Methyclothiazide

135-07-9

360.24

H2O : < 0.1 mg/mL (insoluble); DMSO : 72 mg/mL (199.87 mM; Need ultrasonic and warming)

Metabolic Enzyme/Protease

Methyclothiazide is an orally active antihypertensive agent and a diuretic agent. Methyclothiazide leads to a reduction of the vascular response to the action of endogenous vasoconstricting stimuli, such as Norepinephrine (HY-13715). Methyclothiazide is against voltage-dependent Ca-channel (VDCC) activity in vitro^[1][2][3]. IC50 & Target: IC50: voltage-dependent Ca-channel (VDCC) In Vitro: Methyclothiazide (0-100 uM) induces endothelium-dependent inhibition of the vasoconstrictor responses to NE and AVP only in aortas from SHR, and the maximal vasoconstrictive effect of Norepinephrine (HY-13715) and arginine vasopressin (AVP) is decreased by 59% and 32.3 %, respectively^[1].
Methyclothiazide (0-100 uM) induces inhibitory effect on the contractile response to Norepinephrine (HY-13715) is abolished by N-nitro-L-arginine (NOLA) but not indomethacin^[1].
Methyclothiazide (100 uM) affects the vascular responses to extracellular Ca²⁺ under high-K⁺ depolarizing conditions. It can reduce Ca²⁺ contracture in a high-K⁺, Ca²⁺-free solution. The maximal contracture is reduced by 90.4%^[1].