Remodelin


CAS No. : 949912-58-7

949912-58-7
Price and Availability of CAS No. : 949912-58-7
Size Price Stock
5mg $66 In-stock
10mg $99 In-stock
25mg $180 In-stock
50mg $240 In-stock
100mg $320 In-stock
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Cat. No. : HY-16706
M.Wt: 282.36
Formula: C15H14N4S
Purity: >98 %
Solubility: DMSO : 125 mg/mL (ultrasonic)
Introduction of 949912-58-7 :

Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model[1][2][3][4]. In Vitro:Remodelin (10-40 μΜ, 1-7 days) inhibits NAT10 activity and cell proliferation with a dose-dependent manner in both AR-positive and AR-negative prostate cancer cells[2].
Remodelin (20 μΜ, 24 hours) inhibits NAT10 and slows DNA replication in prostate cancer cells[2].
Remodelin (1 μΜ, 7 days) decreases nuclear shape defects and increase genomic stability in LmnaG609G/G609G fibroblasts[3].
In Vivo:Remodelin (2 or 20 mg/kg, i.p., once every two days for 4 weeks) significantly reduces AR-negative prostate cancer tumor growth in tumor xenograft nude mice model[2].
Remodelin (100 mg/kg, p.o.) inhibits NAT10 and significantly enhances the healthspan in aLmnaG609G/G609G hutchinson-gilford progeria syndrome (HGPS) mouse model. Remodelin (5 mg/kg, p.o.) shows a T1/2 of 1.81 hours and oral bioavailability (F%) of 43.5% in mice[3].
Pharmacokinetic parameters for Remodelin in Mice[1]
Pharmacokinetic parameters for Remodelin in Mice[1]
Route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng/h/mL) AUC0-Ꝏ (ng/h/mL) MRT_last (h) F(%)
p.o. 5 1.81 0.25 409 235 259 0.84 43.5%

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Route Dose (mg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng/h/mL) AUC0-Ꝏ (ng/h/mL) MRT_last (h) F(%)
p.o. 5 1.81 0.25 409 235 259 0.84 43.5%