KRN4884 is a K+ channel opener. In the presence of intracellular ATP (1 mM), KRN4884 (0.1-3 μM) activates KATP channels (EC50=0.55 μM) in a concentration-dependent fashion.

Physicochemical Properties

Molecular Formula	C15H14CLN5
Molecular Weight	299.75816
Exact Mass	299.093
CAS #	152802-84-1
PubChem CID	9817785
Appearance	Typically exists as solid at room temperature
LogP	2.2
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	5
Heavy Atom Count	21
Complexity	402
Defined Atom Stereocenter Count	0
InChi Key	NDGLGOGSZCDCPI-UHFFFAOYSA-N
InChi Code	InChI=1S/C15H14ClN5/c16-14-4-2-1-3-11(14)5-6-20-15(21-10-17)12-7-13(18)9-19-8-12/h1-4,7-9H,5-6,18H2,(H,20,21)
Chemical Name	5-amino-N'-[2-(2-chlorophenyl)ethyl]-N-cyanopyridine-3-carboximidamide
Synonyms	KRN4884; KRN 4884; KRN-4884
HS Tariff Code	2934.99.9001
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)

Biological Activity

ln Vitro	Without altering the slope, KRN4884 (0.3 μM) causes a rightward shift and slight upward shift in the concentration-response relationship for ATP-induced blockage of KATP channels. KRN4884 (1 and 3 μM) partially recovers the activity of the KATP channel following channel degradation caused by Ca2+ ions or spontaneously. Additionally, uridine 5'-diphosphate (3 mM) increased the effects of KRN4884. In addition to decreasing the channel's ATP sensitivity, KRN4884 directly stimulates the opening of cardiac KATP channels. The concentration-dependent rise in outward current of KRN4884 (0.3 and 3 μM) is comparable to that of KATP channels in an ATP-free solution, with a single current amplitude [1].
ln Vivo	Sprague-Dawley rats were used to examine the impact of KRN4884, a new picolidine-type KATP channel opener, on blood triglyceride levels. Serum triglyceride levels were significantly lowered after 10 days of oral KRN4884 (3 mg/kg), which was equivalent to clofibrate (160 mg/kg). Low-density lipoprotein and chylomicron triglyceride levels decreased in tandem with the lowering of serum triglyceride levels caused by KRN4884 and clofibrate. Treatment with KRN4884 raised levels of free fatty acids but had no effect on serum concentrations of phospholipids or total cholesterol. Rats given KRN4884 showed elevated levels of lipoprotein lipase (LPL) in their skeletal muscle and adipose tissue [2].
References	[1]. Shinbo A, et al. Activation of cardiac ATP-sensitive K+ channels by KRN4884, a novel K+ channel opener. J Pharmacol Exp Ther. 1997 Nov;283(2):770-7. [2]. Yokoyama T, et al. Effects of KRN4884, a novel pyridinecarboxamidine type KATP channel opener, on serum triglyceride levels in rats. Br J Pharmacol. 1997 Apr;120(8):1471-6

Solubility Data

Solubility (In Vitro)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	3.3360 mL	16.6800 mL	33.3600 mL
	5 mM	0.6672 mL	3.3360 mL	6.6720 mL
	10 mM	0.3336 mL	1.6680 mL	3.3360 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.