Azalanstat dihydrochloride  (Synonyms: RS-21607 dihydrochloride)

Azalanstat dihydrochloride (RS-21607 dihydrochloride) is an inhibitor of heme oxygenase and lanosterol 14α-demethylase, with inhibitory activity against HO-1 (IC₅₀ = 5.5 µM) and HO-2 (IC₅₀ = 24.5 µM). Azalanstat dihydrochloride reduces the maturation rate of rat oocytes, increases rat oocyte degeneration, and partially inhibits progesterone production in preovulatory follicles of rats^[1][2][3].

Azalanstat dihydrochloride (Compounds I) 可在体外抑制大鼠脾脏微粒体 HO-1 (IC₅₀ = 5.8 μM) 和大鼠脑微粒体 HO-2 (IC₅₀ = 28.0 μM)，对 HO-1 相对 HO-2 的选择性指数为 5^[1]。
Azalanstat dihydrochloride (0-100 μM) 可在体外抑制大鼠肝微粒体 CYP3A1/3A2 的活性，其 IC₅₀ 为 48.1 μM^[1]。
Azalanstat dihydrochloride (0-200 μM; 3-24 h, or 6 h + 24 h inhibitor-free culture) 在高浓度下 (6 h 处理时≥50 μM，24 h 处理时≥10 μM)，会以剂量和时间依赖的方式降低 GVBD，同时卵母细胞退化程度增加；其中在 100 μM 浓度下处理 6 h 后，卵母细胞的退化具有不可逆性^[2]。
Azalanstat dihydrochloride (1-100 μM; 6-24 h with 5 μg/mL LH) 在 1-100 μM 作用 24 h 时，它会以剂量依赖的方式降低 LH 诱导的 GVBD，同时伴随卵母细胞和卵泡的退化增加^[2]。
Azalanstat dihydrochloride (1-100 μM; 6-24 h with 5 μg/mL LH) 在 1、50、100 μM 浓度下作用 6 或 24 h 时，可在体外以剂量依赖的方式部分抑制大鼠排卵前卵泡中 LH 诱导的孕酮合成^[2]。

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

Azalanstat dihydrochloride (2.15-215 μg/bursa；囊内注射；单次给药) 可在测试的最高囊内剂量下显著抑制未成熟 Wistar 系雌性大鼠的排卵^[2]。

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

502.88

C₂₂H₂₆Cl₃N₃O₂S

143484-82-6

Room temperature in continental US; may vary elsewhere.

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

• [1]. Salerno L, et al. Progress in the development of selective heme oxygenase-1 inhibitors and their potential therapeutic application. Eur J Med Chem. 2019 Apr 1;167:439-453.  [Content Brief]

  [2]. Kinobe RT, et al. Selectivity of imidazole-dioxolane compounds for in vitro inhibition of microsomal haem oxygenase isoforms. Br J Pharmacol. 2006;147(3):307-315.  [Content Brief]

  [3]. Vaknin KM, et al. Role of meiosis-activating sterols in rat oocyte maturation: effects of specific inhibitors and changes in the expression of lanosterol 14alpha-demethylase during the preovulatory period. Biol Reprod. 2001 Jan;64(1):299-309.  [Content Brief]