Minodronic acid (hydrate)

Minodronic acid (YM-529) hydrate is an FPP synthase inhibitor with an IC₅₀ of 3 nM, and also an antagonist of P2X2/3 receptors with an IC₅₀ of 62.7 μM. Minodronic acid hydrate induces tumor cell apoptosis and inhibits cell growth. Minodronic acid hydrate also suppresses bone resorption. Minodronic acid hydrate can be used in research related to osteoporosis and cancer^[1][2]. In Vitro:Minodronic acid (5-100 μM; 72 h) hydrate inhibits the proliferation of human bladder cancer cell lines 253J, 5637, RT4, RT112, TCCSUP, KU-7 and UM-UC-3 in a dose-dependent manner^[1].
Minodronic acid (30 μM; 48 h) hydrate induces apoptosis in human bladder cancer cells^[1].
Minodronic acid (0.25-2.0 × IC₅₀; 72 h) hydrate exhibits synergistic or additive antiproliferative effects when combined with Cisplatin (HY-17394) or Paclitaxel (HY-B0015) in human bladder cancer cell lines KU-7, RT112 and UM-UC-3^[1].
Minodronic acid (0.1-1 μM; 3 days) hydrate potently inhibits osteoclast-mediated bone resorption in rabbits and induces dose-dependent morphological changes; at 1 μM, it almost completely inhibits bone resorption and causes osteoclast detachment, while at 0.1 μM, it only exerts partial inhibitory effects accompanied by the disappearance of the ruffled border^[2]. In Vivo:Minodronic acid (80 μg/kg; subcutaneous injection; once weekly; for 3 consecutive weeks) hydrate significantly inhibits the growth of bladder cancer bone metastases in BALB/c nu/nu mice without causing adverse effects^[1].
Minodronic acid (30-100 μM; transurethral administration; 5 days) hydrate inhibits the growth of orthotopic bladder cancer in SCID mice ^[1].
Minodronic acid (0.05-5 mg/kg; subcutaneous injection; single administration) hydrate accumulates in the calcified and ossified regions of rat bones, concentrates in osteoclast-containing bone tissue sites, and exhibits dose-dependent bone tissue localization characteristics^[2].