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5.32978

PLD2 Inhibitor, ML395

Synonim(y):

PLD2 Inhibitor, ML395, Phosppolipase D2 inhibitor, VU0468809, ML-395

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Gabaryty przesyłkiSKUDostępnośćCena netto
10 mg
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979,00 zł

Informacje o tej pozycji

Wzór empiryczny (zapis Hilla):
C26H29N5O2
Numer CAS:
Masa cząsteczkowa:
443.54
MDL number:
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥97% (HPLC)
Form:
solid
Quality level:
Storage condition:
OK to freeze, protect from light

979,00 zł


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assay

≥97% (HPLC)

Quality Level

form

solid

potency

360 nM IC50

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, protect from light

color

off-white

solubility

DMSO: 50 mg/mL

storage temp.

2-8°C

General description

A cell permeable, triazaspirone derivative that acts as a highly potent, selective, and direct allosteric inhibitor of phospholipase D2 (PLD2; IC50 = 360 nM in exogenous biochemical assay). Exhibits >80-fold selectivity over phospholipase D1 (PLD1; IC50 = 30 µM). Shown to permeate the blood-brain barrier. Protects A549 cells from multiple strains of influenza virus when cells were pre-treated with this compound. Exhibits excellent DMPK profile (hepatic microsomal clearance = 82.1 ml/min/kg in Sprague-Dawley rats) and conforms to Lipinski′s rule and has favorable lipophilicity. Also displays favorable cytochrome P450 profile (CYP3A4 IC50 = 3.9 µM, CYP2D6 IC50 =16.4 µM, CYP1A2 IC50>30 µM, and CYP2C9 IC50>30 µM).
ML395 is a cell permeable, highly potent, selective, and direct allosteric inhibitor of phospholipase D2 (PLD2; IC₅₀ = 360 nM) that exhibits >80-fold selectivity over PLD1.

Biochem/physiol Actions

Primary Target
PLD2
Reversible: yes

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C).

Other Notes

O′Reilly, M.C., et al. 2014. ChemMedChem9, 2633.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)
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Ta pozycja
5282455.32910WH0005338M1
form

solid

form

powder

form

solid

form

buffered aqueous solution

assay

≥97% (HPLC)

assay

≥99% (HPLC)

assay

≥98% (HPLC)

assay

-

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

-

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

−20°C

storage temp.

−20°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, protect from light

storage condition

-


Klasa składowania

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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SKUNUMER GTIN
532978000104055977281972

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