An ALK5 inhibitor
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IN 1130

Item No. 43285

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[[5-(6-methyl-2-pyridinyl)-4-(6-quinoxalinyl)-1H-imidazol-2-yl]methyl]-benzamide
CAS Number
868612-83-3
Molecular Formula
C25H20N6O
Formula Weight
420.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
NC(C1=CC(CC2=NC(C3=CC=CC(C)=N3)=C(C4=CC(N=CC=N5)=C5C=C4)N2)=CC=C1)=O
InChi Code
InChI=1S/C25H20N6O/c1-15-4-2-7-20(29-15)24-23(17-8-9-19-21(14-17)28-11-10-27-19)30-22(31-24)13-16-5-3-6-18(12-16)25(26)32/h2-12,14H,13H2,1H3,(H2,26,32)(H,30,31)
InChi Key
RYKSGWSKILPDDY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $109

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    10 mg

    $207

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    25 mg

    $491

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    50 mg

    $818

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    Product Description

    IN 1130 is an inhibitor of activin receptor-like kinase 5 (ALK5), also known as TGF-β receptor type 1 (TGF-βRI; IC50 = 5.3 nM).1 It is selective for ALK5 over a panel of 27 other kinases at 5 µM. IN 1130 (10 mg/kg per day) decreases renal fibrogenesis, inflammatory cell infiltration, and tubular atrophy in a mouse model of unilateral ureteral obstruction. It also reduces kidney levels of TGF-β1, α-smooth muscle actin (α-SMA), hydroxyproline, and fibronectin in the same model. IN 1130 (5 mg/kg per day) decreases tunica plaque area, increases elastin fiber numbers, and reverses penile curvature in a rat model of Peyronie's disease induced by TGF-β1 overexpression.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Moon, J.-A., Kim, H.-T., Cho, I.-S., et al. IN-1130, a novel transforming growth factor-β type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy. Kidney Int. 70(7), 1234-1243 (2006).

    2. Ryu, J.-K., Piao, S., Shin, H.-Y., et al. IN-1130, a novel transforming growth factor-beta type I receptor kinase (activin receptor-like kinase 5) inhibitor, promotes regression of fibrotic plaque and corrects penile curvature in a rat model of Peyronie’s disease. J. Sex Med. 6(5), 1284-1296 (2009).