Levcromakalim |
| رقم الكتالوجGC14923 |
Levcromakalim ((-) - Cromakalim) هو منشط قناة K + (KATP) حساس لـ ATP
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 94535-50-9
Sample solution is provided at 25 µL, 10mM.
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Levcromakalim ((-)-Cromakalim) is an ATP-sensitive K+ channel (KATP) activator.
Levcromakalim ((-)-Cromakalim) inhibits spontaneous contractions completely in a glibenclamide-sensitive manner. LevCromakalim (5 µM) inhibits spontaneous contractions, which are recovered by glibenclamide. Levcromakalim (1, 5 and 10 µM) inhibits phasic contractions to 34±21.1%, 20.1±20.0% and 0% of the control (n=5, respectively; P<0.05). Glibenclamide reverses the inhibition of spontaneous isometric contractions caused by LevCromakalim (5 µM) to 84±1.5% of the control (n=5; P<0.05). Levcromakalim (20 and 100 µM) also inhibits oxytocin (OXT) (10 nM)-induced phasic contractions to 34±21.4% and 14±12.6% of the control (n=6 and 4, respectively; P<0.05). Glibenclamide reverses the inhibition of spontaneous isometric contractions by LevCromakalim (100 µM) to 79±3.5% of the control (n=4; P<0.05). Tonic contraction by OXT is also suppressed by Cromakalim in a glibenclamide-sensitive manner[2].The function of the KATP channels is examined with the specific channel opener LevCromakalim (Cromakalim). LevCromakalim induces dose-dependent relaxation in both the young and old mesenteric artery (MAs); and there is no difference in relaxation with age. However, the relaxation is markedly reduced in response to the high-salt (HS) diet in the old MAs (P<0.05). Maximum dilations to Levcromakalim (10-4 M) are 97 ± 3% in the young MAs versus 98 ± 1% in the young salt arteries, while dilations are 99±0.7% in the old MAs when compared with 85 ± 5% in the old salt arteries (P<0.05)[3].
References:
[1]. Matsumoto T, et al. Tunicamycin-Induced Alterations in the Vasorelaxant Response in Organ-Cultured Superior Mesenteric Arteries of Rats. Biol Pharm Bull. 2016;39(9):1475-81.
[2]. Hong SH, et al. Regulation of myometrial contraction by ATP-sensitive potassium (KATP) channel via activation of SUR2B and Kir 6.2 in mouse. J Vet Med Sci. 2016 Aug 1;78(7):1153-9.
[3]. Whidden MA, Altered potassium ATP channel signaling in mesenteric arteries of old high salt-fed rats. J Exerc Nutrition Biochem. 2016 Jun;20(2):58-64.
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Kinase experiment: |
Levcromakalim (Cromakalim) is dissolved in 10% DMSO and Krebs solution[3].The endothelium-dependent relaxation is tested by performing concentration-response experiments with acetylcholine (ACh; 10 nM-10 μM). Typically, MAs are exposed to each dose of ACh for at least 6 minutes and maximal responses are determined. Function of the KATP channels are examined with 10 µM of glibenclamide (a selective KATP channel inhibitor) and Levcromakalim (Cromakalim) (10 nM to 100 μM), a KATP channel opener. The addition of glibenclamide to the arterial bath 10 minutes prior to ACh does not alter passive maximum internal diameters of any MAs in our groups.The vessel diameter changes are presented as percentages (%) of dilation of the preconstricted vessels, calculated[3]. |
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References: [1]. Matsumoto T, et al. Tunicamycin-Induced Alterations in the Vasorelaxant Response in Organ-Cultured Superior Mesenteric Arteries of Rats. Biol Pharm Bull. 2016;39(9):1475-81. |
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| Cas No. | 94535-50-9 | SDF | |
| Chemical Name | (3S,4R)-3-hydroxy-2,2-dimethyl-4-(2-oxopyrrolidin-1-yl)chroman-6-carbonitrile | ||
| Canonical SMILES | O[C@H](C(C)(C)OC1=C2C=C(C#N)C=C1)[C@@H]2N3CCCC3=O | ||
| Formula | C16H18N2O3 | M.Wt | 286.33 |
| الذوبان | DMSO : ≥ 50 mg/mL (174.62 mM) | Storage | Store at 2-8°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4925 mL | 17.4624 mL | 34.9247 mL |
| 5 mM | 698.5 μL | 3.4925 mL | 6.9849 mL |
| 10 mM | 349.2 μL | 1.7462 mL | 3.4925 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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