Disease Area, Renal Disease
Product Name: CDDO (Bardoxolone) l anti-inflammatory (#C2336-5)
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CDDO is a synthetic oleanane triterpenoid. It is 400,000x more potent than natural product oleanolic acid in
inhibiting cellular iNOS production when stimulated by IFN-gamma, TNF-alpha, and IL-1 [1]. The
mechanism of action of CDDO remain elusive, despite its broad biological activities, including proliferation
inhibition, apoptosis induction[2], and oxidative stress and inflammation suppression.
CDDO-methyl ester,an orally-available form of CDDO, is undergoing clinical development for the treatment of
advanced chronic kidney disease (CKD) in type 2 diabetes mellitus patients.
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Details
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Chemical Formula:
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C31H41NO4
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CAS No.:
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218600-44-3
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Molecular weight:
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491.66
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Purity:
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> 98%
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Appearance:
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Brown
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Chemical name:
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2-cyano-3, 12-dioxo-oleana-1,9(11)-dien-28-oic acid
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Solubility:
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Up to 10 mM in DMSO
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Synonyms:
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CDDO, RTA-401, RTA401, Bardoxolone
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Storage:
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For longer shelf life, store solid powder or DMSO solution at -20oC
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1. Sporn MB, et al. New synthetic triterpenoids: potent agents for prevention and treatment of tissue injury
caused by inflammatory and oxidative stress. J Nat Prod. 2011; 74(3):537-45. Pubmed ID: 21309592
2. Suh N, et al. A novel synthetic oleanane triterpenoid, 2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid, with
potent differentiating, antiproliferative, and anti-inflammatory activity. Cancer Res. 1999; 59(2):336-41.
Pubmed ID: 9927043
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Product Name: FG-4592 (ASP1517) l HIF prolyl-hydroxylase hibitor (#C3445-10)
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FG-4592 is an orally-available isoquinoline-based inhibitor of hypoxia-inducible factor (HIF) prolyl
hydroxylase for the treatment of anemia and patients with chronic kidney disease. [1] Phase 2 studies
indicate that oral administration of FG-4592 three times a week increased mean hemoglobin levels in the first
eight weeks, regardless of supplementation with IV or oral iron, or no iron supplementation. FG-4592 is novel
in that it allows integration of red blood cell production and efficient iron incorporation simultaneously. [1]
Data from Phase 2 trials comparing with epoetin alpha indicate that treatment with FG-4592 alone results in a
sustained reduction of total plasma cholesterol levels by an average of 20%, while no reduction was seen
with epoetin alpha. [2, 3]
In December, 2012, Fibrogen and Astellas Pharma announced the initiation of a Phase 3 clinical development
program for the treatment of anemia associated with chronic kidney disease in patients not on dialysis and
on dialysis. [4]
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Details
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Chemical Formula:
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C19H16N2O5
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CAS No.:
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808118-40-3
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Molecular weight:
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353.24
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Purity:
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> 98%
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Appearance:
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Yellow
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Chemical name:
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2-(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxamido)acetic acid
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Solubility:
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Up to 100mM in DMSO
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Synonyms:
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FG-4592, FG4592, ASP1517
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Storage:
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For longer shelf life, store solid powder at 4oC desiccated, or DMSO solution
at -20oC
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References
1. "Correction of anemia without IV iron supplementation in incident dialysis patients" Fibrogen press release,
Nov. 5, 2012
2. "FG-4592 and epoetin alpha in Phase II anemia study", Datamonitor Research Store, Nov. 11, 1012.
3. "Hemoglobin correction and maintenance in end-stage renal patients" Fibrogen press release, Nov. 5, 2012
4. Fibrogen press release, Dec. 11, 2012 (Phase 3 announcement)
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