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| CROMAKALIM Basic information |
| Product Name: | CROMAKALIM | | Synonyms: | Cromakalim=([+/-]-trans-6-Cyano-3,4-dihydro-2,2-;(+/-)-CROMAKALIM;CROMAKALIM;TRANS-3,4-DIHYDRO-3-HYDROXY-2,2-DIMETHYL-4-(2-OXO-1-PYRROLIDINYL)-2H-1-BENZOPYRAN-6-CARBONITRILE;(+/-)-TRANS-6-CYANO-3,4-DIHYDRO-2,2-DIMETHYL-4-(2-OXOPYRROLIDIN-1-YL)-2H-1-BENZOPYRAN-3-OL;[+/-]-TRANS-6-CYANO-3,4-DIHYDRO-2,2-DIMETHYL-4-[2-OXOPYRROLIDIN-1-YL]-2H-1-BENZOPYRAN-3-OL;BRL-34915;rac-(3α*,4β*)-3,4-Dihydro-3-hydroxy-2,2-dimethyl-4-(2-oxopyrrolidine-1-yl)-2H-1-benzopyran-6-carbonitrile | | CAS: | 94470-67-4 | | MF: | C16H18N2O3 | | MW: | 286.33 | | EINECS: | | Product Categories: | All Inhibitors;Inhibitors | | Mol File: | 94470-67-4.mol |
| CROMAKALIM Chemical Properties |
| Melting point | 242-244°C | | storage temp. | 2-8°C | | solubility | Soluble in DMSO (up to 40 mg/ml) or in Ethanol (up to 10 mg/ml). | | form | solid | | color | Off-white | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
| CROMAKALIM Usage And Synthesis |
| Description | (±)-Cromakalim is a prototypical activator of the ATP-sensitive potassium channel, SUR2-Kir6, that displays anti-ischemic (EC25 = 8.9 μM) and cardioprotective (IC50 = 0.03 μM) effects in rat hearts. (±)-Cromakalim has also been shown to relax bladder smooth muscle in vitro. It has been used to investigate potassium channel biology and as a scaffold to develop increasingly selective K+ channel openers with clinical relevance. | | Chemical Properties | White Crystalline Solid | | Uses | Cromakalim causes vasodilation by activation of potassim channels
| | Uses | Cromakalim has been used:- as a potassium channel agonist to study its response to an acute increase in downstream pressure in rat lymphatic vessels.
- as a potassium channel opener to study its effects on the release of transmitters from adrenergic nerves in rat vas deferens.
- as a potassium channel activator to study its effects on the release of transmitters from purinergic and cholinergic nerves in the rat detrusor muscle.
| | Biological Activity | Prototypical K ATP channel opener. Relaxes rabbit isolated portal vein with an IC 50 value of 21 nM . Potent, orally active and hypotensive in vivo . | | Biochem/physiol Actions | Cromakalim is an activator of the potassium channel. It is involved in the relaxation of the vascular smooth muscles. Cromakalim exhibits anti-hypertensive activity. | | References | 1) Sanguinetti?et al. (1988),?BRL 34915 (cromakalim) activates ATP-sensitive K+ current in cardiac muscle; Proc. Natl. Acad. Sci. USA,?85?8360
2) Wu?et al.?(2011),?Reopening of ATP-sensitive potassium channels reduces neuropathic pain and regulates astroglial gap junctions in the rat spinal cord; Pain,?152?2605
3) Roy Chowdhury?et al.?(2017),?ATP sensitive potassium channel openers: A new class of ocular hypotensive agents; Exp. Eye Res.,?158?85
4) Cao?et al.?(2016),?Opening of the Adenosine Triphosphate-sensitive Potassium Channel Attenuates Morphine Tolerance by Inhibiting JNK and Astrocyte Activation in the Spinal Cord; Clin. J. Pain,?32?617 |
| CROMAKALIM Preparation Products And Raw materials |
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