MW 494 Da, Purity >99%. Selective blocker of ATP-sensitive (KIR6.x) inward rectifier K+ channels. Achieve your results faster with highly validated, pure and trusted compounds.
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- Brain : a journal of neurology 145:2332-23462022AMPK-mediated potentiation of GABAergic signalling drives hypoglycaemia-provoked spike-wave seizures.Applications:Unspecified applicationReactive species:Unspecified reactive speciesKathryn A Salvati,Matthew L Ritger,Pasha A Davoudian,Finnegan O'Dell,Daniel R Wyskiel,George M P R Souza,Adam C Lu,Edward Perez-Reyes,Joshua C Drake,Zhen Yan,Mark P BeenhakkerPubMed 35134125
- PloS one 14:e02159522019Glibenclamide, a Sur1-Trpm4 antagonist, does not improve outcome after collagenase-induced intracerebral hemorrhage.Applications:Unspecified applicationReactive species:Unspecified reactive speciesCassandra M Wilkinson et. al.PubMed 31042750
- Frontiers in pharmacology 7:452016Ion Fluxes through KCa2 (SK) and Cav1 (L-type) Channels Contribute to Chronoselectivity of Adenosine A1 Receptor-Mediated Actions in Spontaneously Beating Rat Atria.Applications:Unspecified applicationReactive species:Unspecified reactive speciesBruno Bragança et. al.PubMed 27014060
Key facts
- CAS number
- 10238-21-8
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 494 Da
- Molecular formula
- C23H28ClN3O5S
- PubChem identifier
- 3488
- Nature
- Synthetic
Target data
Alternative names
(R)-limonene 6-monooxygenase, (S)-limonene 6-monooxygenase, (S)-limonene 7-monooxygenase, 1,8-cineole 2-exo-monooxygenase, 2700049B16Rik, 3110031N04Rik, ABC member 16, MDR/TAP subfamily, ABC16, ABC36, ABC37, ABCB1, ABCBB_HUMAN, ABCC8_HUMAN, ABCC9_HUMAN, AI414027, AI449286, ATFB12, ATP binding cassette sub family B (MDR/TAP) member 11, ATP binding cassette sub family C (CFTR/MRP) member 8, ATP binding cassette transporter sub family C member 8 (1), ATP sensitive inward rectifier potassium channel 11, ATP-binding cassette sub-family B member 11, ATP-binding cassette sub-family C member 8, ATP-binding cassette sub-family C member 9, ATP-binding cassette transporter sub-family C member 9, ATP-binding cassette, sub-family C (CFTR/MRP), member 9, AU043990, AW743335, Albendazole monooxygenase, Albendazole sulfoxidase, BIR, BK channel, BK channel beta subunit, BK channel subunit beta-1, BK channel subunit beta-2, BK channel subunit beta-4, BKCA alpha, BKCA alpha subunit, BKTM, BKbeta, BKbeta1, BKbeta2, BKbeta4, BRIC2, BXR, Beta cell inward rectifier subunit, Bile salt export pump, Bsep, C10orf70, CANTU, CAPC, CDGSH iron sulfur domain 1, CDGSH iron-sulfur domain-containing protein 1, CISD1_HUMAN, CMD1O, CP2C9_HUMAN, CP33, CP34, CP3A4_HUMAN, CPC12, CPC8, CPC9, CPCJ, CYP2C, CYP2C10, CYP3, CYP3A, CYP3A3, CYP3A4, CYPIIC9, CYPIIIA3, CYPIIIA4, Calcium activated potassium channel beta 4 subunit, Calcium activated potassium channel subfamily M subunit beta 1, Calcium activated potassium channel subfamily M subunit beta 2, Calcium activated potassium channel subfamily M subunit beta 4, Calcium-activated potassium channel, Calcium-activated potassium channel subunit alpha-1, Calcium-activated potassium channel subunit beta, Calcium-activated potassium channel subunit beta-1, Calcium-activated potassium channel subunit beta-2, Calcium-activated potassium channel subunit beta-4, Charybdotoxin receptor subunit beta-1, Charybdotoxin receptor subunit beta-2, Charybdotoxin receptor subunit beta-4, Cytochrome P-450MP, Cytochrome P450 2C9, Cytochrome P450 3A3, Cytochrome P450 3A4, Cytochrome P450 HLp, Cytochrome P450 MP-4, Cytochrome P450 MP-8, Cytochrome P450 NF-25, Cytochrome P450 PB-1, Cytochrome P450 family 3 subfamily A polypeptide 4, Cytochrome P450 subfamily IIIA polypeptide 4, Cytochrome P450, family 2, subfamily C, polypeptide 9, Cytochrome P450-PCN1, Cytokeratin-associated protein in cancer, D10Ertd214e, Drosophila slowpoke like, FLJ36852, FLJ55736, Glucocorticoid inducible P450, HHF 2, HHF1, HI, HLP, HRINS, Hbeta1, Hbeta2, Hbeta3, Hbeta4, IKATP, IRK 11, Inward rectifier K(+) channel Kir6.2, Inwardly rectifying potassium channel KIR6.2, K(VCA)alpha, K(VCA)beta, K(VCA)beta-1, K(VCA)beta-2, K(VCA)beta-4, KCMA1_HUMAN, KCMB1_HUMAN, KCMB2_HUMAN, KCMB4_HUMAN, KCNJ11, KCNMA, KCNMA1, KCNMB 1, KCNMB 2, KCa1.1, Kir 6.2, LRC26_HUMAN, Large conductance Ca2+ activated K+ channel beta 1 subunit, Large conductance Ca2+ activated K+ channel beta2 subunit, Large conductance calcium activated potassium channel beta 2 subunit, Large conductance calcium dependent potassium ion channel beta 4 subunit, Leucine-rich repeat-containing protein 26, Liver-specific organic anion transporter 1, Lrrc26, MDS029, MGC126680, MGC133230, MGC14684, MGC149605, MGC22431, MGC45260, MGC57945, MGC88320, Maxi K channel, Maxi K channel beta subunit, Maxi K channel subunit beta-1, Maxi K channel subunit beta-2, Maxi K channel subunit beta-4, Maxi Potassium channel alpha, MaxiK, MaxiK channel beta 2 subunit, Microsomal monooxygenase, MitoNEET, NF 25, NR1I2_HUMAN, Nifedipine oxidase, Nuclear receptor subfamily 1 group I member 2, OAT1, OATP-2, OATP-C, ONR 1, OTTHUMP00000020135, OTTHUMP00000215173, OTTHUMP00000215174, OTTHUMP00000215175, OTTHUMP00000236796, OTTHUMP00000236797, OTTHUMP00000236798, OTTHUMP00000236799, Organic anion transporter 1, Orphan nuclear receptor PAR 1, Orphan nuclear receptor PXR, P450 III steroid inducible, P450 MP, P450 PB 1, P450 PCN1, P450, family III, P450C2C, P450C3, P450IIC19, P450IIC9, PAH transporter, PAHT, PAR, PAR q, PFIC 2, PGY4, PHHI, PRR, Para aminohippurate transporter, Potassium channel inwardly rectifing subfamily J member 11, Potassium channel, inwardly rectifying subfamily J member 11, Potassium inwardly rectifying channel J11, Potassium large conductance calcium activated channel subfamily M beta member 1, Potassium large conductance calcium activated channel subfamily M beta member 2, Potassium large conductance calcium activated channel subfamily M beta member 4, Pregnane X receptor, Quinine 3-monooxygenase, RGD1309529, ROAT1, Renal organic anion transporter 1, S-mephenytoin 4-hydroxylase, S22A6_HUMAN, SAKCA, SLC21A6, SLCO1B1, SLO, SO1B1_HUMAN, SUR1delta2, SUR2, SUR2A, SUR2B, SXR, Sister of P glycoprotein, Slo homolog, Slo-alpha, Slo-beta, Slo-beta-1, Slo-beta-2, Slo-beta-4, Slo1, Slowpoke homolog, Sodium-independent organic anion-transporting polypeptide 2, Solute carrier family 21 member 6, Solute carrier family 22 (organic anion transporter) member 6, Solute carrier family 22 member 6, Solute carrier organic anion transporter family member 1B1, Spgp, Steroid and xenobiotic receptor, Sulfonylurea receptor (hyperinsulinemia), Sulfonylurea receptor 1, Sulfonylurea receptor 2, Sulfonylurea-binding protein 2, TNDM 3, TNDM2, Taurochenodeoxycholate 6-alpha-hydroxylase, Xenobiotic monooxygenase, ZCD1, Zinc finger CDGSH type domain 1, bA350O14.10, cytochrome P-450 S-mephenytoin 4-hydroxylase, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 3, cytochrome P450, subfamily IIIA (niphedipine oxidase), polypeptide 4, cytokeratin-associated protein, flavoprotein-linked monooxygenase, hOAT1, hPAHT, hROAT1, hSlo, hslo beta, pregnane X nuclear receptor variant 2, progressive familial intrahepatic cholestasis 2, subfamily M subunit alpha-1, subfamily M subunit beta-1, subfamily M subunit beta-2, subfamily M subunit beta-4
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MW 494 Da, Purity >99%. Selective blocker of ATP-sensitive (KIR6.x) inward rectifier K+ channels. Achieve your results faster with highly validated, pure and trusted compounds.
Key facts
- CAS number
- 10238-21-8
- Purity
- > 99%
- Form
- Solid
- Molecular weight
- 494 Da
- Molecular formula
- C23H28ClN3O5S
- PubChem identifier
- 3488
- Nature
- Synthetic
- Solubility
Soluble in DMSO to 100 mM.
- Biochemical name
- Glyburide
- Biological description
Selective blocker of ATP-sensitive (KIR6.x) inward rectifier K+ channels.
- Canonical SMILES
- COC1=C(C=C(C=C1)Cl)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCCCC3
- InChI
- InChI=1S/C23H28ClN3O5S/c1-32-21-12-9-17(24)15-20(21)22(28)25-14-13-16-7-10-19(11-8-16)33(30,31)27-23(29)26-18-5-3-2-4-6-18/h7-12,15,18H,2-6,13-14H2,1H3,(H,25,28)(H2,26,27,29)
- InChIKey
- ZNNLBTZKUZBEKO-UHFFFAOYSA-N
- IUPAC name
- 5-chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxybenzamide
Storage
- Shipped at conditions
- Ambient - Can Ship with Ice
- Appropriate short-term storage conditions
- Ambient
- Appropriate long-term storage conditions
- Ambient
- Storage information
- The product can be stored for up to 12 months
Supplementary info
- This supplementary information is collated from multiple sources and compiled automatically.
- Activity summary
Cytochrome P450 3A4 (CYP3A4) is part of the cytochrome P450 superfamily and plays an important role in drug metabolism. It has a mass of around 57 kDa and is widely expressed in liver and intestinal tissues. Known also as CYP3A4 it is responsible for oxidizing small foreign organic molecules like toxins or drugs so the body can eliminate them. Other proteins like CYP2C9 CYP2C8 and CYP2C19 are related due to shared enzymatic functions. Additionally Maxi potassium channels including SLO KCNMB1 and KCNMB4 facilitate potassium ion flow across cell membranes influencing cell excitability and signaling. SUR1 Kir6.2 and related ABC transporters like ABCB11 (also named BSEP) are involved in ion channel regulation and bile acid transport respectively.
- Biological function summary
CYP3A4 detoxifies harmful compounds and metabolizes pharmaceuticals which is essential for the liver's chemical processing. It works in conjunction with other cytochrome P450 enzymes such as CYP2C9 and CYP2C8 and participates in a PXR-modulated gene expression complex that enhances drug clearance. Potassium channels such as SLO coordinate with regulatory subunits like KCNMB1 to modulate neuronal activity and muscle tone. These channels integrate with Kir6.2/BIR to form structures that control cellular response to metabolic change while bile transporters like ABCB11/BSEP regulate bile salt export critical for hepatic function.
- Pathways
CYP3A4 is central to the drug metabolism pathway significantly impacting the pharmacokinetic properties of many medications. It interacts with PXR which senses the presence of foreign substances to upregulate detoxifying enzymes. The Renin-Angiotensin-Aldosterone System (RAAS) and the potassium ion channels are related through the regulation of vascular tone and blood pressure by KCNMB1 and SUR1. These complexes interconnect to mediate hormonal balancing and renal filtration with ties to ABC transporters managing hepatic excretion of metabolic byproducts.
- Associated diseases and disorders
CYP3A4's involvement in drug metabolism has direct implications for drug-drug interactions and adverse drug reactions particularly affecting medications like glyburide and glibenclamide widely used antidiabetics. Alterations in CYP3A4 can lead to improper drug breakdown causing over-medication or incomplete therapeutic relief impacting conditions like hypertension when linked to potassium channel mutations. Relatedly KCNMB1 and SUR1 are associated with cardiovascular disorders due to their roles in blood pressure regulation and cardiac excitability. Mutations or dysregulation in these proteins and pathways can contribute to conditions such as hypertension and heart failure.
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2 product images
Chemical Structure - Glibenclamide (Glyburide), K+ channel blocker (ab120267)
2D chemical structure image of ab120267, Glibenclamide (Glyburide), K+ channel blocker
Functional Studies - Glibenclamide (Glyburide), K+ channel blocker (ab120267)
MEF1 cells were incubated at 37°C for 24h with vehicle control (0 μM) and 5 μM of glibenclamide (ab120267) in DMSO. Increased expression of JNK1+JNK2 (phospho T183 + Y185) (Anti-JNK1 + JNK2 (phospho T183 + Y185) antibody ab4821) correlates with an increase in glibenclamide concentration, as described in literature.
Whole cell lysates were prepared with RIPA buffer (containing protease inhibitors and sodium orthovanadate), 10 μg of each were loaded on the gel and the WB was run under reducing conditions. After transfer the membrane was blocked for an hour using 3% milk before being incubated with ab4821at 1/1000 dilution and ab85139 at 1 μg/ml overnight at 4°C. Antibody binding was detected using an anti-rabbit antibody conjugated to HRP (Goat Anti-Rabbit IgG H&L (HRP) ab97051) at 1/10000 dilution and visualised using ECL development solution.
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