Antifibrotic agent 1

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Antifibrotic agent 1 is an orally active anti-idiopathic pulmonary fibrosis (IPF) agent. Antifibrotic agent 1 effectively attenuates IPF-related processes, including TGF-β induced EMT and FMT processes, as well as pro-fibrotic M2 polarization. Antifibrotic agent 1 selectively inhibits CSF-1R, PDGFR-α and Src family kinases (SFKs), while sparing VEGFRs, FGFRs and Abl to minimize off-target toxicity. Antifibrotic agent 1 has potent anti-fibrotic activity in Bleomycin (BLM) (HY-108345)-induced pulmonary fibrosis mice model.

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Antifibrotic agent 1 Chemical Structure

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•Related Small Molecules:

•Related Proteins:

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PDGFR PDGFRβ PDGFRα

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Lck Fyn Blk Hck Lyn Yes

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

PDGFRα

Collagen I

40.5 nM (IC₅₀)

Fyn

Hck

Lyn

Lck

Yes

In Vitro

Antifibrotic agent 1 (Compound 22) (0.001-10 μM，48 h,) exhibits profound anti-fibrotic activity, suppressing COL1A1 expression by 95.0% at 1 μM, with an IC₅₀ of 40.5 nM in A549 cells^[1].
Antifibrotic agent 1 (1-200 μM) exhibits anti-fibrotic effects with low cytotoxicity across A549, HEK293 and L02 cells (CC_{50_{> 200μM)^[1].

Antifibrotic agent 1 (0.1-10 μM, 48 h) dose-dependently reduces the protein level of COL1A1, inhibiting IPF-related EMT and FMT processes in TGF-β-stimulated A549, HFL1 and HLFs cells^[1].

Antifibrotic agent 1 (1-10 μM, 48 h) selectively inhibits the bone marrow-derived macrophages (BMDM) polarization towards the pro-fibrotic M2 phenotype at a concentration of 10 μM^[1].

Antifibrotic agent 1 (1-100 nM) selectively inhibits CSF-1R, PDGFR-α and SFKs to mitigate IPF progression, while sparing VEGFRs, FGFRs and Abl to minimize off-target toxicity^[1].}}

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

Western Blot Analysis^[1]

Cell Line:	A549 cells, HFL1 cells, HLFs cells
Concentration:	0.1, 0.5, 1, 10 μM
Incubation Time:	48 h after TGF-β stimulated 48 h
Result:	Dose-dependently reduced the protein level of COL1A1 in IPF-related EMT and FMT models and primary human lung fibroblasts model.

Parmacokinetics

Species	Dose	SampleTime	Route	Indicator	value
Mice	2 mg/kg	0.25, 0.5, 1, 2, 4, 8, 24 h	i.v.	T_1/2	2.37 hr
Mice	5 mg/kg	0.25, 0.5, 1, 2, 4, 8, 24 h	p.o.	T_1/2	3.15 hr
Mice	2 mg/kg	0.25, 0.5, 1, 2, 4, 8, 24 h	i.v.	AUC_last	437 ng·h/mL
Mice	5 mg/kg	0.25, 0.5, 1, 2, 4, 8, 24 h	p.o.	T_max	0.42 hr
Mice	2 mg/kg	0.25, 0.5, 1, 2, 4, 8, 24 h	i.v.	MRT_0-∞	0.4 hr
Mice	5 mg/kg	0.25, 0.5, 1, 2, 4, 8, 24 h	p.o.	C_max	137 ng·h/mL
Mice	2 mg/kg	0.25, 0.5, 1, 2, 4, 8, 24 h	i.v.	CL	79.8 mL/min/kg
Mice	5 mg/kg	0.25, 0.5, 1, 2, 4, 8, 24 h	p.o.	MRT_0-∞	2.32 hr
Mice	2 mg/kg	0.25, 0.5, 1, 2, 4, 8, 24 h	i.v.	V_ss	1.802 L/kg
Mice	5 mg/kg	0.25, 0.5, 1, 2, 4, 8, 24 h	p.o.	F	12.6 %

In Vivo

Antifibrotic agent 1 (Compound 22) (60  mg/kg, p.o., daily for 14 days) has a moderate oral bioavailability and favorable safety profile, with no significant hepatotoxicity or nephrotoxicity at doses up to 60 mg/kg in BLM-induced pulmonary fibrosis mice model^[1].
Antifibrotic agent 1 (60  mg/kg, p.o., daily for 10 days) has superior anti-fibrotic efficacy, significantly alleviating lung fibrosis, reducing inflammation and pro-fibrotic M2-associated cytokine levels, and improving lung function in BLM-induced pulmonary fibrosis mice model^[1].

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

Animal Model:	Male C57BL/6 mice (8 weeks old) were given an intratracheal administration of BLM (1.8 mg/kg) to induce pulmonary fibrosis^[1].
Dosage:	30, 60 mg/kg
Administration:	Oral gavage (p.o.), daily for 14 days and then measured body and lung tissues weight as well as collected lung tissues.
Result:	Significantly alleviated weight losses, increased survival rate and improved lung functions with increased lung coefficient value in mice mode. Notably downregulated Tgf-β mRNA, reduced both the mRNA and protein levels of Fn1 and Col1a1, and decreased hydroxyproline content in the lung tissues in mice model at the dose of 60 mg/kg. Significantly reduced Tnf and Ccl2 mRNA levels but increased IL-10 mRNA level, modulating inflammation to further alleviate pulmonary fibrosis in mice model. Strongly downregulated M2-associated genes (Arg1, Mrc1) but not the M1 marker CD86, selectively inhibiting M2 macrophage polarization without significantly affecting M1 polarization in mice model. Potently alleviated pathological changes related lung fibrosis and decreased collagen fibers with a 54.6 % reduction in fibrosis area in mice model at the dose of 60 mg/kg.

Molecular Weight

498.96

Formula

C₂₇H₂₃ClN₆O₂

SMILES

CC(NC1=CC=C(C(Cl)=C1)NC(C2=CC=C(C(C#CC3=CC(C4=CN(N=C4)C)=CN=C3N)=C2)C)=O)=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

Handling Instructions (2659 KB)

References

[1]. Chen X, et al. Design, synthesis, and biological evaluation of N-(2-amino-phenyl)-5-(4-aryl-pyrimidin-2-yl) amino)-1H-indole-2-carboxamide derivatives as novel inhibitors of CDK9 and class I HDACs for cancer treatment [J]. Bioorganic Chemistry, 2025: 108577.