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R-IMPP - 10mM in DMSO, high purity , CAS No.2133832-83-2

    Grade & Purity:
  • 10mM in DMSO
In stock
Item Number
R422578
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R422578-1ml
1ml
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$248.90

PCSK9 Inhibitors

Basic Description

Synonyms (R)-N-(isoquinolin-1-yl)-3-(4-methoxyphenyl)-N-(piperidin-3-yl)propanamide | PF-00932239
Specifications & Purity 10mM in DMSO
Biochemical and Physiological Mechanisms R-IMPP is an inhibitor of PCSK9 secretion, half maximal inhibitory concentration [IC50] = 4.8 μM.
Storage Temp Store at -80°C
Shipped In
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Product Description

Information

R-IMPP R-IMPP is an inhibitor of PCSK9 secretion, half maximal inhibitory concentration [IC50] = 4.8 μM.

Targets

PCSK9

In vitro

R-IMPP promotes uptake of LDL-C in hepatoma cells by increasing LDL-R levels, without altering levels of secreted transferrin. R-IMPP does not decrease PCSK9 transcription or increase PCSK9 degradation, but instead causes transcript-dependent inhibition of PCSK9 translation. R-IMPP is discovered that exhibited weak PCSK9 anti-secretagogue activity (half maximal inhibitory concentration [IC50] = 4.8 μM), but does not affect intracellular ATP levels in the recombinant CHO-K1 cells, a measure of cytotoxicity, nor decrease secretion of a control protein, secreted alkaline phosphatase, a measure of relative selectivity. The inhibitory response of R-IMPP is stereospecific.

Cell Research(from reference)

Cell lines:Huh7 cells 

Concentrations:10, 30 μM 

Incubation Time:24 h 

Product Properties

ALogP 3.684
HBD Count 1
Rotatable Bond 6

Associated Targets(Human)

KCNH2 Tclin HERG (29587 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PCSK9 Tclin Subtilisin/kexin type 9 (362 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Huh-7 (12904 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPSA Tbio 80S Ribosome (239 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

CHO-K1 (1115 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name N-isoquinolin-1-yl-3-(4-methoxyphenyl)-N-[(3R)-piperidin-3-yl]propanamide
INCHI InChI=1S/C24H27N3O2/c1-29-21-11-8-18(9-12-21)10-13-23(28)27(20-6-4-15-25-17-20)24-22-7-3-2-5-19(22)14-16-26-24/h2-3,5,7-9,11-12,14,16,20,25H,4,6,10,13,15,17H2,1H3/t20-/m1/s1
InChIKey OKTGXQMSOIQCTJ-HXUWFJFHSA-N
Smiles COC1=CC=C(C=C1)CCC(=O)N(C2CCCNC2)C3=NC=CC4=CC=CC=C43
Isomeric SMILES COC1=CC=C(C=C1)CCC(=O)N([C@@H]2CCCNC2)C3=NC=CC4=CC=CC=C43
PubChem CID 122198706
Molecular Weight 389.49

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Chemical and Physical Properties

DMSO(mg / mL) Max Solubility 77
DMSO(mM) Max Solubility 197.6944209
Water(mg / mL) Max Solubility 7
Water(mM) Max Solubility 17.97222008
Molecular Weight 389.500 g/mol
XLogP3 3.800
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 4
Rotatable Bond Count 6
Exact Mass 389.21 Da
Monoisotopic Mass 389.21 Da
Topological Polar Surface Area 54.500 Ų
Heavy Atom Count 29
Formal Charge 0
Complexity 520.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 1
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

Reviews

Customer Reviews

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