Perindopril-d₃ erbumine  (Synonyms: Perindopril-d₃ tert-butylamine salt; S-9490-d₃ erbumine)

Perindopril-d₃ (erbumine) is deuterated labeled Perindopril (erbumine) (HY-B0130A). Perindopril erbumine is an angiotensin-converting enzyme inhibitor. Perindopril erbumine modulates NF-κB and STAT3 signaling and inhibits glial activation and neuroinflammation. Perindopril erbumine can be used for the research of Chronic Kidney Disease and high blood pressure^[1][2][3][4].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].
Perindopril erbumine (1 μM, 24 h) ameliorats gliosis and blunts decrease induced by LPS (HY-D1056) in AT2R expression in Rat astrocytoma cell line (C6) and murine microglial cell line (BV2)^[2].
Perindopril erbumine (1 μM, 24 h) prevents IκBα degradation, NF-кB nuclear translocation and STAT3 activation induced by LPS (HY-D1056) in C6 and BV2^[2].
Perindopril erbumine (1 μM, 24 h) ameliorats the imbalance in the release of inflammatory cytokine and blunts the aberrant ROS production and the nitrite release induced by LPS (HY-D1056) in C6 and BV2^[2].

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

Perindopril erbumine (0.1 mg/kg, Oral gavage, once a day for five consecutive days) prevents LPS-induced neuroinflammation in rats^[2].
Perindopril erbumine (0.42 mg/kg, Oral, once a day for 4 weeks) with Huangqi-Danshen decoction (HDD) (4.7 g/kg, Oral, once a day for 4 weeks) attenuates adenine(HY-B0152)-induced Chronic kidney disease (CKD) in rats^[3].
Perindopril erbumine (0.4-1.5 mg/kg, Oral, once a day for 4-24 weeks) has a persistent effect on blood pressure in spontaneously hypertensive rats (SHR)^[5].

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

444.62

C₂₃H₄₀D₃N₃O₅

107133-36-8

O=C([C@H]1N(C([C@@H](N[C@H](C(OCC)=O)CCC)C([2H])([2H])[2H])=O)[C@@]2([H])CCCC[C@@]2([H])C1)O.CC(C)(C)N

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Bhat S A, et al. Angiotensin receptor blockade modulates NFκB and STAT3 signaling and inhibits glial activation and neuroinflammation better than angiotensin-converting enzyme inhibition [J]. Molecular neurobiology, 2016, 53: 6950-6967.  [Content Brief]

  [3]. Wei X, et al. Combination of perindopril erbumine and huangqi-danshen decoction protects against chronic kidney disease via sirtuin3/mitochondrial dynamics pathway [J]. Evidence-Based Complementary and Alternative Medicine, 2022, 2022.  [Content Brief]

  [4]. Afonso T, et al. Pharmacodynamic evaluation of 4 angiotensin‐converting enzyme inhibitors in healthy adult horses [J]. Journal of veterinary internal medicine, 2013, 27(5): 1185-1192.  [Content Brief]

  [5]. Thybo N K, et al. Dose-dependent effects of perindopril on blood pressure and small-artery structure [J]. Hypertension, 1994, 23(5): 659-666.  [Content Brief]