J-1149

Cat. No.: HY-163429: FAQs
Data Sheet Handling Instructions

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J-1149 is a potent ALK5 inhibitor, with an IC₅₀ value of 0.017 μM. J-1149 also shows weak p38α MAP kinase inhibitory activity, with an IC₅₀ value of 0.435 μM. J-1149 can be used for liver fibrosis research.

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

J-1149 Chemical Structure

CAS No. : 2883580-95-6

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

ALK5

0.017 μM (IC₅₀)

p38α MAPK

In Vitro

J-1149 (compound 15g) (5-40 μM, 24 h) efficiently inhibits extracellular matrix (ECM) deposition in TGF-β-induced hepatic stellate cells (HSCs), and eventually suppresses HSC activation^[1].
J-1149 (20 μM, 24 h) inhibits the expression of α-SMA and collagen I stimulated by TGF-β^[1].

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

Western Blot Analysis^[1]

Cell Line:	LX-2 cells
Concentration:	20 μM
Incubation Time:	1 h prior to TGF-β stimulation for continuous 24 h
Result:	Inhibited the expression of α-SMA and collagen I stimulated by TGF-β.

In Vivo

J-1149 (compound 15g) shows a good pharmacokinetic (PK) profile with a favorable half-life (t_1/2 = 9.14 h)^[1].

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

Animal Model:

Sprague Dawley (SD) rats^[1]

Dosage:

4 mg/kg (IV), 15 mg/kg (PO)

Administration:

IV or PO, once (Pharmacokinetic Analysis)

Result:

Pharmacokinetic Parameters of J-1149 in male Sprague-Dawley rats^[1].

	IV (4 mg/kg)	PO (15 mg/kg)
T_max (h)	0.00 ± 0.00	0.11 ± 0.13
C_max (ng/mL)	43,144 ± 35,001	1386 ± 882
AUC_0-t (ng/mL∗h)	12,529 ± 978	1217 ± 20
AUC_0-∞ (ng/mL∗h)	12,802 ± 1160	2667 ± 1136
t_1/2 (h)	2.24 ± 1.05	9.14 ± 5.13
CL (mL/h/kg)	314 ± 28	6564 ± 3372
F (%)		2.59%

Molecular Weight

452.51

Formula

C₂₅H₂₄N₈O

CAS No.

2883580-95-6

SMILES

N[C@H](CC1=CC=CC=C1)C(NCC2=NC(C3=CC=CC(C)=N3)=C(C4=CN5C(C=C4)=NC=N5)N2)=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]. Meng YQ, et al. Synthesis and anti-liver fibrosis activity of imidazole and thiazole compounds containing amino acids. Eur J Med Chem. 2024 Mar 13;269:116311. [Content Brief]

J-1149 Related Classifications

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Dilution Calculator

The molarity calculator equation

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

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

J-11492883580-95-6J1149J 1149TGF-β Receptorp38 MAPKTransforming growth factor beta receptorsTGF-βα-SMAcollagen ILX-2 cellsliver fibrosishepatic stellate cellsInhibitorinhibitorinhibit

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