Manidipine 2HCl

Catalog No.S2482 Batch:S248202

Technical Data

Formula	C₃₅H₃₈N₄O₆.2HCl
Molecular Weight	683.62	CAS No.	89226-75-5
Solubility (25°C)*	In vitro	DMSO	137 mg/mL (200.4 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Manidipine 2HCl (CV-4093) is a HCl salt form of Manidipine, which is a calcium channel blocker with IC50 of 2.6 nM, used clinically as an antihypertensive. Phase 4.

Targets

Calcium channel ^[1]
(Guinea-pig single ventricular cells )

2.6 nM

In vitro

At a holding potential of −37 mV, Manidipine decreases the Ca²⁺ current at concentrations above 0.1 nM, and abolishes it at 100 nM. ^[1] Manidipine concentration-dependently inhibits the calcium concentration response curves. Manidipine inhibits coronay artery and renal artery with pIC50 of 9.3 nM and 9.1 nM, respectively. ^[2] Manidipine partly inhibits sympathetic nerve activity and suppresses the mean arterial pressure response to infused norepinephrine. Manidipine also inhibits aldosterone secretion. Manidipine increases in both urinary calcium and uric acid. ^[3] In addition, Manidipine, at nanomolar concentrations, is efficacious in modulating gene transcriptions that are involved in proinflammatory changes of mesangial cells. ^[4]

In vivo

Manidipine (3 mg/kg and 10 mg/kg, p.o.) dose-dependently decreases systolic blood pressure in the three types of hypertensive rats. At the dose of 10 mg/kg, Manidipine decreases the blood pressure to the normotensive level between 1 hour and 3 hours after Manidipine is administered; the antihypertensive effect lasted for at least 8 hours. ^[5] When Manidipine is administered at 10 μg/kg, the hypotensive action is markedly augmented. ^[6] Manidipine potently inhibits the Ca inward current, When the potential is at -60 mV. Manidipine consistently inhibits the Ca current evoked by depolarization to 0 mV. However, a low concentration of Manidipine (1-3 nM) enhances the Ca current evoked by the depolarizing pulse of -20 mV, when the membrane potential is held at -80 mV. Inhibition of the Ca current induced by Manidipine develops slowly and over 10 minutes is required to reach the maximum inhibition. ^[7]

Protocol (from reference)

Cell Assay:^{^[4]}	Cell lines Mesangial cells Concentrations 10 nM Incubation Time Days 1, 3 and 5 Method The mitogenic effect is measured by the amout of [3H]thymidine incorporated into DNA of human MCs and by assessment of cell proliferation. In brief, 1 × 105 quiescent cells is seeded into a 25-mL cell culture bottle and kept in low serum medium (0.1% FCS). On the following day, the cells are preincubated for 3 hours with Manidipine (10 nM) followed by stimulation with PDGF-BB (10 ng/mL) or incubated with low serum medium abone. The medium is replaced each day, and the cells are counted at days 1, 3 and 5.
Animal Study:^{^[5]}	Animal Models Normotensive male Wistar-Kyoto rats and male stroke-prone SHR Dosages 1 mg/kg, 3 mg/kg and 10 mg/kg Administration Administered via p.o.

Cell Assay:^{^[4]}

Cell lines
Mesangial cells
Concentrations
10 nM
Incubation Time
Days 1, 3 and 5
Method
The mitogenic effect is measured by the amout of [3H]thymidine incorporated into DNA of human MCs and by assessment of cell proliferation. In brief, 1 × 105 quiescent cells is seeded into a 25-mL cell culture bottle and kept in low serum medium (0.1% FCS). On the following day, the cells are preincubated for 3 hours with Manidipine (10 nM) followed by stimulation with PDGF-BB (10 ng/mL) or incubated with low serum medium abone. The medium is replaced each day, and the cells are counted at days 1, 3 and 5.

Animal Study:^{^[5]}

Animal Models
Normotensive male Wistar-Kyoto rats and male stroke-prone SHR
Dosages
1 mg/kg, 3 mg/kg and 10 mg/kg
Administration
Administered via p.o.

References

+ Expand

Customer Product Validation

: Data from [Data independently produced by , , Antiviral Res, 2018, 150:130-136]

Selleck's Manidipine 2HCl has been cited by 3 publications

Selective Translation of Maternal mRNA by eIF4E1B Controls Oocyte to Embryo Transition [ Adv Sci (Weinh), 2023, 10(11):e2205500]	PubMed: 36755190
HCMV-IE2 promotes atherosclerosis by inhibiting vascular smooth muscle cells' pyroptosis [ Front Microbiol, 2023, 14:1177391]	PubMed: 37234524
Evidence for Specific Receptor-Mediated Toxicity of Pharmaceuticals in Aquatic Organisms Derived from Acute and Chronic Standard Endpoints [ Environ Toxicol Chem, 2021, 10.1002/etc.5018]	PubMed: 33595135

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.