5.30655

Mitochondrial GPDH Inhibitor, iGP-1

• Synonyme(s) : Mitochondrial GPDH Inhibitor, iGP-1, N-(4-(1H-Benzoimidazol-2-yl)-phenyl)-succinamic acid, Mitochondrial sn-Glycerol-3-Phosphate Dehydrogenase Inhibitor, mGPDH Inhibitor, inhibitor of m GPDH 1, iGP1, N-(4-(1H-Benzoimidazol-2-yl)-phenyl)-succinamic acid, Mitochondrial sn-Glycerol-3-Phosphate Dehydrogenase Inhibitor, mGPDH Inhibitor, inhibitor of mGPDH 1, iGP1
• Formule empirique (notation de Hill) : C₁₇H₁₅N₃O₃
• CAS Number: 27031-00-1
• Poids moléculaire : 309.32
• Numéro MDL: MFCD00395378
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Essai: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: solid
• Puissance: 6.3 μM IC₅₀
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: beige
• Solubilité: DMSO: 50 mg/mL
• Température de stockage: 2-8°C
• Chaîne SMILES: [nH]1c2c(nc1c3ccc(cc3)NC(=O)CCC(=O)O)cccc2
• Clé InChI: ARVPDCQNTCJVSU-UHFFFAOYSA-N

Description

Description générale

A cell-permeable thiadiazolyl-butyl-pyridazinyl compound that displays increased fluorescence with acidified pH (by 8-fold from pH 7.0 to 1.5; Ex 342 nm & Em 378 nm) and selectively inhibits mitochondrial sn-glycerol 3-phosphate (GP) dehydrogenase (mGPDH) activity (IC₅₀ = 6.3 µM by DCPIP assay using rat skeletal muscle mitochondria preparation with 1 µ Ca²⁺), but not cytosolic GPDH (up to 80 µM using rabbit cGPDH), by targeting free mGPDH in a GP-competitive manner (K_icK_iu2-dependent complex I activity and little potency toward unbiquinol/QH₂-dependent complex III activity, nor FMN-dependent complex I or II activity. Under conditions where Lactate dehydrogenase-mediated NAD⁺ generation is blocked by Oxamate in murine cortical synaptosome preparations, a small but significant dependence on mGPDH-mediated GP shuttle for NAD⁺ generation to support the high glycolytic demand for pyruvate generation from glucose (15 mM) is reported, as evidenced by a more pronounced mitochondrial respiration inhibition in the presence of FCCP and Oligomycin (4 µg/mL; Cat. No. 495455 ) with the combined treatment of 0.5 mM aminooxyacetate (AOA) and 100 µM iGP-1 than with AOA alone.

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
mGPDH

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Autres remarques

Orr, A.L., et al. 2014. PLoS One9, e89938.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable