Englerin A - ≥99% , CAS No.1094250-15-3

CAS: 1094250-15-3 Cat. No.: E646206 Summenformel: C₂₆H₃₄O₆ Molekulargewicht: 442.54 EG-Nummer: 805-134-0 PubChem CID: 46242512

QUALITÄT & REINHEIT ≥99%

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Übersicht

Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC 50 s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+ influx and Ca 2+ cell overload

In Vitro

Englerin A (0.15-2500 nM; 48 h) characteristic concentration-dependent suppresses cells growth of the A-498 cells treated with the control siRNA while has little effect on the growth of cells treated with TRPC4 siRNAs. Englerin A (0.001nM-10 μM; 48 h) inhibits cells viability in HEK293T cells overexpressing TRPC5. Englerin A (3 nM; 1-240 s) evokes sustained elevation of the intracellular Ca 2+ concentration within 1 min in HEK 293 cells over-expressing human TRPC4. Englerin A (0.1-1000 nM; 1-300 s) evokes intracellular Ca 2+ elevations in A498 cells as well with an EC 50 of 10 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Englerin A (5 mg/kg; i.p daily except Sunday) markedly inhibits tumor growth during the 2-week treatment period in mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Form:Solid

IC50& Target:hTRPC4 11.2 nM (EC 50 ) hTRPC5 7.6 nM (EC 50 )

Spezifikationen

Spezifikationen & Reinheit

≥99%

Biochemische und physiologische Mechanismen

Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC 50 s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+ influx and Ca 2+ cell overload.

Storage

Store at -20°C

Verschickt in

Ice chest + Ice pads

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Aktionsart

ACTIVATOR

Reinheit

≥99%

Namen und Kennungen

Kanonisches Lächeln

CC1CCC2C1C(C3(CC(C2(O3)C)OC(=O)CO)C(C)C)OC(=O)C=CC4=CC=CC=C4

IUPAC Name

[(1S,2R,5R,6R,7S,8R,10R)-10-(2-hydroxyacetyl)oxy-1,5-dimethyl-8-propan-2-yl-11-oxatricyclo[6.2.1.02,6]undecan-7-yl] (E)-3-phenylprop-2-enoate

InChIKey

GACOFEKSDCOVMV-RRYXBOBMSA-N

INCHI

1S/C26H34O6/c1-16(2)26-14-20(30-22(29)15-27)25(4,32-26)19-12-10-17(3)23(19)24(26)31-21(28)13-11-18-8-6-5-7-9-18/h5-9,11,13,16-17,19-20,23-24,27H,10,12,14-15H2,1-4H3/b13-11+/t17-,19-,20-,23-,24+,25+,26-/m1/s1

Isomere SMILES

C[C@@H]1CC[C@@H]2[C@@H]1[C@@H]([C@@]3(C[C@H]([C@]2(O3)C)OC(=O)CO)C(C)C)OC(=O)/C=C/C4=CC=CC=C4

PubChem CID

46242512

Molekulargewicht

442.54

Taxonomic Classification

Taxonomy Tree

• Kingdom Organic compounds
  • Superclass Lipids and lipid-like molecules
    • Klasse Prenol lipids
      • Subclass Sesquiterpenoids

• Kingdom: Organic compounds
• Superclass: Lipids and lipid-like molecules
• Klasse: Prenol lipids
• Subclass: Sesquiterpenoids
• Intermediate Tree Nodes: Not available
• Direct Parent: Sesquiterpenoids
• Alternative Parents: Cinnamic acid esters Styrenes Fatty acid esters Oxanes Dicarboxylic acids and derivatives Tetrahydrofurans Enoate esters Oxacyclic compounds Dialkyl ethers Primary alcohols Organic oxides Hydrocarbon derivatives Carbonyl compounds
• Molecular Framework: Aromatic heteropolycyclic compounds
• Substituents: Sesquiterpenoid - Cinnamic acid or derivatives - Cinnamic acid ester - Styrene - Fatty acid ester - Monocyclic benzene moiety - Dicarboxylic acid or derivatives - Fatty acyl - Oxane - Benzenoid - Alpha,beta-unsaturated carboxylic ester - Enoate ester - Tetrahydrofuran - Carboxylic acid ester - Organoheterocyclic compound - Oxacycle - Ether - Dialkyl ether - Carboxylic acid derivative - Primary alcohol - Organooxygen compound - Hydrocarbon derivative - Organic oxide - Carbonyl group - Alcohol - Organic oxygen compound - Aromatic heteropolycyclic compound
• Beschreibung: This compound belongs to the class of organic compounds known as sesquiterpenoids. These are terpenes with three consecutive isoprene units.
• External Descriptors: cinnamate ester - guaiane sesquiterpenoid - glycolate ester

Data sources

1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.

DOI: 10.1186/s13321-016-0174-y

Zugehörige Ziele (menschlich)

TRPC4 Tchem Short transient receptor potential channel 4 (0 Activities)

Discover Target: TRPC4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TRPC5 Tchem Short transient receptor potential channel 5 (0 Activities)

Discover Target: TRPC5

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

A498 (42825 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ACHN (49357 Activities)

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CAKI-1 (44928 Activities)

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RXF 393 (41971 Activities)

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SN12C (47755 Activities)

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TK-10 (45540 Activities)

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UO-31 (46270 Activities)

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786-0 (47912 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

TRPC5 Tchem Short transient receptor potential channel 5 (300 Activities)

Discover Target: TRPC5

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PRKD3 Tchem Protein kinase C (PKC) (1010 Activities)

Discover Target: PRKD3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Zugehörige Ziele (nicht menschlich)

Mus musculus (284745 Activities)

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Plasma (328 Activities)

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Wirkungsmechanismen

Chemische und physikalische Eigenschaften

• Molekulargewicht: 442.500 g/mol
• XLogP3: 4.800
• Hydrogen Bond Donor Count: 1
• Hydrogen Bond Acceptor Count: 6
• Rotatable Bond Count: 8
• Exact Mass: 442.236 Da
• Monoisotopic Mass: 442.236 Da
• Topological Polar Surface Area: 82.100 Ų
• Heavy Atom Count: 32
• Formal Charge: 0
• Complexity: 741.000
• Isotope Atom Count: 0
• Defined Atom Stereocenter Count: 7
• Undefined Atom Stereocenter Count: 0
• Defined Bond Stereocenter Count: 1
• Undefined Bond Stereocenter Count: 0
• The total count of all stereochemical bonds: 1
• Covalently-Bonded Unit Count: 1