the adipocyte maturation stage; exposure starting on day 4 does not significantly alter adipogenesis, suggesting that decreased Lep expression can be dissociated from changes in adipogenesis^[2].
Brief exposure to BI-9774 (1.25 μM; administered for the first 2 days followed by washout until day 8) during the initial stage of mADSC adipogenic differentiation persistently reduces lipid accumulation and adipogenic index, and decreases PPARγ protein and leptin in the culture supernatant. No sustained phosphorylation of AMPKα Thr172, ACC Ser79, or ULK1 Ser555 is detected on day 8, and ACC inhibition within the same time window cannot replicate this adipogenic phenotype^[2].
BI-9774 (1.25 μM; during adipogenic differentiation) reduces intracellular TGFβ protein and increases Tgfbr2 mRNA, but does not significantly alter ERK/SMAD2/3 signaling or β-catenin nuclear translocation^[2].

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

Western Blot Analysis^[2]

Cell Line:

Undifferentiated primary mADSCs
Concentration:

1.25 or 10 μM
Incubation Time:

2 h
Result:

Increased p-ACCSer79, p-ULK1Ser555, and p-AMPKαThr172; no significant difference in phosphorylation was observed between 1.25 and 10 μM.

Western Blot Analysis^[2]

Cell Line:

Mature primary murine adipocytes
Concentration:

1.25 or 10 μM
Incubation Time:

3 days
Result:

Increased p-ACCSer79; no significant increase in p-ULK1Ser555 or p-AMPKαThr172 was observed.

RT-PCR^[2]

Cell Line:

Differentiating primary mADSCs
Concentration:

1.25 μM
Incubation Time:

8 days
Result:

Reduced Pparg, Lpl, Plin1, Adipoq, and Lep mRNA.

ELISA Assay^[2]

Cell Line:

Differentiating primary mADSCs
Concentration:

1.25 μM
Incubation Time:

During differentiation
Result:

Reduced cellular TGFβ protein but did not significantly alter downstream ERK/SMAD signaling.

Parmacokinetics

Species	Dose	Route	AUC_0-∞	T_1/2	CL	V_ss	C_max	Bioavailability
Mice^[4]	1 mg/kg	i.v.	2.3 μM·h	2.8 h	13.5 mL/min/kg	0.78 L/kg	/	/
Mice^[4]	5 mg/kg	p.o.	5.12 μM·h	3 h	/	/	1.54 μM	45 %

In Vivo

BI-9774 (30 mg/kg; oral gavage; once daily; 6 weeks) reduces terminal liver weight by 2.5%, hepatic lipids by 10%, significantly decreases plasma ALT levels, and slows the progression of sebaceous atrophy in male Lep^ob/Lep^ob NASH mice induced by AMLN diet, whereas no significant changes are observed in hepatic collagen-I immunopositive area or NAS^[4].
BI-9774 (30 mg/kg; oral gavage; once daily; 6 weeks) reduces hepatic Col1a1, Col1a2, Col4a1 and Timp1 mRNA by 61%, 59%, 55% and 55%, respectively, and decreases circulating IL-6, IL-1β and KC/GRO in AMLN diet-induced Lep^ob/Lep^ob mice, while Col5a1 mRNA and hepatic CD68⁺ macrophage infiltration show no significant changes^[4].
BI-9774 (30 mg/kg; oral gavage; once daily; 4 weeks) impairs glucose tolerance in AMLN diet-induced Lep^ob/Lep^ob mice, accompanied by a dose-dependent decrease in plasma insulin at 15 min after glucose loading^[4].
BI-9774 (1, 3, 10, or 30 mg/kg; oral gavage; single administration; 1 h before glucose challenge) dose-dependently improves glucose control in diet-induced obese male C57BL/6 mice^[4].
BI-9774 (30 mg/kg; oral gavage; once daily; 6 weeks) increases the heart weight/body weight ratio by 13.3%, enhances myocardial glycogen storage and ventricular wall thickness, and dose-dependently restores Nppa and Ankrd1 expression in AMLN diet-induced Lep^ob/Lep^ob mice^[4].

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

Animal Model:

Lep^ob/Lep^ob (male, ~8 weeks old, fed high trans-fat/high fructose/high cholesterol AMLN diet for 14 weeks)^[4]
Dosage:

3 mg/kg
Administration:

Oral gavage; once daily; for 6 weeks
Result:

Macrosteatosis worsened in 50% of mice versus 63% in the vehicle group.

Animal Model:

C57BL/6 (male, ~6 months old, diet-induced obese via 60% kcal high-fat diet for 3.5 months)^[4]
Dosage:

1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

p.o.; single dose
Result:

Showed a dose-dependent reduction in glucose area under the curve (AUC) relative to vehicle-treated mice, consistent with improved glucose control.

Animal Model:

Lepob/Lepob (male, ~8 weeks old, fed high trans-fat/high fructose/high cholesterol AMLN diet for 14 weeks)^[4]
Dosage:

30 mg/kg
Administration:

Oral gavage; once daily; for 6 weeks
Result:

Reduced terminal liver weight by 2.5% and liver lipid by 10%.
Reduced plasma ALT significantly.
Reduced Col1a1, Col1a2, Col4a1, and Timp1 mRNA by 61%, 59%, 55%, and 55%, respectively.
Reduced circulating IL-6, IL-1β, and KC/GRO.
Did not significantly alter collagen-I immunopositive area or NAS.
Increased heart weight/body weight ratio by 13.3%, cardiac glycogen storage, and ventricular wall thickness.

Related Protocols :

Chemical Information

CAS No. 1644498-53-2
분자량 541.02
화학식 C₂₆H₂₅ClN₄O₅S
SMILES

O(C1=NC=2C(N1)=CC(Cl)=C(N2)C3=CC=C(C=C3)C4=CC=C(N=S(C)(C)=O)C=C4)[C@H]5[C@@]6([C@](OC5)([C@H](O)CO6)[H])[H]
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 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]. Himmelsbach F, et al. NEW AZABENZIMIDAZOLE DERIVATIVES. WO 2015/007669 A1. 2015-01-22.

[2]. Bustraan S, et al. AMP-activated protein kinase activation suppresses leptin expression independently of adipogenesis in primary murine adipocytes. The Biochemical journal. 2024 Mar 06;481(5):345-362.

[3]. Papadopoulou G, et al. Adenosine 2A receptor-dependent activation of AMPK represses T17 cell pathogenicity through epigenetic and metabolic reprogramming. Science signaling. 2025 Sep 23;18(905):eadr3177.

[4]. Mather KM, et al. Direct β1/β2 AMPK activation reduces liver steatosis but not fibrosis in a mouse model of non-alcoholic steatohepatitis. bioRxiv [Preprint]. 2024 Jun 2:2024.05.30.596624.

Calculators

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

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Volume Volume

Molecular Weight Molecular Weight

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Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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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BI-9774

All AMPK Isoforms