Size | Price | Stock | Qty |
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5mg |
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10mg |
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50mg |
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Other Sizes |
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ln Vitro |
In a glyburide-sensitive way, levcromakalim ((-)-Cromakalim) totally blocks autocontractions. Autoconstriction is inhibited by LevCromakalim (5 μM) and then recovered by glibenclamide. Autocontraction was suppressed by levcromakalim (1, 5 and 10 μM) to 34±21.1%, 20.1±20.0% and 0% of the control group (n = 5; P<0.05). Levcromakalim (20 and 100 μM) also inhibited the isometric contractions induced by oxytocin (OXT) (10 nM) Staged shrinkage to 34±21.4% and 14±12.6% of control (n=6 and 4, respectively; P<0.05). Glibenclamide restored the isometric contractions induced by LevCromakalim (5 μM) to 84±1.5% of control (n=5). LevCromakalim (100 μM) auto-isometric contraction transcription was reversed by glibudide to 79±3.5% of control (n=4; P<0.05). Additionally, glibenclamide-sensitive cromakalim reduced OXT's tetanic contraction [P < 0.05]. 2]. LevCromakalim (Cromakalim) is a specialized channel opener that is required for KATP channel operation. LevCromakalim causes stress contractions in both elderly and young persons' mesenteric arteries (MAs); age has no effect on the relaxing of the MAs. Nevertheless, an elderly MA's reaction (P<0.05) to a high-salt (HS) diet is dramatically decreased [3].
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References |
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Additional Infomation |
Levcromakalim is a 1-benzopyran.
A potassium-channel opening vasodilator that has been investigated in the management of hypertension. It has also been tried in patients with asthma. (Martindale, The Extra Pharmacopoeia, 30th ed, p352) |
Molecular Formula |
C16H18N2O3
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Molecular Weight |
286.331
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Exact Mass |
286.132
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CAS # |
94535-50-9
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PubChem CID |
93504
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Appearance |
White to off-white solid powder
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Density |
1.31g/cm3
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Boiling Point |
482.3ºC at 760mmHg
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Flash Point |
245.5ºC
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LogP |
1.691
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Hydrogen Bond Donor Count |
1
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Hydrogen Bond Acceptor Count |
4
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Rotatable Bond Count |
1
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Heavy Atom Count |
21
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Complexity |
481
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Defined Atom Stereocenter Count |
2
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SMILES |
CC1([C@H]([C@@H](C2=C(O1)C=CC(=C2)C#N)N3CCCC3=O)O)C
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InChi Key |
TVZCRIROJQEVOT-CABCVRRESA-N
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InChi Code |
InChI=1S/C16H18N2O3/c1-16(2)15(20)14(18-7-3-4-13(18)19)11-8-10(9-17)5-6-12(11)21-16/h5-6,8,14-15,20H,3-4,7H2,1-2H3/t14-,15+/m1/s1
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Chemical Name |
(3S,4R)-3-hydroxy-2,2-dimethyl-4-(2-oxopyrrolidin-1-yl)-3,4-dihydrochromene-6-carbonitrile
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Synonyms |
BRL 38227; Lemakalim; Levcromakalim
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~174.62 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.4925 mL | 17.4624 mL | 34.9247 mL | |
5 mM | 0.6985 mL | 3.4925 mL | 6.9849 mL | |
10 mM | 0.3492 mL | 1.7462 mL | 3.4925 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.