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Barnidipine hydrochloride

MCE China：Barnidipine hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-107322

CAS：104757-53-1

Synonyms：Mepirodipine hydrochloride; YM-09730-5

Purity：99.96%

Storage：4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Barnidipine (Mepirodipine) hydrochloride is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki = 0.21 nmol/L, has selective action against CaA receptors. Barnidipine hydrochloride is an orally active antihypertensive agent that can reduce the level of platelet-derived growth factor B-chain mRNA and peripheral vascular resistance.

In Vivo：Barnidipine hydrochloride (53 mg/kg; Feed administration; 3 weeks) reduces the level of platelet-derived growth factor B chain mRNA, and has a effect on lowering blood pressure in spontaneously hypertensive rats[2]. Pharmacokinetic analysis in rats and dogs after intravenous administration[3] Parameters Rat Dog Dose (mg/kg) 0.05 0.05 C0 (ng/ml) 57.9 40.2 t1/2α (h) 0.06 0.3 t1/2β (h) 0.6 4.1 AUC (ng·h/ml) 17.7 30.2 Clp (l/h/kg) 2.8 1.7 CLb (l/h/kg) 5.2 3.3 V1 (l/kg) 0.9 1.3 V2 (l/kg) 1.1 2.8 Vdss (l/kg) 2.0 4.1 Kel (h-1) 3.3 1.3 K12 (h-1) 4.9 0.6 K21 (h-1) 3.9 0.3 Pharmacokinetic analysis in rats after oral administration[3] Parameters 0.4 (mg/kg) 1.0 (mg/kg) 3.0 (mg/kg) tmax (h) 0.3 0.3 0.3 Cmax (ng/ml) 19.0 75.8 292.6 AUC0-∞ (ng·h/ml) 15.2 47.4 191.1 t1/2β (h) 1.0 1.7 1.0 F (%) 11 13 18 Pharmacokinetic analysis in dogs after oral administration[3] 口服后在犬中的药代动力学分析[3] Parameters 0.2 (mg/kg) 0.4 (mg/kg) 1.0 (mg/kg) tmax (h) 0.3 0.4 0.3 Cmax (ng/ml) 4.6 9.7 44.0 AUC0-∞ (ng·h/ml) 6.8 16.2 60.2 t1/2β (h) 4.3 3.6 3.6 F (%) 6 7 9 Pharmacokinetic analysis in dogs after oral administration[3] 口服后在犬中的药代动力学分析[3] Parameters 0.2 (mg/kg) 0.4 (mg/kg) 1.0 (mg/kg) tmax (h) 0.3 0.4 0.3 Cmax (ng/ml) 4.6 9.7 44.0 AUC0-∞ (ng·h/ml) 6.8 16.2 60.2 t1/2β (h) 4.3 3.6 3.6 F (%) 6 7 9 Pharmacokinetic analysis in dogs after oral administration[3] 口服后在犬中的药代动力学分析[3] Parameters 0.2 (mg/kg) 0.4 (mg/kg) 1.0 (mg/kg) tmax (h) 0.3 0.4 0.3 Cmax (ng/ml) 4.6 9.7 44.0 AUC0-∞ (ng·h/ml) 6.8 16.2 60.2 t1/2β (h) 4.3 3.6 3.6 F (%) 6 7 9 Pharmacokinetic analysis in dogs after oral administration[3] 口服后在犬中的药代动力学分析[3] Parameters 0.2 (mg/kg) 0.4 (mg/kg) 1.0 (mg/kg) tmax (h) 0.3 0.4 0.3 Cmax (ng/ml) 4.6 9.7 44.0 AUC0-∞ (ng·h/ml) 6.8 16.2 60.2 t1/2β (h) 4.3 3.6 3.6 F (%) 6 7 9 Pharmacokinetic analysis in dogs after oral administration[3] Parameters 0.2 (mg/kg) 0.4 (mg/kg) 1.0 (mg/kg) tmax (h) 0.3 0.4 0.3 Cmax (ng/ml) 4.6 9.7 44.0 AUC0-∞ (ng·h/ml) 6.8 16.2 60.2 t1/2β (h) 4.3 3.6 3.6 F (%) 6 7 9

IC50 & Target：L-type calcium channel

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References：

[1]. van Zwieten PA, et al. Pharmacological profile of barnidipine: a single optical isomer dihydropyridine calcium antagonist. Blood Press Suppl. 1998;1:5-8.  [Content Brief]

[2]. Hashimoto M, et al. Treatment with a Ca(2+) channel blocker, barnidipine, reduces platelet-derived growth factor B-chain mRNA in glomeruli of spontaneously hypertensive rats. Am J Nephrol. 1999;19(5):615-21.  [Content Brief]

[3]. Teramura T, et al. Pharmacokinetics of barnidipine hydrochloride, a new dihydropyridine calcium channel blocker, in the rat, dog and human. Xenobiotica. 1995 Nov;25(11):1237-46.  [Content Brief]

[4]. Malhotra HS, et al. Barnidipine. Drugs. 2001;61(7):989-96; discussion 997-8.  [Content Brief]