SB525334 free base · Synonyms: SB-525334 · SB 525334

SB 525334 is a potent and selective transforming growth factor β1 receptor inhibitor.

For research use only. Not for human or veterinary use.

Purity >98% Stock Inquire

Data Sheet SDS COA

SB525334 structure

CAS No.: 356559-20-1

Pack sizes & pricing

Size	Price	SKU	Stock
1 g	USD 328.00	BP-02068-1g	In stock	Get quote
5 g	USD 1,350.00	BP-02068-5g	In stock	Get quote
10 g	USD 2,450.00	BP-02068-10g	In stock	Get quote
25 g	Inquire	BP-02068-25g	Inquire	Inquire

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Description

SB 525334 is a potent and selective transforming growth factor β1 receptor (ALK5) inhibitor with an IC50 of 14.3 nM.

Biological activity

In Vitro SB525334 (1 μM; for 15 minutes before stimulating with 0.625 ng/ml of TGF-β1, assesses after 6 days) inhibits TGF-β1-mediated proliferation of familial idiopathic pulmonary arterial hypertension (iPAH) pulmonary artery smooth muscle cells (PASMCs) at an IC50 of 295 nM. In Vivo SB525334 (3-30 mg/kg; p.o.; daily from days 17 to 35) significantly reverses pulmonary arterial pressure in a rat model of pulmonary arterial hypertension (PAH).

Identifiers

SMILES: CC1=CC=CC(=N1)C1=C(N=C(N1)C(C)(C)C)C1=CC=C2N=CC=NC2=C1
InChIKey: DKPQHFZUICCZHF-UHFFFAOYSA-N

Specifications

MW (average): 343.4249
Formula: C₂₁H₂₁N₅
CAS No.: 356559-20-1
Physical state: Solid
Color: Light yellow to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

References

[1]. Grygielko ET, et al. Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis. J Pharmacol Exp Ther, 2005, 313(3), 943-951.

[2]. Thomas M, et al. ALK5 mediates abnormal proliferation of vascular smooth muscle cells from patients with familial pulmonary arterial hypertension and is involved in the progression of experimental pulmonary arterial hypertension induced by monocrotaline.

[3]. Laping NJ, et al. Tumor-specific efficacy of transforming growth factor-beta RI inhibition in Eker rats. Clin Cancer Res, 2007, 13(10), 3087-3899.