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Cat. No.: HY-N21896

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Correolide

Correolide is a pentacyclic nortriterpene isolated from Spachea correa. Correolide blocks Kv1 family voltage-gated potassium channels (Kv1.3 K_d = 90 nM) and acts on the inner pore between the selectivity filter and the activation gate, thereby inhibiting T cell proliferation and modulating vascular tone. Correolide can be used in research on delayed-type hypersensitivity and autoimmune diseases.

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CAS No.: 190017-00-6
Formule: C₄₀H₅₂O₁₆
Masse moléculaire:788.83

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Please store the product under the recommended conditions in the Certificate of Analysis.

Correolide Chemical Structure

CAS No.: 190017-00-6

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

^[2]

Kv1.3

90 nM (Kd)

In Vitro

OthersAdaptive ImmunityLocal Vascular Regulation

Others

Correolide (10-100 μmol/L) inhibits heterologously expressed human PASMC Kv1.5 channels in CHO cells^[1].
Correolide (90 nM) blocks Kv1.3 channels with a K_d of 90 nM^[2].
Correolide (1 μmol/L) inhibits KDR currents in rat mesenteric artery smooth muscle cells, and its effect on grade 2 vessels is stronger than on grade 4 vessels^[8].
Correolide (1 μM; 60 to 90 minutes) increases the amplitude of spontaneous contractions in human detrusor smooth muscle strips without affecting contraction frequency or baseline tension^[10].

Adaptive Immunity

Correolide inhibits mitogen-induced T cell proliferation^[2].

Local Vascular Regulation

Correolide (50 nM)-sensitive Kv1 family current density was greater in RCA myocytes (22.0 pA/pF) than in LCA myocytes (12.6 pA/pF), indicating that the difference in Kv current between LCA and RCA cells is attributable to the Kv1 current family^[6].
Correolide (1-10 μM)-sensitive K_V1 subunits constitute the major portion of the delayed rectifier K⁺ current in porcine coronary artery smooth muscle cells^[7].
Correolide (1 µM)-sensitive K_Vα1 channels constitute the major portion of voltage-dependent K⁺ current in rabbit cerebral arteriolar smooth muscle cells^[9].
Correolide (1 µM) induces vasoconstriction in endothelin-1-preconstricted rabbit cerebral small arteries, supporting the functional role of K_Vα1 channels in counteracting vasoconstriction^[9].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Regulation of Cardiac Pump FunctionCardiovascular RegulationOthers

Regulation of Cardiac Pump Function

Cardiovascular Regulation

Correolide (0.3-3 μM; intracoronary infusion)-sensitive K_V1 channels maintain baseline coronary vascular tone, reduce coronary blood flow by approximately 25% at rest, and contribute to metabolic and ischemic coronary vasodilation in pigs^[7].

Others

Correolide (1 μmol/L; bath application) inhibits Kv1-containing K_DR channels and enhances myogenic reactivity in rat mesenteric arteries, indicating that these channels play a key role in the myogenic control of arterial diameter^[8].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Domestic swine (adult male, n=10)^[7]
Dosage:

0.3, 1, 3 μM; 3 μM
Administration:

Intracoronary infusion
Result:

Decreased coronary blood flow by approximately 25% (from ~1.0 to 0.72 mL/min/g with 3 μM).
Reduced baseline coronary blood flow by approximately 25% (from 1.06 to 0.79 mL/min/g).
Decreased the overall volume of repayment after 15-second occlusion by approximately 35% (from 1.86 to 1.21 mL/g).

Animal Model:

Sprague-Dawley (Male)^[8]
Dosage:

1 μmol/L
Administration:

bath application
Result:

Maintained a stable diameter in 2nd order conduit RMAs with increasing transmural pressure between 60 to 120 mm Hg, preventing passive dilation.
Enhanced the myogenic response in 4th order resistance RMAs, causing a greater reduction in arterial diameter compared with control conditions.
Induced spontaneous oscillations in diameter in 2 of 6 4th order vessels.

Related Protocols :

Chemical Information

CAS No. 190017-00-6
Masse moléculaire 788.83
Formule C₄₀H₅₂O₁₆
SMILES

COC([C@]12[C@]3([C@]([C@@]4([H])[C@]([C@@H]([C@@H]3OC(C)=O)OC(C)=O)([C@]5([H])[C@@](CC4)([C@@]6([H])[C@@]([C@H]([C@H]5OC(C)=O)OC(C)=O)(COC(C=C6)=O)C(C)OC(C)=O)C)C)(CC([C@@]1([H])O2)=C)O)C)=O
Structure Classification
- Terpenoids
- Pentacyclic Triterpenoids
Initial Source
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Archer SL, et al. Preferential expression and function of voltage-gated, O2-sensitive K+ channels in resistance pulmonary arteries explains regional heterogeneity in hypoxic pulmonary vasoconstriction: ionic diversity in smooth muscle cells. Circulation research. 2004 Aug 6;95(3):308-18.

[2]. Chandy KG, et al. K+ channels as targets for specific immunomodulation. Trends in pharmacological sciences. 2004 May;25(5):280-9.

[3]. Baell JB. Potassium channel blockers as immunosuppressants. Expert Opinion on Therapeutic Patents. 2005 Sep 1;15(9):1209-20.

[4]. Wulff H, et al. K+ channel modulators for the treatment of neurological disorders and autoimmune diseases. Chemical reviews. 2008 May;108(5):1744.

[5]. Beeton C, et al. Targeting effector memory T cells with a selective peptide inhibitor of Kv1.3 channels for therapy of autoimmune diseases. Molecular pharmacology. 2005 Apr;67(4):1369-81.

[6]. Gautier M, et al. Heterogeneous Kv1 function and expression in coronary myocytes from right and left ventricles in rats. American journal of physiology. Heart and circulatory physiology. 2007 Jan;292(1):H475-82.

[7]. Goodwill AG, et al. Critical contribution of KV1 channels to the regulation of coronary blood flow. Basic research in cardiology. 2016 Sep;111(5):56.

[8]. Plane F, et al. Heteromultimeric Kv1 channels contribute to myogenic control of arterial diameter. Circulation research. 2005 Feb 04;96(2):216-24.

[9]. Cheong A, et al. Expression and function of native potassium channel [K(V)alpha1] subunits in terminal arterioles of rabbit. J Physiol. 2001 Aug 1;534(Pt 3):691-700.

[10]. Davies AM, et al. Potassium channel KV alpha1 subunit expression and function in human detrusor muscle. J Urol. 2002 Apr;167(4):1881-6.

Calculators

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Calculateur de dilution

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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