PNU 37883 hydrochloride

Vascular Kir6 (KATP) channel blocker CAS# 57568-80-6

PNU 37883 hydrochloride

Catalog No. BCC7262----Order now to get a substantial discount!

Product Name & Size Price Stock
PNU 37883 hydrochloride: 5mg $92 In Stock
PNU 37883 hydrochloride: 10mg Please Inquire In Stock
PNU 37883 hydrochloride: 20mg Please Inquire Please Inquire
PNU 37883 hydrochloride: 50mg Please Inquire Please Inquire
PNU 37883 hydrochloride: 100mg Please Inquire Please Inquire
PNU 37883 hydrochloride: 200mg Please Inquire Please Inquire
PNU 37883 hydrochloride: 500mg Please Inquire Please Inquire
PNU 37883 hydrochloride: 1000mg Please Inquire Please Inquire
Related Products

Quality Control of PNU 37883 hydrochloride

Number of papers citing our products

Chemical structure

PNU 37883 hydrochloride

3D structure

Chemical Properties of PNU 37883 hydrochloride

Cas No. 57568-80-6 SDF Download SDF
PubChem ID 64392 Appearance Powder
Formula C21H36ClN3O M.Wt 381.98
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 25 mM in DMSO and to 100 mM in ethanol
Chemical Name N-(1-adamantyl)-N'-cyclohexylmorpholine-4-carboximidamide;hydrochloride
SMILES C1CCC(CC1)N=C(NC23CC4CC(C2)CC(C4)C3)N5CCOCC5.Cl
Standard InChIKey FZALCKUJYZCDOX-UHFFFAOYSA-N
Standard InChI InChI=1S/C21H35N3O.ClH/c1-2-4-19(5-3-1)22-20(24-6-8-25-9-7-24)23-21-13-16-10-17(14-21)12-18(11-16)15-21;/h16-19H,1-15H2,(H,22,23);1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of PNU 37883 hydrochloride

DescriptionNovel antagonist selective for the vascular form of Kir6 (KATP) channel; inhibits Kir6 currents in isolated mesenteric artery smooth muscle cells (Kd = 65 nM) but not in cardiac or skeletal myocytes. Inhibits blood vessel relaxation and hypotension induced by pinacidil in vivo. Displays weak diuretic effects.

PNU 37883 hydrochloride Dilution Calculator

Concentration (start)
x
Volume (start)
=
Concentration (final)
x
Volume (final)
 
 
 
C1
V1
C2
V2

calculate

PNU 37883 hydrochloride Molarity Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
g/mol

calculate

Preparing Stock Solutions of PNU 37883 hydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.6179 mL 13.0897 mL 26.1794 mL 52.3588 mL 65.4485 mL
5 mM 0.5236 mL 2.6179 mL 5.2359 mL 10.4718 mL 13.0897 mL
10 mM 0.2618 mL 1.309 mL 2.6179 mL 5.2359 mL 6.5448 mL
50 mM 0.0524 mL 0.2618 mL 0.5236 mL 1.0472 mL 1.309 mL
100 mM 0.0262 mL 0.1309 mL 0.2618 mL 0.5236 mL 0.6545 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Organizitions Citing Our Products recently

 
 
 

Calcutta University

University of Minnesota

University of Maryland School of Medicine

University of Illinois at Chicago

The Ohio State University

University of Zurich

Harvard University

Colorado State University

Auburn University

Yale University

Worcester Polytechnic Institute

Washington State University

Stanford University

University of Leipzig

Universidade da Beira Interior

The Institute of Cancer Research

Heidelberg University

University of Amsterdam

University of Auckland
TsingHua University
TsingHua University
The University of Michigan
The University of Michigan
Miami University
Miami University
DRURY University
DRURY University
Jilin University
Jilin University
Fudan University
Fudan University
Wuhan University
Wuhan University
Sun Yat-sen University
Sun Yat-sen University
Universite de Paris
Universite de Paris
Deemed University
Deemed University
Auckland University
Auckland University
The University of Tokyo
The University of Tokyo
Korea University
Korea University
Featured Products
New Products
 

References on PNU 37883 hydrochloride

Molecular analysis of the subtype-selective inhibition of cloned KATP channels by PNU-37883A.[Pubmed:14757705]

Br J Pharmacol. 2004 Mar;141(5):867-73.

1. In this study, we have used Kir6.1/Kir6.2 chimeric proteins and current recordings to investigate the molecular basis of PNU-37883A inhibition of cloned K(ATP) channels. 2. Rat Kir6.1, Kir6.2 and Kir6.1/Kir6.2 chimeras were co-expressed with either SUR2B or SUR1, following RNA injection into Xenopus oocytes, and fractional inhibition of K(ATP) currents by 10 microm PNU-37883A reported. 3. Channels containing Kir6.1/SUR2B were more sensitive to inhibition by PNU-37883A than those containing Kir6.2/SUR2B (mean fractional inhibition: 0.70, cf. 0.07). 4. On expression with SUR2B, a chimeric channel with the Kir6.1 pore and the Kir6.2 amino- and carboxy-terminal domains was PNU-37883A insensitive (0.06). A chimera with the Kir6.1 carboxy-terminus and Kir6.2 amino-terminus and pore was inhibited (0.48). These results, and those obtained with other chimeras, suggest that the C-terminus is an important determinant of PNU-37883A inhibition of Kir6.1. Similar results were seen when constructs were co-expressed with SUR1. Further chimeric constructs localised PNU-37883A sensitivity to an 81 amino-acid residue section in the Kir6.1 carboxy-terminus. 5. Our data show that structural differences between Kir6.1 and Kir6.2 are important in determining sensitivity to PNU-37883A. This compound may prove useful in probing the structural and functional differences between the two channel subtypes.

Different molecular sites of action for the KATP channel inhibitors, PNU-99963 and PNU-37883A.[Pubmed:12746230]

Br J Pharmacol. 2003 May;139(1):122-8.

1. We investigated the mechanism of action of two novel nonsulphonylurea ATP-sensitive potassium channel (K(ATP)) inhibitors, PNU-99963 and PNU-37883A, on four types of cloned K(ATP) channels. 2. Whole-cell currents were recorded in a symmetrical potassium (140 mM) gradient in HEK-293 cells stably expressing Kir6.2/SUR1, Kir6.2/SUR2A, Kir6.2/SUR2B or Kir6.1/SUR2B. 3. PNU-99963 potently inhibited the four K(ATP) channel clones. The concentration at which half-maximum current was inhibited (IC(50)) was 66, 41, 43 and 11 nM for Kir6.2/SUR1, Kir6.2/SUR2A, Kir6.2/SUR2B and Kir6.1/SUR2B, respectively. In contrast, PNU-99963 up to a concentration of 3 microM had no significant effect on current generated in HEK-293 cells by transiently expressing Kir6.2Delta26, a C-terminal truncated pore-forming subunit of Kir6.2. 4. PNU-37883A inhibited four types of K(ATP) channels, but to different extents. Inhibition of the putative smooth muscle K(ATP) channel types, Kir6.2/SUR2B (IC(50); 15 microM) and Kir6.1/SUR2B (IC(50); 6 microM), was significantly greater than inhibition of either the pancreatic beta cell or cardiac K(ATP) channel clones. Moreover, PNU-37883A significantly inhibited currents generated by expressing Kir6.2Delta26 alone, with an IC(50) of 5 microM, which was significantly increased to 38 microM when Kir6.2Delta26 was expressed with SUR2B. 5. In conclusion, two structurally different nonsulphonylurea compounds, PNU-99963 and PNU-37883A, inhibit K(ATP) channels via different mechanisms, namely through the sulphonylurea receptor (SUR) and the pore-forming subunits, respectively, although SUR2B reduced the inhibitory effect of PNU-37883A. While PNU-99963 potently inhibits all the four cloned K(ATP) channels, PNU-37883A has a degree of selectivity towards both smooth muscle K(ATP) channels, but could not discriminate between them.

K-ATP-blocking diuretic PNU-37883A reduces plasma renin activity in dogs.[Pubmed:9641474]

J Cardiovasc Pharmacol. 1998 Jun;31(6):894-903.

We determined the effects of the K-adenosine triphosphate (ATP)-blocking diuretic PNU-37883A on plasma renin activity (PRA) in conscious and anesthetized dogs. In conscious dogs, oral PNU-37883A (6-60 mg/kg) was less potent than hydrochlorothiazide (0.15-1.5 mg/kg) and furosemide (FURO; 0.3-3.0 mg/kg) but exhibited high natriuretic efficacy with little kaliuresis. Unlike the standard diuretics, PNU-37883A reduced PRA by 46-76%, and its high dose minimally affected 24-h urinary aldosterone excretion. PNU-37883A, 1 mg/kg i.v., also blunted the hyperreninemia induced by 1 mg/kg i.v. FURO. In cannulated dogs, 10 mg/kg i.v. PNU-37883A maximally increased fractional Na+ clearance 140% and reduced PRA 76%, but these effects were accompanied by a mean 13 mm Hg pressor effect. In anesthetized dogs, renal artery-infused PNU-37883A (3 mg/kg/h i.r.a.) increased Na+ excretion and reduced renal venous PRA independent of hemodynamics, whereas half this dosage selectively reduced renal venous PRA and renin release, independent of hemodynamics and natriuresis. These data demonstrate that the K-ATP blocker diuretic PNU-37883A reduces PRA in dogs after oral, i.v., and i.r.a. administration and could be a useful pharmacologic agent for exploring the role of K-ATP channels in regulating renin release.

Keywords:

PNU 37883 hydrochloride,57568-80-6,Natural Products,Potassium Channel, buy PNU 37883 hydrochloride , PNU 37883 hydrochloride supplier , purchase PNU 37883 hydrochloride , PNU 37883 hydrochloride cost , PNU 37883 hydrochloride manufacturer , order PNU 37883 hydrochloride , high purity PNU 37883 hydrochloride

Online Inquiry for:

      Fill out the information below

      • Size:Qty: - +

      * Required Fields

                                      Result: