[CAS NO. 320386-54-7] SKF-34288hydrochloride
PRODUCTS SPECIFICATIONS [320386-54-7]
DESCRIPTION [320386-54-7]
Overview
| MDL | MFCD01320417 |
|---|---|
| Molecular Weight | 191.64 |
| Molecular Formula | C6H6ClNO2S |
| SMILES | O=C(C1=NC=CC=C1S)O.[H]Cl |
Summary
SKF-34288 (3-Mercaptopicolinic acid) hydrochloride is an orally active phosphoenolpyruvate carboxykinase ( PEPCK ) inhibitor ( K i : 2-9 μM). SKF-34288 hydrochloride is a potent hypoglycemic agent by inhibiting glucose synthesis. SKF-34288 hydrochloride also inhibits Asn metabolism and increases amino acids and amides [1] [2] .
IC50 & Target
Ki: 2-9 μM (PEPCK) [1]
In Vitro
SKF-34288 hydrochloride (0.01-1 mM, 48 h) inhibits C2C12 cell proliferation
[4]
.
SKF-34288 hydrochloride (0.25-1 mM, 0-5 day) induces myogenic differentiation of C2C12 cells
[4]
.
SKF-34288 hydrochloride (0.25 or 1 mM) reduces mRNA expression of Pck2 and genes associated with serine biosynthesis
[4]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [4]
| Cell Line: | C2C12 cell |
| Concentration: | 0, 0.01, 0.1, 0.25, 0.5, 1 mM |
| Incubation Time: | 48 h |
| Result: | Dose-dependently inhibited C2C12 cell proliferation. |
In Vivo
SKF-34288 hydrochloride (37.5-150mg/kg, p.o.) reduces blood glucose in starved rats
[6]
.
SKF-34288 hydrochloride (25 mg/kg, s.c.) neutralizes Salbutamol- mediated hyperglycaemia in rabbits
[3]
.
SKF-34288 hydrochloride (30 and 300 mg/kg, i.p.) reduces Pyruvate-induced blood glucose level in rats
[5]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Starved rats [6] |
| Dosage: | 37.5, 75 and 150mg/kg |
| Administration: | Oral administration (p.o.) |
| Result: | Showed dose-dependent magnitude and duration of the hypoglycaemic effect. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 5 mg/mL ( 26.09 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 5.2181 mL | 26.0906 mL | 52.1812 mL |
| 5 mM | 1.0436 mL | 5.2181 mL | 10.4362 mL |
| 10 mM | 0.5218 mL | 2.6091 mL | 5.2181 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 3.33 mg/mL (17.38 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
References
- [1] Balan MD, et al. Inhibition and Allosteric Regulation of Monomeric Phosphoenolpyruvate Carboxykinase by 3-Mercaptopicolinic Acid. Biochemistry. 2015 Sep 29;54(38):5878-87.
- [2] Bailey KJ, et al. Nitrogen recycling from the xylem in rice leaves: dependence upon metabolism and associated changes in xylem hydraulics. J Exp Bot. 2016 Apr;67(9):2901-11.
- [3] Reverte M, et al. Changes in plasma glucose and lactate evoked by alpha and beta 2-adrenoceptor stimulation in conscious fasted rabbits. Fundam Clin Pharmacol. 1991;5(8):663-76.
- [4] Brearley MC, et al. The phosphoenolpyruvate carboxykinase (PEPCK) inhibitor, 3-mercaptopicolinic acid (3-MPA), induces myogenic differentiation in C2C12 cells. Sci Rep. 2020 Dec 17;10(1):22177.
- [5] Ohmori H, et al. The Production of a Rat Model That Inhibits Phosphoenolpyruvate Carboxykinase (PEPCK), a Rate-Limiting Enzyme of Hepatic Gluconeogenesis. Adv Exp Med Biol. 2019;1155:113-118.
- [6] DiTullio NW, et al. 3-mercaptopicolinic acid, an inhibitor of gluconeogenesis. Biochem J. 1974 Mar;138(3):387-94.