Lercanidipine hydrochloride Chemical Properties

Melting point:

175-177°C

storage temp. 

2-8°C

solubility 

soluble in Methanol

form 

powder

color 

yellow

Merck 

14,5446

InChIKey

WMFYOYKPJLRMJI-UHFFFAOYSA-N

SMILES

C1(C)NC(C)=C(C(OC(C)(C)CN(CCC(C2=CC=CC=C2)C2=CC=CC=C2)C)=O)C(C2=CC=CC([N+]([O-])=O)=C2)C=1C(OC)=O.[H]Cl

CAS DataBase Reference

132866-11-6(CAS DataBase Reference)

Safety Information

Hazard Codes 

T

Risk Statements 

25

Safety Statements 

36/37-45

RIDADR 

UN 2811

WGK Germany 

3

HS Code 

2933.39.4100

Toxicity

LD50 in mice (mg/kg): 83 i.p.; 657 orally (Nardi)

Lercanidipine hydrochloride Usage And Synthesis

Chemical Properties

Pale-Yellow Powder

Uses

long-acting dihydropyridine calcium channel blocker, antihypertensive

Uses

A dihydropyridine calcium channel blocker. Antihypertensive.

Definition

ChEBI: Lercanidipine hydrochloride is a diarylmethane.

brand name

Cardiovasc (Recor dati, Italy); Carmen (Recordati, Italy); Corifeo (Recordati, Italy); Lercadip (Recordati, Italy); Lercan (Recordati, Italy); Lercapin (Recordati, Italy); Lercaton (Recordati, Italy); Lerkamen (Recordati, Italy); Lerzam (Recordati, Italy); Renovia (Recordati, Italy); Vasodip (Recordati, Italy); Zandip (Recordati, Italy); Zanicor (Recordati, Italy).

Biological Activity

L-type Ca 2+ channel blocker that displays higher vascular selectivity than Felodipine (4-(2,3-Dichlorophenyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylic acid ethyl methyl ester ). Causes peripheral vasodilation with only weak negative inotropic activity. Antihypertensive.

Biochem/physiol Actions

Lercanidipine hydrochloride is a L-type (Cav1.2b) vascular channel antagonist; L-type (Cav1.2a) cardiac channel agonist voltage-dependent and highly lipophylic compound, which exhibits a slower onset and longer duration of action than other calcium channel antagonists; an antihypertensive agent in patients with mild-to-moderate hypertension; more vasoselective than lacidipine and amlodipine.

Synthesis

The general procedure for the synthesis of 3-(1-((3,3-diphenylpropyl)(methyl)amino)-2-methylpropan-2-yl)5-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate hydrochloride from the compound (CAS:957215-03-1) is as follows: 10 mmol of oxalate salt (Example 4) was dissolved in 100 mL of dichloromethane and 20 mL of aqueous solution containing 20 mmol of potassium carbonate was added. The organic phase was separated and the aqueous phase was extracted with 2 x 10 mL of dichloromethane. The organic phase was combined and treated with 20 mL of 1N hydrochloric acid solution. The organic phase was separated and concentrated. The residue was dissolved in 2,000 mL of water and 2 mL of 1N hydrochloric acid and 5 mL of saturated aqueous sodium chloride were added to form I hydrochloride hemihydrate and the product was collected by filtration. Yield: 6.2 g (95%); Purity: 99.8% (HPLC); Melting point: 118-122 ° C. HPLC conditions: RP 16 column, 125×3 mm ID, 5 μm, Detection wavelength: 233 nm; Eluent composition: 0.01 mol Na2HPO4/MeOH/acetonitrile=25/65/10; Retention time: about 15 min.

Description

BCL10 Human Recombinant produced in E. coli is a single polypeptide chain containing 257 amino acids (1-233) and having a molecular mass of 28.8kDa (molecular weight on SDS-PAGE will appear higher).
BCL10 is fused to a 24 amino acid His-tag at N-terminus & purified by proprietary chromatographic techniques.

Source

Ecoli

Background

BCL10 holds a caspase recruitment domain (CARD), and is known as an inducer of apoptosis and as NF-kappaB activator. BCL10 cooperates with other CARD domain containing proteins such as CARD9, 10, 11 and 14, which operates as upstream regulators in NF-kappaB signaling. BCL10 is known to create a complex with MALT1, a protein encoded by another gene and is translocated in MALT lymphoma. MALT1 and BCL10 protein synergize the activation of NF-kappaB, and the deregulation of either of them facilitates the same pathogenetic process which leads to the malignancy.

References

[1] Patent: EP1860102, 2007, A1. Location in patent: Page/Page column 1; 8; 15

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