Name: L-651,582
Brand: Alomone Labs
SKU: L-110

Cat #: L-110

Alternative Name Carboxyamidotriazole

Lyophilized Powder yes

Bioassay Tested

Source Synthetic

MW: 424.7

Purity: >99%

Effective concentration 0.5-200 μM.

Structure

Chemical name 5-Amino-1-[[3,5-dichloro-4-(4-chlorobenzoyl)phenyl]methyl]-1H-1,2,3-triazole-4-carboxamide.

Molecular formula C₁₇H₁₂Cl₃N₅O₂.

CAS No.: 99519-84-3

Activity L-651,582 inhibits Ca_V channels as well as receptor activated Ca²⁺ signals in guinea pig atrial cells¹, thus it is an L-type, voltage-gated Ca²⁺ channel blocker with additional antiproliferative activities².

References-Activity

Hupe, D.J. et al. (1991) J. Biol. Chem. 266, 10136.
Guo, L. et al. (1991) Eur. J. Pharmacol. 538, 15.

Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Solubility DMSO. Centrifuge all product preparations before use (10000 x g 5 min).

Storage of solutions Up to four weeks at 4°C or three months at -20°C.

Our bioassay

Alomone Labs L-651,582 blocks L-type Ca²⁺ currents in Xenopus oocytes.
A. Time course of L-type channel (Ca_V1.2+α₂δ₁+β_1a) activity before and during applications of 1, 10 and 100 μM L-651,582 (#L-110) and upon wash. Holding potential was -100 mV and currents were elicited every 10 seconds by 100 ms steps to 0 mV. Periods of compound application are indicated by symbols in the inset. B. Example of superimposed current traces before and during application of 1, 10 and 100 μM L-651,582 (taken from the experiment described in A).

References - Scientific background

Schramm, M. et al. (1988) Calcium in drug actions (Baker, P. F., ed), 90-113.
Narahashi, T. et al. (1988) Calcium in drug actions (Baker, P. F., ed), 255-174.
Kohn, E.C. et al. (1990) J. Nat. Cancer Int. 82, 54.
Felder, C.C. et al.(1991) J. Pharm. Exp. Ther. 257, 967.
Hupe, D.J. et al. (1991) J. Biol. Chem. 266, 10136.
Yang, J.L. et al. (2008) Int. J. Cancer 123, 258.

Scientific background

Two subtypes of voltage-gated Ca²⁺channels (VGCC, Ca_V) are found in most non-excitable cells, the T-type (Ca_V3) and the L-Type (Ca_V1) Ca²⁺channels^1-2.

L-651,582 is an anti-proliferative, anti-angiogenic, anti-metastatic and anti-parasitic agent^3-5, which is also selective towards numerous mismatch repair-deficient tumor cell lines in vitro.⁶ It is a voltage-gated L-type Ca²⁺channel blocker with an IC₅₀ of 0.5 µg/ml⁵ . Patch clamp measurements of current through L- and T-type channels in guinea pig atrial cells also indicate that L-651,582 is a Ca²⁺antagonist⁵. Block of L-type Ca²⁺channels is voltage-dependent and the apparent dissociation constant for the high affinity state is 0.2 µg/ml. The IC₅₀ for block of T-type Ca²⁺channels is 1.4 µg/ml⁵.

Target L-type Ca²⁺ channels

Lyophilized Powder

Last update: 02/01/2022

L-651,582 (#L-110) is a highly pure, synthetic, and biologically active compound.

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L-651,582

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